Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 1986 |
| CHEMBL ID | 20 |
| CHEBI ID | 27690 |
| SCHEMBL ID | 23219 |
| SCHEMBL ID | 11049053 |
| MeSH ID | M0000127 |
| Synonym |
|---|
| AC-12779 |
| BIDD:GT0643 |
| MLS001148438 |
| 5-acetamido-1,3,4-thiadiazole-2-sulfonamide |
| n-(5-sulfamoyl-[1,3,4]thiadiazol-2-yl)-acetamide |
| DIVK1C_000017 |
| KBIO1_000017 |
| CHEBI:27690 , |
| 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide |
| acetazolamidum |
| n-[5-(aminosulfonyl)-1,3,5-thiadiazol-2-yl]acetamide |
| 5-acetylamino-1,3,4-thiadiazole-2-sulfonamide |
| n-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]acetamide |
| defiltran |
| acetazolamida |
| ccris 5811 |
| 2-acetamido-5-sulfonamido-1,3,4-thiadiazole |
| nsc 145177 |
| acetamide, n-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)- |
| acetamide, n-(5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl)- |
| einecs 200-440-5 |
| hsdb 3002 |
| acetazolamidum [inn-latin] |
| acetazolamida [inn-spanish] |
| n-(5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl)acetamide |
| 5-acetamide-1,3,4-thiadiazole-2-sulfonamide |
| ai3-52458 |
| diuriwas |
| diureticum-holzinger |
| EU-0100039 |
| D00218 |
| acetazolamide (jp17/usp/inn) |
| SPECTRUM_000018 |
| SPECTRUM5_000738 |
| BPBIO1_000007 |
| PRESTWICK_4 |
| lopac-a-6011 |
| NCGC00015074-01 |
| NCGC00015074-02 |
| cas-59-66-5 |
| PRESTWICK3_000003 |
| PRESTWICK2_000003 |
| BSPBIO_000005 |
| BSPBIO_001788 |
| AB00051906 |
| C06805 |
| 59-66-5 |
| acetazolamide |
| 5-acetamide-1,4-thiadiazole-2-sulfonamide |
| dehydratin |
| edemox |
| didoc |
| wln: t5nn dsj cszw emv1 |
| 4-diamox |
| eumicton |
| fonurit |
| 2-acetamido-5-sulfonamido-1,4-thiadiazole |
| glaupax |
| 1,4-thiadiazole-2-sulfonamide, 5-acetamido- |
| glupax |
| nsc145177 |
| diacarb |
| donmox |
| acetozalamide |
| acetamidothiadiazolesulfonamide |
| acetazoleamide |
| duiramid |
| natrionex |
| vetamox |
| diluran |
| nephramid |
| diuramid |
| cidamex |
| acetazolamid |
| phonurit |
| diamox |
| diakarb |
| sk-acetazolamide |
| diutazol |
| carbonic anhydrase inhibitor no. 6063 |
| acetamox |
| nephramide |
| nsc-145177 |
| 1,3,4-thiadiazole-2-sulfonamide, 5-acetamido- |
| n-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide |
| acetazolamide, aza |
| 1YDA |
| acetazolamide, 5 |
| 2H4N |
| acetazolamide, azm |
| chembl20 , |
| aza2 |
| 1YDB |
| acerazolamide, aaz |
| 1ZSB |
| acetazolamide, aaz |
| 1YDD |
| DB00819 |
| bdbm10880 |
| acetazolamide (aaz) |
| NCGC00023455-07 |
| NCGC00023455-04 |
| NCGC00023455-05 |
| smr000058394 |
| MLS000028435 , |
| KBIOSS_000358 |
| KBIOGR_000558 |
| KBIO2_000358 |
| KBIO3_001288 |
| KBIO2_002926 |
| KBIO2_005494 |
| NINDS_000017 |
| SPBIO_000004 |
| SPECTRUM3_000284 |
| SPBIO_001926 |
| PRESTWICK0_000003 |
| PRESTWICK1_000003 |
| SPECTRUM4_000139 |
| SPECTRUM2_000082 |
| SPECTRUM1500102 |
| IDI1_000017 |
| LOPAC0_000039 |
| NCGC00023455-03 |
| NCGC00015074-03 |
| NCGC00023455-06 |
| acetazolamide, >=99%, powder |
| NCGC00015074-06 |
| HMS2091G05 |
| A 6011 , |
| 3CZV |
| NCGC00015074-11 |
| atenezo |
| l 579486 |
| AKOS000715163 |
| HMS500A19 |
| bzkpwhyzmxoidc-uhfffaoysa- |
| inchi=1/c4h6n4o3s2/c1-2(9)6-3-7-8-4(12-3)13(5,10)11/h1h3,(h2,5,10,11)(h,6,7,9) |
| HMS1920A05 |
| HMS1568A07 |
| NCGC00015074-10 |
| A832415 |
| n-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)ethanamide |
| HMS3259I13 |
| HMS2095A07 |
| HMS3260G19 |
| unii-o3fx965v0i |
| acetazolamide [usp:inn:ban:jan] |
| diamox sequels |
| glaumox |
| o3fx965v0i , |
| n-[5-(aminosulfonyl)-1,3,4-thiadiozol-2-yl]-acetamide |
| dtxsid7022544 , |
| tox21_302773 |
| NCGC00256374-01 |
| dtxcid002544 |
| tox21_201559 |
| NCGC00259108-01 |
| pharmakon1600-01500102 |
| nsc-755854 |
| nsc755854 |
| tox21_110078 |
| HMS2232G23 |
| S4506 |
| CCG-38900 |
| NCGC00015074-12 |
| NCGC00015074-07 |
| NCGC00015074-08 |
| NCGC00015074-04 |
| NCGC00015074-09 |
| NCGC00015074-05 |
| acetazolamine |
| atenezol |
| carbonic anhydrase inhibitor 6063 |
| acetamide, n-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]- |
| NCGC00015074-15 |
| LP00039 |
| 1JD0 |
| 3ML5 |
| 1AZM |
| HMS3370P01 |
| gtpl6792 |
| acetazolamide [inn] |
| acetazolamide [who-dd] |
| acetazolamide [ep monograph] |
| acetazolamide [usp monograph] |
| acetazolamide [mart.] |
| acetazolamide [usp-rs] |
| acetazolamide [jan] |
| acetazolamide [ep impurity] |
| acetazolamide [mi] |
| acetazolamidum [who-ip latin] |
| acetazolamide [vandf] |
| acetazolamide [orange book] |
| acetazolamide [who-ip] |
| acetazolamide [hsdb] |
| NC00491 |
| SCHEMBL23219 |
| 4G0C |
| 3DC3 |
| 2XTK |
| tox21_110078_1 |
| NCGC00015074-14 |
| 3UCJ |
| 2UY4 |
| 3HS4 |
| tox21_500039 |
| NCGC00260724-01 |
| CS-3568 |
| SCHEMBL11049053 |
| Q-200579 |
| Q-200580 |
| 5-acetamido-1,3,4-thiadiazol-2-sulfonamide |
| HY-B0782 |
| AB00051906_15 |
| OPERA_ID_288 |
| mfcd00003105 |
| acetazolamide, european pharmacopoeia (ep) reference standard |
| acetazolamide, analytical standard |
| Z277559108 |
| SR-01000000065-2 |
| sr-01000000065 |
| acetazolamide, united states pharmacopeia (usp) reference standard |
| acetazolamide for system suitability, european pharmacopoeia (ep) reference standard |
| SR-01000000065-4 |
| SR-01000000065-6 |
| SBI-0050028.P004 |
| HMS3712A07 |
| acetazolamide, pharmaceutical secondary standard; certified reference material |
| Q413690 |
| (1z)-n-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)ethanimidic acid |
| 124442-28-0 |
| AS-13169 |
| BRD-K43457670-001-22-9 |
| BRD-K43457670-001-26-0 |
| BCP29616 |
| SDCCGSBI-0050028.P005 |
| NCGC00015074-22 |
| AMY3289 |
| HMS3744A21 |
| D88526 |
| NCGC00015074-17 |
| EN300-119493 |
| CS-0694998 |
| HY-B0782R |
| acetazolamide (standard) |
| 1,3,4-thiadiazole-2-sulfonamide, 5-acetamido |
| acetazolamida (inn-spanish) |
| acetazolamidum (inn-latin) |
| carbonic anhydrase inhibitor no 6063 |
| acetazide |
| acetazolamide (ep monograph) |
| s01ec01 |
| 2-acetamido-1,3,4-thiadiazole-5-sulfonamide |
| acetazolamide (usp-rs) |
| acetazolamide extended-release |
| acetazolamide (ep impurity) |
| atenazol |
| acetazolamide (usp monograph) |
| acetazolamide (mart.) |
| acetazolamide (usp:inn:ban:jan) |
| n-(5-(aminosulfonyl)-1,3,5-thiadiazol-2-yl)acetamide |
Acetazolamide (AZA) is a carbonic anhydrase inhibitor (CAI) with neuroprotective effects. It has been used off-label for many years in the treatment of macular edema due to diabetes.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Acetazolamide is an old drug used as an antiepileptic agent, amongst other indications. " | ( Acetazolamide: Old drug, new evidence? Delanty, N; Dolan, E; Shukralla, AA, 2022) | 3.61 |
| "Acetazolamide (AZA) is a carbonic anhydrase inhibitor (CAI) with neuroprotective effects. " | ( The Protective Effects of Acetazolamide Against Homocysteine-Induced Blood-Brain-Barrier Disruption by Regulating the Activation of the Wnt/β-Catenin Signaling Pathway. Li, C; Zhang, B, 2022) | 2.46 |
| "Acetazolamide (ACZ), which is a CAI, is an active substance that has been used off-label for many years in the treatment of macular edema due to diabetes and many other diseases." | ( Ocular pharmacokinetics and toxicity of nanoparticular acetazolamide: In vivo distribution and safety of PHBV-ACZ nanoparticle. Akyol, M; Alçığır, ME; Arslan, A; Bakici, C; Batur, B; Ekim, O; Erdal, E; Salih, B; Uğurlu, N; Yaman, ME, 2023) | 1.88 |
| "Acetazolamide (AZL) is a carbonic anhydrase inhibitor that causes an increase in bicarbonate excretion and consequently urine alkalinisation." | ( Addition of low dose acetazolamide as an adjunct in patients undergoing high dose methotrexate is safe and beneficial. Bazargan, A; Ku, M; Tam, C, 2020) | 1.6 |
| "Acetazolamide is a carbonic anhydrase (CA) inhibitor sometimes used as a respiratory stimulant for patients with chronic obstructive pulmonary disease (COPD) with the goal of improving oxygenation, reducing carbon dioxide retention, and aiding liberation from mechanical ventilation and/or attempting to correct a metabolic alkalosis. " | ( Acetazolamide Use in Severe Chronic Obstructive Pulmonary Disease. Pros and Cons. Adamson, R; Swenson, ER, 2017) | 3.34 |
| "Acetazolamide is a treatment option for MME associated with ON but without an impact on the visual function." | ( Acetazolamide Reduces Retinal Inner Nuclear Layer Thickness in Microcystic Macular Edema Secondary to Optic Neuropathy. Abegg, M; Borruat, FX; Dysli, M; Voide, N, 2018) | 2.64 |
| "Acetazolamide is a carbonic anhydrase inhibitor typically used for indications including epilepsy, glaucoma, edema, and altitude sickness but it may be prescribed in hospitalized patients for off-label indications. " | ( Evaluating off-label uses of acetazolamide. Elefritz, JL; Van Berkel, MA, 2018) | 2.21 |
| "Acetazolamide is an option for hypochloremic metabolic alkalosis, but there are limited reports in children." | ( Acetazolamide in critically ill neonates and children with metabolic alkalosis. Andrews, MG; Harrison, DL; Johnson, PN; Lammers, EM; Miller, JL, 2013) | 3.28 |
| "Acetazolamide is a carbonic anhydrase inhibitor that is used to treat idiopathic intracranial hypertension, glaucoma, and epilepsy." | ( Possible association between acetazolamide administration during pregnancy and multiple congenital malformations. Al-Jobair, AM; Al-Saleem, AI, 2016) | 1.45 |
| "Acetazolamide is a medication commonly used to prevent acute mountain sickness, but it has an uncommon side effect of transient myopia." | ( Myopic Changes in a Climber after Taking Acetazolamide and the Use of Corrective Lenses to Temporize Symptoms: A Case Report from Mount Kilimanjaro. Hill, AD, 2016) | 1.42 |
| "Acetazolamide (AZM) is a carbonic anhydrase inhibitor, mainly used to reduce IOP in the treatment of glaucoma." | ( Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide. Allemandi, DA; Cruz, L; Ferreira, LM; Palma, SD; Quinteros, DA; Schaffazick, SR, 2016) | 1.39 |
| "Oral acetazolamide is a potent medical treatment for pediatric glaucoma, but ophthalmologists may have concerns that it retards weight gain in children and may choose surgical management instead." | ( The effect of oral acetazolamide on weight gain in children. Dupuis, A; Hébert, D; Levin, AV; Sharan, S, 2010) | 1.2 |
| "Acetazolamide is a common treatment but has never been examined in a randomised controlled trial." | ( A randomised controlled trial of treatment for idiopathic intracranial hypertension. Ball, AK; Burdon, MA; Clarke, CE; Davies, MB; Furmston, A; Howell, S; Howman, A; Jacks, AS; Lawden, M; Matthews, T; Sharrack, B; Sinclair, AJ; Sivaguru, A; Wheatley, K, 2011) | 1.09 |
| "Acetazolamide is a sulfonamide derivative and carbonic anhydrase inhibitor used to lower intraocular pressure in glaucomatous patients. " | ( Stevens-Johnson syndrome induced by acetazolamide. Her, Y; Kil, MS; Kim, CW; Kim, SS; Park, JH, 2011) | 2.09 |
| "Acetazolamide is a potent inhibitor of the reversible hydration of CO(2) catalyzed by the enzyme carbonic anhydrase and is commonly used to increase cerebral blood flow e.g. " | ( Enhancing effects of acetazolamide on neuronal activity correlate with enhanced visual processing ability in humans. Aamand, R; Fago, A; Møller, A; Roepstorff, A; Skewes, J, ) | 1.89 |
| "The acetazolamide is a known anti-resorptive agent, and its use as root canal dressing may increase the success rates in the treatment of root resorption." | ( Evaluation of the anti-resorptive ability of an experimental acetazolamide paste for the treatment of late replanted teeth: a study in rats. Castilho, LR; Mori, GG; Poi, WR, 2013) | 1.11 |
| "Acetazolamide (AZ) is an carbonic anhydrase inhibitor, which has been used in the treatment of seizures, mountain sickness and glaucoma. " | ( Acetazolamide impairs fear memory consolidation in rodents. Chien, WL; Fu, WM; Liou, HC; Lu, DH; Yang, MT, 2013) | 3.28 |
| "Acetazolamide (Ace) is a putative inhibitor of carbonic anhydrase (CA), an enzyme that catalyzes the equilibration of carbon dioxide and carbonic acid and plays a key role in HCO(3)(-) and water reabsorption and acid secretion. " | ( Influence of acetazolamide on AQP1 gene expression in testis and on sperm count/motility in epididymis of rats. Bai, Q; Koide, SS; Li, XJ; Sun, BM; Yu, HM, ) | 1.94 |
| "Acetazolamide is a mild diuretic and a respiratory stimulant. " | ( Acetazolamide improves central sleep apnea in heart failure: a double-blind, prospective study. Javaheri, S, 2006) | 3.22 |
| "Acetazolamide (AZ) is a carbonic anhydrase inhibitor with diuretic actions at the proximal tubule. " | ( Adenosine A1 receptor antagonist blunts urinary potassium excretion, but not renal hemodynamic effects, induced by carbonic anhydrase inhibitor in rats. Kost, CK; Zhou, X, 2006) | 1.78 |
| "Acetazolamide is a carbonic anhydrase inhibitor used topically for local secondary treatment of posttraumatic or postoperative edema." | ( [Contact dermatitis caused by acetazolamide under occlusion]. Daveluy, A; Haramburu, F; Marty, L; Miremont-Salamé, G; Moore, N; Vial, T, 2007) | 2.07 |
| "Acetazolamide (A) is a potent inhibitor of carbonic anhydrase. " | ( Effect of acetazolamide on normoxic and hypoxic exercise in humans at sea level. Bates, PW; Larson, EB; Pierson, DJ; Schoene, RB, 1983) | 2.11 |
| "Acetazolamide is a carbonic anhydrase inhibitor used for a variety of purposes, including adjunctively in the management of various types of epilepsy. " | ( Acetazolamide in bipolar affective disorders. Hayes, SG, 1994) | 3.17 |
| "Acetazolamide is a carbonic anhydrase inhibitor commonly used to reduce intraocular pressure (IOP). " | ( The pharmacokinetics of acetazolamide during CAPD. Blaustein, DA; Schwenk, MH; Wagner, JD, 1994) | 2.04 |
| "Acetazolamide is a beneficial adjunctive agent in the pharmacotherapy of epilepsy and should be considered in refractory epilepsy. " | ( Acetazolamide in the treatment of seizures. Oles, KS; Reiss, WG, 1996) | 3.18 |
| "Acetazolamide is known to be a potent cerebral vasodilator." | ( Cerebral blood flow reserve in patients with syndrome X. Brunelli, C; Caponnetto, S; Nobili, F; Olivotti, L; Rodriguez, G; Rossettin, P; Spallarossa, P, 1996) | 1.02 |
| "Acetazolamide is an efficient alternative for treatment of patients with respiratory acidosis and metabolic alkalosis, particularly when other more common measures in this condition (discontinuation of diuretics and/or volemic replacement) have failed or are contraindicated. " | ( [Efficacy of acetazolamide treatment of patients with hypercapnia and superimposed metabolic alkalosis]. Cancelo Suárez, P; del Portillo Rubí, A; Guillem Ares, E; Prada Mínguez, A; Prieto de Paula, JM; Sanz de la Fuente, H; Villamandos Nicás, V, 1997) | 2.11 |
| "Acetazolamide (Diamox) is a carbonic anhydrase inhibitor commonly used in patients with glaucoma in order to reduce intraocular pressure. " | ( Acute hemorrhagic gastritis associated with acetazolamide intoxication in a patient with chronic renal failure. Kitamura, M; Matsuo, K; Nakamoto, M; Nishihara, G; Nozoe, T; Takeda, K; Urabe, M; Yasunaga, C, 1997) | 2 |
| "Acetazolamide is a thiazide derivative clinically used in skeletal muscle disorders related to altered K+ homeostasis such as the periodic paralyses. " | ( Acetazolamide opens the muscular KCa2+ channel: a novel mechanism of action that may explain the therapeutic effect of the drug in hypokalemic periodic paralysis. Barbieri, M; Camerino, DC; Tricarico, D, 2000) | 3.19 |
| "The acetazolamide (AZA) test is a well-accepted method for measuring the vascular reactivity of the cerebral arteries. " | ( Cerebrovascular reactivity in patients under long-term acetazolamide treatment. Gadot, N; Kesler, A; Lampl, Y; Lorberboyn, M; Sadeh, M, 2002) | 1.12 |
| "Acetazolamide appears to be an acceptable treatment for occasional patients with myotonia who are unresponsive to or intolerant of other therapies." | ( Effects of acetazolamide on myotonia. Engel, WK; Griggs, RC; Moxley, RT; Riggs, JE, 1978) | 1.37 |
| "Acetazolamide is a weak diuretic used to decrease production of aqueous humor in the eye. " | ( Acetazolamide in hemodialysis patients: a rational use after ocular surgery. Dufresne, LR; Legault, L; Long, H; Morin, C; Roy, LF, 1992) | 3.17 |
| "Acetazolamide is a useful prophylactic for acute mountain sickness causing marked reduction in headache, nausea, vomiting, weakness, etc. " | ( Acetazolamide and high altitude diseases. Bradwell, AR; Imray, C; Winterborn, M; Wright, AD, 1992) | 3.17 |
| "Acetazolamide is a useful alternative, or an adjunct, to carbamazepine in the treatment of paroxysmal dystonia in CDD." | ( Acetazolamide treatment of paroxysmal dystonia in central demyelinating disease. Adams, RJ; Hess, DC; Huffnagle, VH; Sethi, KD, 1992) | 2.45 |
| "Acetazolamide is a potent cerebral vasodilator, and its administration combined with cerebral blood flow studies allows assessment of cerebral vasoreactivity." | ( Impaired cerebral vasoreactivity after embolization of arteriovenous malformations: assessment with serial acetazolamide challenge xenon CT. Durham, S; Hecht, ST; Horton, JA; Johnson, DW; Jungreis, CA; Pentheny, S; Tarr, RW; Yonas, H, ) | 1.07 |
| "Acetazolamide is a simple and effective method of achieving urinary alkalinisation with advantages over oral and intravenous bicarbonate." | ( Acetazolamide for alkalinisation of urine in patients receiving high-dose methotrexate. Earl, H; Shamash, J; Souhami, R, 1991) | 2.45 |
Acetazolamide has been shown to decrease blood pressure, improve arterial oxygenation and prevent high altitude periodic breathing in healthy volunteers ascending to high altitude. It has no positive effect in controlling CSF leak after dural opening/dural tear in adults who undergo spinal surgery.
Acetazolamide did not produce a natriuresis in the DIURESIS-CHF trial, and in ADVOR, immediate effects on symptoms and body weight were not reported, and the drug had no effect on morbidity or mortality after 90 days. Oral acetazolamide may cause poor weight gain in a small subset of children on treatment.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Acetazolamide did not produce a natriuresis in the DIURESIS-CHF trial, and in ADVOR, immediate effects on symptoms and body weight were not reported, and the drug had no effect on morbidity or mortality after 90 days." | ( Similarities and distinctions between acetazolamide and sodium-glucose cotransporter 2 inhibitors in patients with acute heart failure: Key insights into ADVOR and EMPULSE. Butler, J; Packer, M, 2023) | 1.9 |
| "Oral acetazolamide may cause poor weight gain in a small subset of children on treatment. " | ( The effect of oral acetazolamide on weight gain in children. Dupuis, A; Hébert, D; Levin, AV; Sharan, S, 2010) | 1.2 |
| "Acetazolamide can suppress the xenograft tumor growth by inhibiting the expression of AQP-1." | ( Acetazolamide inhibits aquaporin-1 expression and colon cancer xenograft tumor growth. Bin, K; Shi-Peng, Z, ) | 3.02 |
| "Acetazolamide can suppress tumor metastasis, at least in part, by inhibiting the expression of AQP1. " | ( Acetazolamide suppresses tumor metastasis and related protein expression in mice bearing Lewis lung carcinoma. Li, T; Li, XJ; Ma, B; Xiang, Y; Yu, HM, 2002) | 3.2 |
| "Acetazolamide induced an increase of the preretinal Po(2) to a greater extent when it was associated with carbogen breathing (DeltaPo(2) = 15.15 +/- 9.15 mm Hg; n = 7) than when it was combined with hyperoxia (DeltaPo(2) = 6.96 +/- 4.49 mm Hg; n = 7)." | ( Experimental retinal vein occlusion: effect of acetazolamide and carbogen (95% O2/5% CO2) on preretinal PO2. Munoz, JL; Petropoulos, IK; Pournaras, CJ; Pournaras, JA, 2004) | 1.3 |
| "Acetazolamide increase %FEPO4 in urine primarily by reducing deep nephron PO4 reabsorption." | ( Juxtamedullary and superficial nephron phosphate reabsorption in the cat. Goldfarb, S, 1980) | 0.98 |
| "Acetazolamide caused CBF to increase by 70.5-99.1% in Group B but only increase by 1.7-9.6% or paradoxically decrease in Group A." | ( Cerebral blood flow in normal brain tissue of patients with intracranial tumors. Kumate, S; Nakayama, Y; Tanaka, A; Yoshinaga, S, 1996) | 1.02 |
| "Acetazolamide caused an increase in passive permeability. " | ( Effects of acetazolamide on passive and active transport of fluorescein across the normal BRB. Larsen, M; Lund-Andersen, H; Moldow, B; Sander, B, 1999) | 2.14 |
| "Acetazolamide reduced the increase in pulmonary artery pressure (DeltaPAP) and the rate of pressure rise by approximately 30-50% during hypoxia and combined hypoxia/hypercapnia." | ( Acetazolamide reduces hypoxic pulmonary vasoconstriction in isolated perfused rabbit lungs. Deem, S; Hedges, RG; Kerr, ME; Swenson, ER, 2000) | 2.47 |
| "Acetazolamide can produce a small increase in arterial PO2 and fall in PCO2. " | ( Carbonic anhydrase inhibitors for hypercapnic ventilatory failure in chronic obstructive pulmonary disease. Greenstone, M; Jones, PW, 2001) | 1.75 |
| "Acetazolamide can produce severe lactic acidosis with an increased lactate-to-pyruvate ratio, ketosis with a low beta-hydroxybutyrate-to-acetoacetate ratio, and a urinary organic acid profile typical of pyruvate carboxylase deficiency. " | ( Pathogenic mechanism, prophylaxis, and therapy of symptomatic acidosis induced by acetazolamide. Bagnoli, F; Filippi, L; Margollicci, M; Rubaltelli, FF; Tronchin, M; Zammarchi, E, 2002) | 1.98 |
| "The acetazolamide-induced increase of cerebral blood flow could be reliably monitored by increase of cerebral 99mTc-HMPAO uptake, which varied between 11.4% and 47.6% in the less-affected hemisphere. " | ( 99mTc-HMPAO-SPECT with acetazolamide challenge to detect hemodynamic compromise in occlusive cerebrovascular disease. Fuchs, C; Knop, J; Siepmann, G; Thie, A; Zeumer, H, 1992) | 1.15 |
| "Acetazolamide does not inhibit ammonia secretion." | ( NH3 and NH4+ transport by rabbit renal proximal straight tubules. Burg, MB; Garvin, JL; Knepper, MA, 1987) | 0.99 |
Acetazolamide treatment in vivo inhibited about 50% of the calcium uptake during both pre-exuvial secretion and postexUVial reabsorption. Treatment did not have any negative skeletal effects, but could not mitigate the altitude-induced bone loss.
AZATAX was designed to establish whether acetazolamide is safe and improves cerebellar syndrome in PMM2-CDG. Patients should be informed of such adverse effects of intravenous acetazalamide administration prior to the acetazlamide challenge test for evaluation of cerebrovascular reactivity.
Acetazolamide is used to lower the IOP in patients undergoing continuous ambulatory peritoneal dialysis (CAPD) The developed method was successfully applied to the pharmacokinetic study of acetazolamic capsules after oral administration to beagle dogs.
The therapy of choice for prevention of CIN is controversial. The objective of the study was to investigate the efficacy of acetazolamide (AZA), candesartan (CAN), and triciribine (TCBN) in combination with the antifungal fluconazole.
| Excerpt | Reference | Relevance |
|---|---|---|
| "A cytological analysis of proliferating neoplasic and intestinal epithelium tissues of rats under the effect of cyclophosphane, 6-mercaptopurine, furosemide, diacarbum and of their combination with course-wise introduction was effected." | ( [Effect of diacarb and furosemide in combination with cytostatics on the mitotic activity of tumor and intestines of rats with sarcoma 45]. Aref'eva, AK; Pashinskiĭ, VG, ) | 0.13 |
| "Rubomycin or dipin in combination with diacarb had higher toxicity and antitumor activity as compared to administration of the cytostatic agents alone to mice with transplanted lymphosarcoma, strain L10-1." | ( [Toxicity and antitumor activity of the antibiotic rubomycin and dipin in combination with diuretics (diacarb)]. Stepanova, ES, 1976) | 0.26 |
| " Such cytostatic drugs as cyclophosphamide (alkylating agent) and 5-fluorouracil (antimetabolite) showed a significantly enhanced antitumor and metastation--preventing effect when used in combination with polyene antibiotic amphotericin B and a diuretic drug--diacarb." | ( [Potentiation of the selective antitumoral effect of cyclophosphamide and 5-fluorouracil by its combination with amphotericin B and diacarb]. Bychkov, IA; Iaremenko, KV; Pashinskiĭ, VG, 1986) | 0.27 |
| "In 39 selected patients with open-angle glaucoma, in whom pressure regulation with Timolol alone was inadequate, success was achieved by using this drug in combination with various other glaucoma drugs over treatment periods of 12 to 18 months." | ( [Timolol in combination with other glaucoma drugs (author's transl)]. Merkle, W, 1981) | 0.26 |
| " Drug-drug interactions are further implicated through this study." | ( Cerebral blood flow effects of sumatriptan in drug combinations in the baboon model. Dormehl, IC; Hugo, N; Oliver, DW, 1995) | 0.29 |
| "5%, or oral acetazolamide 250 mg when used alone or when dorzolamide is combined with either timolol or acetazolamide." | ( Effects on aqueous flow of dorzolamide combined with either timolol or acetazolamide. Camras, CB; Toris, CB; Yablonski, ME; Zhan, GL, 2004) | 0.94 |
| " Because the therapy of choice for prevention of CIN is controversial, in this study we compared the preventive efficacy of bicarbonate (Bi) infusion in dextrose water versus normal saline (NLS) infusion alone or in combination with oral acetazolamide (AZ)." | ( A comparison of sodium bicarbonate infusion versus normal saline infusion and its combination with oral acetazolamide for prevention of contrast-induced nephropathy: a randomized, double-blind trial. Adl, F; Hosseini, M; Kafi, M; Khajehdehi, P; Malekmakan, L; Nasab, MH; Nikoo, MH; Ostovan, MA; Pakfetrat, M; Roozbeh, J; Salari, S; Tabandeh, M; Vaziri, NM, 2009) | 0.75 |
| "In a double-blind and randomized clinical trial, all patients undergoing coronary angiography or percutaneous coronary intervention received NLS (NLS group), its combination with AZ (AZ group) or infusion of Bi (Bi group) before the procedures." | ( A comparison of sodium bicarbonate infusion versus normal saline infusion and its combination with oral acetazolamide for prevention of contrast-induced nephropathy: a randomized, double-blind trial. Adl, F; Hosseini, M; Kafi, M; Khajehdehi, P; Malekmakan, L; Nasab, MH; Nikoo, MH; Ostovan, MA; Pakfetrat, M; Roozbeh, J; Salari, S; Tabandeh, M; Vaziri, NM, 2009) | 0.57 |
| "The multiple drug interactions in which CAIs are involved should be carefully considered when such drugs are used in combination with the drug classes mentioned above, as the risks of developing toxicity and serious side effects if the dosages are not adjusted are high." | ( Drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors. Supuran, CT, 2016) | 0.43 |
The effect of CDs on the bioavailability of acetazolamide was assessed by measuring the intraocular pressure in rabbits. In order to enhance the ocular bioavailability, a multicomponent complex with hydroxypropyl-ss-cyclodextrin and triethanolamine was prepared.
| Excerpt | Reference | Relevance |
|---|---|---|
| " From the measured plasma levels, estimates of the bioavailability parameters (area under the plasma concentration versus time curve, time to peak plasma concentration, and peak plasm concentration) were obtained by least-squares digital computer fitting." | ( Bioavailability of acetazolamide tablets. Doluisio, JT; Frome, EL; Leonard, RG; Shah, AC; Yakatan, GJ, 1978) | 0.59 |
| " Production and absorption rate of the CSF were calculated after Pappenheimer and Heisey's equation." | ( [Production and absorption rate of cerebrospinal fluid in the spinal subarachnoid space of the dog (author's transl)]. Ishikawa, S; Kajikawa, H; Kimoto, T; Nosaka, K; Watanabe, K, 1976) | 0.26 |
| " These changes indicate a decreased absorption rate of endolymph in the endolymphatic sac." | ( Modulation of the endolymphatic sac function. Bagger-Sjöbäck, D; Harada, Y; Rask-Andersen, H; Takumida, M, 1991) | 0.28 |
| " Both cyclic GMP and dibutyryl cyclic GMP accelerated serum resorption by 23%, whereas cyclic AMP and dibutyryl cyclic AMP (both used with IBMX) decreased the absorption rate by 46%." | ( Metabolic influences on the absorption of serous subretinal fluid. Kawano, S; Marmor, MF, 1988) | 0.27 |
| " Adding cyclic AMP and related agents to the vitreous and subretinal space slowed down fluid absorption by 25%, whereas cyclic GMP analogues increased the rate of absorption by 33%." | ( Pharmacologic modification of subretinal fluid absorption in the rabbit eye. Marmor, MF; Negi, A, 1986) | 0.27 |
| " The Fel (fraction eliminated unchanged in urine) was calculated from the amount excreted in 36 h in urine and dose, assuming a bioavailability of 1 based on literature data." | ( Urinary excretion of acetazolamide in healthy volunteers after short- and long-term exposure to high altitude. Agrawal, MA; Arancibia, A; Lücker, PW; Paulos, C; Ritschel, WA; Wetzelsberger, KM, 1998) | 0.62 |
| " Clearance uncorrected for bioavailability (Cl/F) increased significantly in group HA compared with group L, and further increased in group HC." | ( Pharmacokinetics of acetazolamide in healthy volunteers after short- and long-term exposure to high altitude. Agrawal, MA; Arancibia, A; Lücker, PW; Paulos, C; Ritschel, WA; Wetzelsberger, KM, 1998) | 0.62 |
| " The effect of CDs on the bioavailability of acetazolamide was assessed by measuring the intraocular pressure in rabbits." | ( Cyclodextrins in acetazolamide eye drop formulations. Ammar, HO; El-Nahhas, SA; Khalil, RM, 1998) | 0.9 |
| " Detachment height was measured using a dual He-Ne beam YAG laser focusing system, and the fluid absorption rate was calculated before and after intravenous injections of saline, acetazolamide or benzolamide." | ( Inhibition of membrane-bound carbonic anhydrase enhances subretinal fluid absorption and retinal adhesiveness. Chiang, RK; Marmor, MF; Takeuchi, A; Wolfensberger, TJ, 2000) | 0.5 |
| " It has been reported to show little effect on the intraocular pressure (IOP) of human and rabbit eyes upon topical application, probably owing to its poor bioavailability and instability at pH >5." | ( Formulation and evaluation of ophthalmic preparations of acetazolamide. Kanwar, M; Kaur, IP; Singh, M, 2000) | 0.55 |
| " Median oral bioavailability was 25 +/- 6%." | ( Pharmacokinetics of acetazolimide after intravenous and oral administration in horses. Alberts, MK; Clarke, CR; Homer, LM; MacAllister, CG, 2000) | 0.31 |
| " Furthermore, the bioavailability of these derivatives in rabbits is comparable to that of acetazolamide, being in the range of 85-90%, showing them as promising candidates for systemically acting CA inhibitors." | ( Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. Scozzafava, A; Supuran, CT, 2002) | 0.54 |
| " Even though it has a poor solubility and penetration power, various studies mentioned in the review indicate that it is possible to successfully formulate topically effective ACZ by using: (i) high concentration of the drug, (ii) surfactant gel preparations of ACZ, (iii) ACZ loaded into liposomes, (iv) cyclodextrins to increase the solubility and hence bioavailability of ACZ, and (v) viscolyzers and other polymers either alone or in combination with cyclodextrins." | ( Acetazolamide: future perspective in topical glaucoma therapeutics. Aggarwal, D; Kapil, M; Kaur, IP; Smitha, R, 2002) | 1.76 |
| " To enhance the bioavailability of acetazolamide by the topical route and to improve the corneal permeability of the drug, niosomes of acetazolamide were prepared (employing span 60 and cholesterol) by different methods." | ( Development of a topical niosomal preparation of acetazolamide: preparation and evaluation. Aggarwal, D; Garg, A; Kaur, IP, 2004) | 0.85 |
| "Niosomes have been reported as a possible approach to improve the low corneal penetration and bioavailability characteristics shown by conventional ophthalmic vehicles." | ( Preparation and evaluation of reverse-phase evaporation and multilamellar niosomes as ophthalmic carriers of acetazolamide. Guinedi, AS; Hathout, RM; Mansour, S; Mortada, ND, 2005) | 0.54 |
| " The use of cyclodextrins to improve the solubility and bioavailability of poorly soluble drugs has however, rekindled an interest in acetazolamide (ACZ), because its poor solubility is one of the major factor responsible for its failure to show topical effectiveness." | ( Development of topically effective formulations of acetazolamide using HP-beta-CD-polymer co-complexes. Aggarwal, D; Kapil, M; Kaur, IP; Smitha, R, 2004) | 0.78 |
| " In order to enhance the bioavailability of acetazolamide by topical route and to improve the corneal permeability of the drug, the niosomes of acetazolamide were prepared (by reverse phase evaporation method) and coated with Carbopol for the latter's bioadhesive effect." | ( Study of the extent of ocular absorption of acetazolamide from a developed niosomal formulation, by microdialysis sampling of aqueous humor. Aggarwal, D; Kaur, IP; Mitra, AK; Pal, D, 2007) | 0.86 |
| "In order to enhance the ocular bioavailability of acetazolamide (ACZ), a multicomponent complex with hydroxypropyl-ss-cyclodextrin (HP-ss-CD) and triethanolamine (TEA) was prepared to be applied topically." | ( An efficient ternary complex of acetazolamide with HP-ss-CD and TEA for topical ocular administration. Allemandi, DA; Granero, GE; Longhi, MR; Palma, SD; Quinteros, D; Tartara, LI, 2009) | 0.89 |
| "The ACZ:HP-beta-CD:TEA complex is an important new approach to improve the ocular bioavailability of this drug." | ( Promising complexes of acetazolamide for topical ocular administration. Granero, GE; Longhi, MR, 2010) | 0.67 |
| "The incorporation of AZM in coagels seems to improve the ocular bioavailability of this drug." | ( Improvement of acetazolamide ocular permeation using ascorbyl laurate nanostructures as drug delivery system. Allemandi, DA; Palma, SD; Quinteros, DA; Saino, V; Tártara, LI, 2012) | 0.73 |
| " Objective of the present study is to increase the topical ocular bioavailability and to sustain the release of drug for longer time." | ( Development, in vitro and in vivo characterization of Eudragit RL 100 nanoparticles for improved ocular bioavailability of acetazolamide. Gupta, RN; Jha, AK; Pandey, R; Verma, P, ) | 0.34 |
| " Our results suggest that carbosilane dendrimers can be used in a safe range of concentrations to enhance the bioavailability of drugs topically administered in the eye." | ( Novel Water-Soluble Mucoadhesive Carbosilane Dendrimers for Ocular Administration. Andrés-Guerrero, V; Argüeso, P; Bravo-Osuna, I; de la Mata, FJ; de Las Heras, B; Gómez, R; Guzmán-Navarro, M; Herrero-Vanrell, R; Molina-Martínez, IT; Ponchel, G; Sánchez-Nieves, J; Vicario-de-la-Torre, M, 2016) | 0.43 |
| " EC508 might offer significant advantages in indications like fertility control and HRT based on its high oral bioavailability and lack of hepatic estrogenicity." | ( A prodrug design for improved oral absorption and reduced hepatic interaction. Ahmed, G; Elger, W; Meece, F; Nair, HB; Nickisch, K; Schneider, B; Wyrwa, R, 2017) | 0.46 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| " Moreover, it suffers from poor aqueous solubility and low corneal permeability limiting its ocular bioavailability and its use topically." | ( Novel cubosome based system for ocular delivery of acetazolamide. El Sorogy, HM; Khalil, IA; Teba, HE, 2021) | 0.87 |
| "We earlier reported that coating poorly water-soluble drugs with nano-hydroxyapatite (nano-HAP) improves bioavailability after oral administration." | ( Nano-hydroxyapatite improves intestinal absorption of acetazolamide (BCS Class IV drug)-but how? Hayman, R; Kaneko, K; Miyasaka, R, 2022) | 0.97 |
| " The most active compounds showed good bioavailability and drug likeness scores." | ( Substituted furan sulfonamides as carbonic anhydrase inhibitors: Synthesis, biological and in silico studies. Angeli, A; Geronikaki, A; Kartsev, V; Komogortsev, A; Lichitsky, B; Petrou, A; Supuran, CT, 2023) | 0.91 |
| " The low solubility and bioavailability of ACZ limit its use in the treatment of DME." | ( Ocular pharmacokinetics and toxicity of nanoparticular acetazolamide: In vivo distribution and safety of PHBV-ACZ nanoparticle. Akyol, M; Alçığır, ME; Arslan, A; Bakici, C; Batur, B; Ekim, O; Erdal, E; Salih, B; Uğurlu, N; Yaman, ME, 2023) | 1.16 |
Acetazolamide is used to treat transient intraocular pressure (IOP) elevation. In treated WB/ReJ fetuses, the probability of expression of edema is independent of the expression of forelimb ectrodactyly. There is no significant increase in acetazolamide-induced resorption.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The dose-response curve for acetazolamide showed that the I50 for inhibition of JtCO2 was 4 microM." | ( Carbonic anhydrase-dependent bicarbonate reabsorption in the rat proximal tubule. Lucci, MS; Rector, FC; Warnock, DG, 1979) | 0.55 |
| " Since calculation of the uncatalyzed hydration of CO2 or dehydration of HCO3-in tissues involves some uncertainty, these rates are generally best defined by studying the dose-response curves of inhibitors and observing the residual activity after full inhibition." | ( Use of inhibitors in physiological studies of carbonic anhydrase. Maren, TH, 1977) | 0.26 |
| " An injection of over 150 micro U of vasopressin lowered ICP, but there was no clear dose-response relationship of the effect of vasopressin on ICP." | ( Effect of vasopressin on intracranial pressure of rabbit. Nagawa, Y; Nakajima, T; Noto, T; Saji, Y, 1978) | 0.26 |
| " Saliva to plasma ratios were consistent for any given individual and, therefore, offer a means of monitoring drug dosage without resorting to frequent blood sampling." | ( GLC analysis of acetazolamide in blood, plasma, and saliva following oral administration to normal subjects. Riegelman, S; Shah, VP; Wallace, SM, 1977) | 0.6 |
| "A dimensionless parameter, the dosage form index (DLtau) is proposed for evaluating the performance of drug delivery systems." | ( Dosage form index: an objective criterion for evaluation of controlled-release drug delivery systems. Bayne, W; Theeuwes, F, 1977) | 0.26 |
| " The method was developed to study plasma level profiles of different dosage forms of acetazolamide." | ( Assay for acetazolamide in plasma. Bayne, WF; Crisologo, N; Rogers, G, 1975) | 0.88 |
| " At this dosage similar increases in renal excretion were obtained with either drug." | ( Tissue electrical admittance (electrolyte concentration) in rat renal medulla: effects of furosemide and acetazolamide. Badzyńska, B; Kompanowska-Jezierska, E; Sadowski, J, 1990) | 0.49 |
| " The dose-response analysis is not interpretable in the WB/ReJ and C57BL/6J strains and their reciprocal F1 fetuses because there was significant response only at the highest dose (2,000 mg/kg) used in this study." | ( Time-response and dose-response to acetazolamide in the WB/ReJ and C57BL/6J mouse strains: genetic interaction in the ectrodactyly response. Biddle, FG; Eales, BA; Mulholland, LR, 1991) | 0.56 |
| " In treated WB/ReJ fetuses, the probability of expression of edema is independent of the expression of forelimb ectrodactyly and, with the dosage regime, there is no significant increase in acetazolamide-induced resorption." | ( Genetically determined transient edema found in the WB/ReJ mouse strain in a teratogenic survey with acetazolamide. Biddle, FG, 1990) | 0.69 |
| " We deem the initial dosage of 16 mg Millicorten/day to be therapeutically effective and adequate." | ( [Pseudotumor cerebri in pregnancy]. Benz, J; Zeller, R, 1990) | 0.28 |
| "Two oral liquid dosage forms of acetazolamide have been developed." | ( Development of oral liquid dosage forms of acetazolamide. Das Gupta, V; Parasrampuria, J, 1990) | 0.83 |
| " These preformulation studies can be used to develop a stable oral liquid dosage form of acetazolamide." | ( Preformulation studies of acetazolamide: effect of pH, two buffer species, ionic strength, and temperature on its stability. Gupta, VD; Parasrampuria, J, 1989) | 0.8 |
| " Dosage and time effects were also determined." | ( Intraocular pressure effects of carbonic anhydrase inhibitors in primary open-angle glaucoma. Lichter, PR; Medzihradsky, F; Musch, DC; Standardi, CL, 1989) | 0.28 |
| " A dosage of 500 mg/d was found to be more effective than 250 mg/d." | ( Acetazolamide for treatment of chronic macular edema in retinitis pigmentosa. Fiscella, RG; Fishman, GA; Gilbert, LD; Jampol, LM; Kimura, AE, 1989) | 1.72 |
| " Although a carbonic anhydrase inhibitor, such as acetazolamide which is frequently used in patients with glaucoma or with metabolic alkalosis, is known to impair the CO2 elimination in the lungs, the dose-response curve of CO2 elimination with acetazolamide has not been well documented in CO2 homeostasis." | ( Disturbance of CO2 elimination in the lungs by carbonic anhydrase inhibition. Mizuno, K; Takahashi, N; Taki, K; Wakusawa, R, 1986) | 0.52 |
| " A dosage of acetazolamide for normalizing metabolic alkalemia has not yet been experimentally determined." | ( Management of acid-base balance with red blood cell carbonic anhydrase (RCA). II. Control of acid-base balance with acetazolamide. Mizuno, K; Takahashi, N; Taki, K; Wakusawa, R, 1987) | 0.85 |
| " One strain, SJL/J, exhibited maternal toxicity to the dosage regime and was excluded from the survey." | ( Genetic differences in the frequency of acetazolamide-induced ectrodactyly in the mouse exhibit directional dominance of relative embryonic resistance. Biddle, FG, 1988) | 0.54 |
| " Dose-response studies with acetazolamide revealed that the protection did not correlate with the inhibition of carbonic anhydrase in the rat gastric mucosa." | ( Gastric mucosal protection by acetazolamide derivatives: role of carbonic anhydrase and sulfhydryls. Kusterer, K; Szabo, S, 1987) | 0.86 |
| "We have demonstrated previously that phenylephrine, a selective postsynaptic alpha-1-adrenergic agonist, significantly potentiates the incidence of acetazolamide-induced right forelimb ectrodactyly in a dose-response manner." | ( Reduction of uterine blood flow by phenylephrine, an alpha-adrenergic agonist, in the day 11 pregnant rat: relationship to potentiation of acetazolamide teratogenesis. Scott, WJ; Ugen, KE, 1987) | 0.67 |
| "Two elderly patients, who were chronically receiving aspirin, developed lethargy, incontinence, and confusion after dosing with acetazolamide." | ( Toxic interaction between acetazolamide and salicylate: case reports and a pharmacokinetic explanation. Brandt, JL; Chapron, DJ; Feig, PU; Gomolin, IH; Kramer, PA; Sweeney, KR, 1986) | 0.78 |
| "2 per cent) who complied with drug dosage instructions." | ( Oral acetazolamide in Menière's disease. Booth, JB; Brookes, GB, 1984) | 0.78 |
| " Monitoring acetazolamide concentrations may be useful in adjusting dosage and preventing toxicity in patients with decreased renal function." | ( Chronic acetazolamide intoxication. Clementi, WA; Garrelts, JC; Garriott, JC; McLemore, TL; Watson, WA; Zinn, PD, ) | 0.94 |
| " The dosage of PGE2 utilized was free of excretory or hemodynamic effects." | ( Interference by prostaglandin E2 with the phosphaturic effects of nonhormonal agents. Dominguez, JH; Pitts, TO; Puschett, JB, 1984) | 0.27 |
| " The dose-response relationship for rats was determined." | ( Addition of the effects of norepinephrine and acetazolamide to decrease formation of cerebrospinal fluid. Godman, DR; Vogh, BP, 1984) | 0.53 |
| " Dosage guidelines and formulation procedures are described in the paper, as are other possible therapeutic alternatives (dialysis, acetazolamide, cimetidine)." | ( Treating severe metabolic alkalosis. Martin, WJ; Matzke, GR, ) | 0.34 |
| " Coadministration of acetazolamide with 14C-labeled indapamide to rats, resulted in a 5-fold drop in the blood levels of total radioactivity, relative to rats dosed with [14C]indapamide alone." | ( Effects of competitive red blood cell binding and reduced hematocrit on the blood and plasma levels of [14C]Indapamide in the rat. Lettieri, JT; Portelli, ST, 1983) | 0.58 |
| "Plasma acetazolamide concentrations were determined enzymatically after administration of three tablet dosage forms and a reference solution to 12 human subjects in a crossover study." | ( Relative bioavailability of acetazolamide tablets. Gollamudi, R; Meyer, MC; Straughn, AB, ) | 0.88 |
| " Other than switching drugs to reduce CAI side effects, one can try reduced dosages, a gradual dosage increase, and patience." | ( Reducing side effects of carbonic anhydrase inhibitors. Lichter, PR, 1981) | 0.26 |
| " The suitability of the method for pharmacokinetic studies was verified in a normal volunteer dosed with 250-mg (solution) and 500-mg (sustained-release tablet) acetazolamide formulations." | ( Quantitation of acetazolamide in plasma by high-performance liquid chromatography. Brien, R; Hossie, RD; Mousseau, N; Sved, S, 1980) | 0.8 |
| " In order to test the validity of FEAD as an absence seizure model, the present experiments determined dose-response relationships for the suppression of FEAD by six antiepileptic drugs with established clinical profiles." | ( Flash-evoked afterdischarge in rat as a model of the absence seizure: dose-response studies with therapeutic drugs. Burnham, WM; King, GA; Livingston, KE, 1980) | 0.26 |
| " The agent should be avoided in patients receiving dialysis unless the dosage is reduced and serum concentration monitoring can be performed in a timely manner." | ( Acetazolamide toxicity and pharmacokinetics in patients receiving hemodialysis. Meese, MG; Schwenk, MH; Singhal, PC; St Peter, WL, ) | 1.57 |
| " Serum acetazolamide concentrations were measured prior to a 250 mg oral dose and 12 additional times during a 24-h dosing interval." | ( The pharmacokinetics of acetazolamide during CAPD. Blaustein, DA; Schwenk, MH; Wagner, JD, 1994) | 1.05 |
| " We examine the relationship between expressivity and penetrance using right and left forelimb data from a previously reported dose-response analysis of the C57BL/6J and WB/ReJ strains to acetazolamide." | ( Penetrance and expressivity of acetazolamide-ectrodactyly provide a method to define a right-left teratogenic gradient that differs between the C57BL/6J and WB/ReJ mouse strains. Biddle, FG; Eales, BA; Mulholland, LR, 1993) | 0.76 |
| "The stability of drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied." | ( Stability of acetazolamide, allopurinol, azathioprine, clonazepam, and flucytosine in extemporaneously compounded oral liquids. Allen, LV; Erickson, MA, 1996) | 0.66 |
| "To clarify the effect of the clinical dosage of acetazolamide on growth in children with epilepsy or febrile convulsion, the standard scores of height and weight in 17 subjects receiving acetazolamide as an adjunct to unchanged monotherapy of antiepileptic drug were compared longitudinally through four phases: before antiepileptic drug administration, with monotherapy of antiepileptic drug, with acetazolamide in addition to monotherapy, and after acetazolamide discontinuation." | ( Growth suppression in children receiving acetazolamide with antiepileptic drugs. Abe, J; Futagi, Y; Otani, K, 1996) | 0.82 |
| "To characterize the pharmacokinetics and pharmacodynamics of acetazolamide in patients with transient intraocular pressure (IOP) elevation and to provide individual patients with the optimal dosage regimen for this drug." | ( Pharmacokinetics and pharmacodynamics of acetazolamide in patients with transient intraocular pressure elevation. Honda, Y; Inatani, M; Inui, K; Ogura, Y; Takano, M; Takayama, A; Tanihara, H; Yano, I, 1998) | 0.81 |
| " The dosage regimen presented in this study is expected to improve the benefits of acetazolamide pharmacotherapy in most elderly patients with transient rises in IOP following intraocular surgery." | ( Pharmacokinetics and pharmacodynamics of acetazolamide in patients with transient intraocular pressure elevation. Honda, Y; Inatani, M; Inui, K; Ogura, Y; Takano, M; Takayama, A; Tanihara, H; Yano, I, 1998) | 0.79 |
| " Based on these observations, it is suggested that patients travelling to high altitude, especially altitudes above 4,000 m, should be closely monitored and acetazolamide dosage adjusted as necessary." | ( Pharmacokinetics of acetazolamide in healthy volunteers after short- and long-term exposure to high altitude. Agrawal, MA; Arancibia, A; Lücker, PW; Paulos, C; Ritschel, WA; Wetzelsberger, KM, 1998) | 0.82 |
| "To compare two dosing regimens of acetazolamide for the reversal of metabolic alkalosis in mechanically ventilated patients with asthma or chronic obstructive pulmonary disease." | ( Single versus multiple doses of acetazolamide for metabolic alkalosis in critically ill medical patients: a randomized, double-blind trial. Devlin, JW; Iannuzzi, MC; Jankowski, MA; Mazur, JE; Peters, MJ; Zarowitz, BJ, 1999) | 0.87 |
| " By using generalized estimating equation techniques, no difference was found between the two dosing regimens at any point over the study period for serum bicarbonate, serum potassium, or urine chloride end points." | ( Single versus multiple doses of acetazolamide for metabolic alkalosis in critically ill medical patients: a randomized, double-blind trial. Devlin, JW; Iannuzzi, MC; Jankowski, MA; Mazur, JE; Peters, MJ; Zarowitz, BJ, 1999) | 0.59 |
| "Groups of pigmented rabbits, six in each group, were dosed during 10 weeks with one of the substances under investigation, and one untreated group was the control." | ( Biochemical and ultrastructural changes in rabbit sclera after treatment with 7-methylxanthine, theobromine, acetazolamide, or L-ornithine. Kobayashi, T; Olsen, EB; Ribel-Madsen, SM; Trier, K, 1999) | 0.52 |
| " To investigate whether the usually applied standard dose of 1 g intravenously will guarantee stable test conditions, the dose-response relationship of AA on cerebral blood flow (CBF) and cerebral blood flow velocity (CBFV) in normal subjects was determined." | ( The dose-response relationship of acetazolamide on the cerebral blood flow in normal subjects. Grossmann, WM; Koeberle, B, ) | 0.41 |
| " The first CBF measurement was taken at rest, the second 15 min after application of AA at a dosage of 5, 10, 13, 15 and 18 mg/kg of body weight, respectively." | ( The dose-response relationship of acetazolamide on the cerebral blood flow in normal subjects. Grossmann, WM; Koeberle, B, ) | 0.41 |
| "A significant dosage dependence of AA on the CBF (fast flow and initial slope index) exists between 5 and 18 mg/kg intravenously." | ( The dose-response relationship of acetazolamide on the cerebral blood flow in normal subjects. Grossmann, WM; Koeberle, B, ) | 0.41 |
| "For the determination of CVR of CBF with AA, a dosage related to body weight is required." | ( The dose-response relationship of acetazolamide on the cerebral blood flow in normal subjects. Grossmann, WM; Koeberle, B, ) | 0.41 |
| " Stone prevention is based on drug withdrawal or change in dosage with additional measures including an increase of diuresis and, if necessary, changes in the urine pH." | ( [Drug-induced urinary calculi in 1999]. Daudon, M, 1999) | 0.3 |
| " Responses to AZ were compared in women with different types of epilepsy and comparing continuous versus intermittent dosing using Fisher's exact tests." | ( Acetazolamide in women with catamenial epilepsy. Foldvary, N; Lee, J; Lim, LL; Mascha, E, 2001) | 1.75 |
| "In vitro experiments followed the effect of the two substances at concentrations between 10(-8)-10(-4) M on purified human red cell CA I and II as well as on human gastric mucosa CA IV using dose-response relationships." | ( Indomethacin activates carbonic anhydrase and antagonizes the effect of the specific carbonic anhydrase inhibitor acetazolamide, by a direct mechanism of action. Baican, M; Coltau, M; Domuta, G; Hecht, A; Ifrim, M; Maghiar, T; Puscas, I, 2001) | 0.52 |
| " A daily dose of 10mg/kg of AZA was first administered and then the dosage was increased up to 20mg/kg based on the clinical response and side effects." | ( Long-term effectiveness and side effects of acetazolamide as an adjunct to other anticonvulsants in the treatment of refractory epilepsies. Katayama, F; Miura, H; Takanashi, S, 2002) | 0.58 |
| " Acetazolamide dosage was given while the patients underwent an immunosuppressive regimen." | ( Pseudotumor cerebri in two adolescents with acquired aplastic anemia. Bhakta, M; Helton, K; Jeng, MR; Rieman, M; Wang, WC, 2002) | 1.22 |
| " Excessive drowsiness can be avoided by proper dosage and proper timing of drug administration." | ( Treatment of epilepsy. BAILEY, AA, 1963) | 0.24 |
| " A 1-week washout period was observed between dosing periods." | ( Effect of perindopril on cerebral vasomotor reactivity in patients with lacunar infarction. Lees, K; Muir, S; Shah, I; Walters, M, 2004) | 0.32 |
| " Dosing with perindopril did not affect resting cerebral blood flow velocity (percent change from baseline +3." | ( Effect of perindopril on cerebral vasomotor reactivity in patients with lacunar infarction. Lees, K; Muir, S; Shah, I; Walters, M, 2004) | 0.32 |
| "Fifty-two eyes (45 patients) with chronic uveitic CME were treated with acetazolamide at an initial dosage of 500 mg/d." | ( Long-term effect of acetazolamide treatment of patients with uveitic chronic cystoid macular edema is limited by persisting inflammation. Bornfeld, N; Heiligenhaus, A; Jurklies, B; Laube, T; Schilling, H, ) | 0.69 |
| " Dose-response relations for PGE2 and subtype receptors EP1/EP3 (sulprostone), EP2 (butaprost), and EP4 (1-OH PGE1) were assessed by cumulated doses of single agonists." | ( Duodenal secretion in humans mediated by the EP4 receptor subtype. Bindslev, N; Hansen, MB; Larsen, R, 2005) | 0.33 |
| " This study aimed to determine whether acetazolamide is effective at dosing relevant to human use at high altitude and to investigate whether its efficacy against hypoxic pulmonary vasoconstriction is dependent on carbonic anhydrase inhibition by testing other potent heterocyclic sulfonamide carbonic anhydrase inhibitors." | ( Pulmonary vasodilation by acetazolamide during hypoxia is unrelated to carbonic anhydrase inhibition. Boemke, W; Francis, RC; Höhne, C; Pickerodt, PA; Swenson, ER, 2007) | 0.91 |
| "Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing acetazolamide are reviewed." | ( Biowaiver monographs for immediate release solid oral dosage forms: acetazolamide. Barends, DM; Becker, C; Dressman, JB; Granero, GE; Junginger, HE; Kopp, S; Longhi, MR; Midha, KK; Shah, VP; Stavchansky, S, 2008) | 0.77 |
| " The optimal dosing of AmB remains unclear." | ( Treatment of acute cryptococcal meningitis in HIV infected adults, with an emphasis on resource-limited settings. Dedicoat, M; Dlamini, S; Paul, N; Sloan, D, 2008) | 0.35 |
| " This treatment has to be continued for at least several months and decreasing the dosage must be progressive." | ( [Benign intracranial hypertension: the role of medical treatment]. Defoort, S; Dhellemmes, P; Vinchon, M, 2008) | 0.35 |
| " The determination was done for an active pharmaceutical ingredient, its pharmaceutical dosage form in the presence of degradation products, and its process-related impurities." | ( A validated stability-indicating LC method for acetazolamide in the presence of degradation products and its process-related impurities. Srinivasu, P; Subbarao, DV; Sudhakar Babu, K; Vegesna, RV, 2010) | 0.62 |
| "ACET used at the dosage of 500 mg per day reduces metabolic alkalosis but has no benefit in terms of improving PaCO(2) or respiratory parameters in weaning COPD patients from mechanical ventilation." | ( Effectiveness of acetazolamide for reversal of metabolic alkalosis in weaning COPD patients from mechanical ventilation. Fagon, JY; Faisy, C; Mokline, A; Sanchez, O; Tadié, JM, 2010) | 0.7 |
| " Acetazolamide induced a decrease in serum bicarbonate with a dose-response relationship." | ( Population pharmacodynamic model of bicarbonate response to acetazolamide in mechanically ventilated chronic obstructive pulmonary disease patients. Faisy, C; Heming, N; Urien, S, 2011) | 1.52 |
| "This study identified several covariates that influenced acetazolamide pharmacodynamics and could allow a better individualization of acetazolamide dosing when treating COPD patients with metabolic alkalosis." | ( Population pharmacodynamic model of bicarbonate response to acetazolamide in mechanically ventilated chronic obstructive pulmonary disease patients. Faisy, C; Heming, N; Urien, S, 2011) | 0.86 |
| " Targeting of multiple mechanisms in combination therapies has proven effective both clinically and commercially although potential improvements with regards to efficacy, tolerability and dosing frequency remain." | ( A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma. Frieman, B; Hegde, SS; Hill, CM; Jiang, L; Kintz, S; Long, DD; Marquess, DG; Purkey, H; Shaw, JP; Steinfeld, T; Wilson, MS; Wrench, K, 2013) | 0.39 |
| "The aim of this study was to develop sustained release dosage forms of acetazolamide (ACZ) preparing its calcium alginate beads and matrix tablets." | ( Preparation and evaluation of sustained release calcium alginate beads and matrix tablets of acetazolamide. Adibkia, K; Bairami-Atashgah, R; Barzegar-Jalali, M; Ghanbarzadeh, S; Hanaee, J; Omidi, Y; Ziaee, S, 2013) | 0.84 |
| " The data show that a low prophylactic dosage of acetazolamide, but not gingko biloba, mitigates the early increase of PASP in a quick ascent profile." | ( Effect of acetazolamide and gingko biloba on the human pulmonary vascular response to an acute altitude ascent. Chen, J; Chen, Y; Hu, Y; Ke, T; Liu, M; Luo, W; Shen, X; Swenson, ER; Wang, J; Yang, Q; Zhang, W; Zhang, X; Zhao, F, 2013) | 1.05 |
| "In vitro studies were used for the dose-response (AlamarBlue) effects of acetazolamide (AZ) and sulforaphane (SFN) on clonogenicity, serotonin-induced growth effect and serotonin content (LC-MS) on H-727 (TC) and H-720 (AC) bronchial carcinoid cell lines and their derived NOD/SCID mice subcutaneous xenografts." | ( Combination of carbonic anhydrase inhibitor, acetazolamide, and sulforaphane, reduces the viability and growth of bronchial carcinoid cell lines. Adeli, K; Cutz, E; Islam, SS; Kumar, S; Mokhtari, RB; Yazdanpanah, M; Yeger, H, 2013) | 0.88 |
| "This is the first study to evaluate acetazolamide dosing for metabolic alkalosis in children with and without cardiac disease." | ( Acetazolamide in critically ill neonates and children with metabolic alkalosis. Andrews, MG; Harrison, DL; Johnson, PN; Lammers, EM; Miller, JL, 2013) | 2.11 |
| " Finally, we demonstrate that systemic administration of acetazolamide to rats with PNI produces an antiallodynic effect by itself and an enhancement of the peak analgesic effect with a change in the shape of the dose-response curve of the α1-sparing benzodiazepine L-838,417." | ( Inhibition of carbonic anhydrase augments GABAA receptor-mediated analgesia via a spinal mechanism of action. Asiedu, MN; Hübner, CA; Kaila, K; Mejia, GL; Price, TJ, 2014) | 0.65 |
| " Simulations indicated that higher acetazolamide dosage (>1000 mg daily) was required to significantly increase minute ventilation (P<." | ( Population pharmacodynamic modeling and simulation of the respiratory effect of acetazolamide in decompensated COPD patients. Clavel, M; Faisy, C; Fulda, V; Gacouin, A; Heming, N; Meziani, F; Planquette, B; Urien, S, 2014) | 0.91 |
| "Low-sodium weight-reduction diet plus the maximally tolerated dosage of acetazolamide (up to 4 g/d) or matching placebo for 6 months." | ( Effect of acetazolamide on visual function in patients with idiopathic intracranial hypertension and mild visual loss: the idiopathic intracranial hypertension treatment trial. Corbett, JJ; Feldon, SE; Friedman, DI; Katz, DM; Keltner, JL; Kieburtz, KD; Kupersmith, MJ; McDermott, MP; Schron, EB; Wall, M, ) | 0.77 |
| " Trial participants (n = 165) with mild visual loss concurrently receiving low-sodium weight-reduction diet plus the maximally tolerated dosage of acetazolamide (up to 4 g/d) or placebo for 6 months." | ( Safety and Tolerability of Acetazolamide in the Idiopathic Intracranial Hypertension Treatment Trial. Friedman, DI; Irrcher, I; McDermott, MP; Patel, AD; ten Hove, MW; Wall, M, 2016) | 0.93 |
| "1%) tolerated the maximum allowed dosage of 4 g/d." | ( Safety and Tolerability of Acetazolamide in the Idiopathic Intracranial Hypertension Treatment Trial. Friedman, DI; Irrcher, I; McDermott, MP; Patel, AD; ten Hove, MW; Wall, M, 2016) | 0.73 |
| "Our results demonstrate that: 1) stone formation during acetazolamide treatment is a relatively infrequent occurrence within the IIH population; 2) among patients who develop a stone, formation is likely to occur within the first year and half; 3) there is no evidence to support the association between acetazolamide daily dosage and stone development; and 4) no unique IIH disease features at the time of diagnosis are associated with stone development." | ( Acetazolamide-Induced Nephrolithiasis in Idiopathic Intracranial Hypertension Patients. Au, JN; Huisingh, C; McGwin, G; Tanne, E; Waslo, CS, 2016) | 2.12 |
| "This reveals that AZM must be formulated as liquid forms with a more complex system of excipients (not usually indicated in pediatrics), or otherwise solid forms capable of assuring uniformity of mass and dose for every dosage unit." | ( Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study. Fariña, JB; Martín-Rodríguez, C; Santoveña, A; Suárez-González, J, 2017) | 0.73 |
| " The rate of acetazolamide elimination into urine was followed for several days after dosing cessation." | ( A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials. Babalonis, S; Hampson, AJ; Krieter, P; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2016) | 1.08 |
| " For each of 4 consecutive mornings after dosing cessation, the rates of urinary acetazolamide elimination remained quantifiable." | ( A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials. Babalonis, S; Hampson, AJ; Krieter, P; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2016) | 0.94 |
| "In the IIHTT, subjects were randomly assigned to placebo-plus-diet or maximally tolerated dosage of acetazolamide-plus-diet." | ( The Longitudinal Idiopathic Intracranial Hypertension Trial: Outcomes From Months 6-12. Auinger, P; Kupersmith, MJ; Moss, EA; Moss, HE; Thurtell, MJ; Wall, M, 2017) | 0.67 |
| "Decisive evidence on the optimal diuretic agent, dosing schedule, and administration route is lacking in acute heart failure (AHF) with congestion." | ( Rationale and design of the ADVOR (Acetazolamide in Decompensated Heart Failure with Volume Overload) trial. Bruckers, L; Damman, K; Droogne, W; Dupont, M; Filippatos, G; Lassus, J; Martens, P; Mebazaa, A; Mullens, W; Nijst, P; Ruschitzka, F; Tartaglia, K; Theunissen, E; Troisfontaines, P; Verbrugge, FH, 2018) | 0.76 |
| " However, evidence indicates that reduced dosage schemes compared to the current recommendations are warranted." | ( Advances in the available non-biological pharmacotherapy prevention and treatment of acute mountain sickness and high altitude cerebral and pulmonary oedema. Balanos, GM; Imray, CHE; Joyce, KE; Lucas, SJE; Wright, AD, 2018) | 0.48 |
| " Further research with more participants with greater rates of AMS would further elucidate this reduced dosage for preventing altitude illness." | ( Reduced Acetazolamide Dosing in Countering Altitude Illness: A Comparison of 62.5 vs 125 mg (the RADICAL Trial). Basnyat, B; Dow, J; Ghale, M; Gurung, TY; Hemphill, M; K Grissom, C; Knott, JR; McDevitt, MC; McIntosh, SE; Thapa, GB; Weber, DC, 2019) | 0.95 |
| "The use of prophylactic acetazolamide in a dosage of 125 mg every 12 h is highly effective at diminishing the risk of HAI." | ( The use of acetazolamide for the prevention of high-altitude illness. Shlim, DR, 2020) | 1.25 |
| "Acetazolamide is the most common medication used for acute mountain sickness prevention, with speculation that a reduced dose may be as efficacious as standard dosing with fewer side effects." | ( A Randomized Controlled Trial of the Lowest Effective Dose of Acetazolamide for Acute Mountain Sickness Prevention. Burnier, A; Hawkins, J; Jurkiewicz, C; Lipman, GS; Lowry, C; Marvel, J; Navlyt, A; Phillips, C; Swenson, ER, 2020) | 2.24 |
| " We previously reported on the pharmacokinetics of a potential adherence marker to noninvasively monitor dosage consumption during a trial without breaking a blind." | ( Subtherapeutic Acetazolamide Doses as a Noninvasive Method for Assessing Medication Adherence. Ellefsen, KN; Epstein, DH; Hampson, AJ; Huestis, MA; Preston, KL; Schroeder, JR; Verrico, CD; Yammine, L, 2020) | 0.91 |
| " Future studies should focus on improving the noninvasive ICP testing, different doses and dosing schedules of AAZ, and the time course of IOP in glaucoma patients not taking AAZ." | ( Intraocular and intracranial pressure in glaucoma patients taking acetazolamide. de Kleine, E; Jansonius, NM; Loiselle, AR; van Dijk, P, 2020) | 0.8 |
| " Herein, we have exploited the unique properties of cubosomes as a novel nano-delivery system for acetazolamide as eye drops dosage form for glaucoma treatment." | ( Novel cubosome based system for ocular delivery of acetazolamide. El Sorogy, HM; Khalil, IA; Teba, HE, 2021) | 1.09 |
| " Furthermore, the non-cytolytic and non-cytotoxic metronomic dosage of hydroxyurea and temozolomide had increased the DBM therapy outcome by strengthening anti-tumor capability." | ( A retrospective observational study on cases of anaplastic brain tumors treated with the Di Bella Method: A rationale and effectiveness. Borghetto, V; Costanzo, E; Di Bella, G, 2021) | 0.62 |
| " IOPs preoperatively and postoperatively were recorded along with the acetazolamide dosage and whether there was evidence of posterior scleral or globe indentation on preoperative MRI." | ( The Effect of Optic Nerve Sheath Fenestration on Intraocular Pressure in Patients With Idiopathic Intracranial Hypertension. Ford, WC; Mancini, R; Mullen, M; Scofield-Kaplan, SM, 2022) | 0.96 |
| "004) in patients who were maintained on the same dosage of acetazolamide in the preoperative and postoperative period." | ( The Effect of Optic Nerve Sheath Fenestration on Intraocular Pressure in Patients With Idiopathic Intracranial Hypertension. Ford, WC; Mancini, R; Mullen, M; Scofield-Kaplan, SM, 2022) | 0.96 |
| " For several years, she was treated for presumed focal seizures with preserved awareness and trialed on adequate dosing of several antiepileptic medications without improvement." | ( A De Novo HECW2 Variant in a Patient with Acetazolamide-Responsive Episodic Ataxia. Detyniecki, K; Margolesky, J; Schrauwen, I; Sharma, S; Tedesco Silva, LM, 2023) | 1.17 |
| "The purpose of this study was to characterize dosing strategies and determine the effectiveness of intravenous (IV) and oral (PO) acetazolamide for patients with heart failure (HF) with diuretic-induced metabolic alkalosis." | ( Intravenous or Oral Acetazolamide for Treatment of Diuretic-Induced Alkalosis in Patients With Heart Failure. Addison, JD; Meyenburg, L; Peterson, EJ, 2023) | 1.44 |
| "This retrospective single-center study evaluated the change in required dosage of acetazolamide and topiramate before and after dural venous sinus stent placement (VSSP) for idiopathic intracranial hypertension (IIH)." | ( Dural Venous Sinus Stent Placement Reduces Dosage Requirements for Carbonic Anhydrase Inhibitors in Patients with Idiopathic Intracranial Hypertension. Martin, J; Sanborn, MR, 2023) | 1.14 |
| "This open-label, single-center pilot study suggests that GLP-1-RAs are an effective and safe treatment option for achieving significant weight loss with a favorable effect on headache, leading to reduced acetazolamide dosage in pwIIH." | ( Treatment with GLP-1 receptor agonists is associated with significant weight loss and favorable headache outcomes in idiopathic intracranial hypertension. Bsteh, G; Harreiter, J; Itariu, B; Krajnc, N; Macher, S; Marik, W; Michl, M; Novak, K; Pemp, B; Wöber, C, 2023) | 1.1 |
| Role | Description |
|---|---|
| EC 4.2.1.1 (carbonic anhydrase) inhibitor | An EC 4.2.1.* (hydro-lyases) inhibitor that interferes with the action of carbonic anhydrase (EC 4.2.1.1). Such compounds reduce the secretion of H(+) ions by the proximal kidney tubule. |
| diuretic | An agent that promotes the excretion of urine through its effects on kidney function. |
| anticonvulsant | A drug used to prevent seizures or reduce their severity. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
| thiadiazoles | |
| monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| cyanate degradation | 4 | 17 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 79.4328 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 17.7828 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.9275 | 0.1000 | 20.8793 | 79.4328 | AID588453; AID588456 |
| GALC protein | Homo sapiens (human) | Potency | 0.6310 | 28.1838 | 28.1838 | 28.1838 | AID1159614 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 34.8063 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 29.8493 | 0.0010 | 22.6508 | 76.6163 | AID1224838 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.1655 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 25.1189 | 0.0002 | 14.3764 | 60.0339 | AID588532 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 24.6090 | 0.0030 | 41.6115 | 22,387.1992 | AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 21.8724 | 0.0008 | 17.5051 | 59.3239 | AID1159531 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 31.5486 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1259401 |
| arylsulfatase A | Homo sapiens (human) | Potency | 21.3313 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.0224 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 11.2202 | 0.5406 | 17.6392 | 96.1227 | AID2364; AID2528 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.8914 | 0.0100 | 39.5371 | 1,122.0200 | AID1479; AID588545 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 61.8150 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
| geminin | Homo sapiens (human) | Potency | 0.1458 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 40.5334 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 0.5623 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 630.9570 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2011 | PloS one, , Volume: 6, Issue:12 | Structural studies of β-carbonic anhydrase from the green alga Coccomyxa: inhibitor complexes with anions and acetazolamide. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1797528 | Esterase Assay from Article 10.1021/jm031057+: \\Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.\\ | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
| AID1796686 | CA Inhibition Assay from Article 10.1016/s0968-0896(00)00026-2: \\2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.\\ | 2000 | Bioorganic & medicinal chemistry, May, Volume: 8, Issue:5 | 2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit. |
| AID1803216 | CA Inhibition Assay from Article 10.3109/14756366.2011.650692: \\Metronidazole-coumarin conjugates and 3-cyano-7-hydroxy-coumarin act as isoform-selective carbonic anhydrase inhibitors.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Metronidazole-coumarin conjugates and 3-cyano-7-hydroxy-coumarin act as isoform-selective carbonic anhydrase inhibitors. |
| AID1796595 | CA Inhibition Assay from Article 10.1021/jm060531j: \\Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.\\ | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
| AID1797029 | Carbonic Anhydrase Inhibition Assay from Article 10.1016/s0006-291x(03)00865-9: \\Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.\\ | 2003 | Biochemical and biophysical research communications, Jun-13, Volume: 305, Issue:4 | Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates. |
| AID1799673 | CA Assay from Article 10.1080/14756360410001689559: \\Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor.\\ | 2004 | Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 19, Issue:3 | Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor. |
| AID1803082 | CA Activity Assay from Article 10.3109/14756366.2011.591290: \\Effects of dopaminergic compounds on carbonic anhydrase isozymes I, II, and VI.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 27, Issue:3 | Effects of dopaminergic compounds on carbonic anhydrase isozymes I, II, and VI. |
| AID1796755 | CA Inhibition Assay from Article 10.1021/jm021123s: \\Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.\\ | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
| AID1803184 | Esterase Activity Assay from Article 10.3109/14756366.2012.712516: \\Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors. |
| AID1799591 | Enzyme Inhbition Assay from Article 10.1111/j.1747-0285.2009.00902.x: \\Carbonic anhydrase inhibitors: glycosylsulfanilamides act as subnanomolar inhibitors of the human secreted isoform VI.\\ | 2009 | Chemical biology & drug design, Dec, Volume: 74, Issue:6 | Carbonic anhydrase inhibitors: glycosylsulfanilamides act as subnanomolar inhibitors of the human secreted isoform VI. |
| AID1799266 | CA Inhibition Assay from Article 10.1016/j.bmc.2009.05.002: \\Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.\\ | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID1803044 | CA Inhibition Assay from Article 10.3109/14756366.2011.629198: \\a-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 27, Issue:1 | α-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters. |
| AID1803033 | CA Activity Assay from Article 10.3109/14756366.2011.588227: \\Acetaldehyde-derived modifications on cytosolic human carbonic anhydrases.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 26, Issue:6 | Acetaldehyde-derived modifications on cytosolic human carbonic anhydrases. |
| AID1803493 | ChEMBL_158313 (CHEMBL763370) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1802978 | Enzyme Activity Assay from Article 10.3109/14756361003733639: \\Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 26, Issue:1 | Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes. |
| AID1803138 | CA Inhibition Assay from Article 10.3109/14756366.2011.637200: \\Inhibition of mammalian carbonic anhydrase isoforms I, II and VI with thiamine and thiamine-like molecules.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Inhibition of mammalian carbonic anhydrase isoforms I, II and VI with thiamine and thiamine-like molecules. |
| AID1803183 | Hydratase Activity Assay from Article 10.3109/14756366.2012.712516: \\Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors. |
| AID1799232 | CA Inhibition Assay from Article 10.1021/jm900641r: \\Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.\\ | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1802355 | CA Inhibition Assay from Article 10.1002/cbic.201600513: \\Structure-Activity Relationships of Benzenesulfonamide-Based Inhibitors towards Carbonic Anhydrase Isoform Specificity.\\ | 2017 | Chembiochem : a European journal of chemical biology, Jan-17, Volume: 18, Issue:2 | Structure-Activity Relationships of Benzenesulfonamide-Based Inhibitors towards Carbonic Anhydrase Isoform Specificity. |
| AID1799586 | Inhibition Assay from Article 10.1111/j.1747-0285.2009.00842.x: \\Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes.\\ | 2009 | Chemical biology & drug design, Aug, Volume: 74, Issue:2 | Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes. |
| AID1803035 | Enzyme Inhibition Assay from Article 10.3109/14756366.2011.578393: \\Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 27, Issue:1 | Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine. |
| AID1799599 | Esterase Activity Assay from Article 10.1111/j.1747-0285.2010.00965.x: \\Carbonic anhydrase inhibitors: Inhibition of human erythrocyte isozymes I and II with a series of phenolic acids.\\ | 2010 | Chemical biology & drug design, May, Volume: 75, Issue:5 | Carbonic anhydrase inhibitors: Inhibition of human erythrocyte isozymes I and II with a series of phenolic acids. |
| AID1803217 | Esterase Activity Assay from Article 10.3109/14756366.2011.651464: \\Analysis of saponins and phenolic compounds as inhibitors of a-carbonic anhydrase isoenzymes.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Analysis of saponins and phenolic compounds as inhibitors of α-carbonic anhydrase isoenzymes. |
| AID1799734 | Inhibition Assay from Article 10.1080/14756360802218441: \\Carbonic anhydrase inhibitors. Biphenylsulfonamides with inhibitory action towards the transmembrane, tumor-associated isozymes IX possess cytotoxic activity against human colon, lung and breast ca | 2009 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 24, Issue:2 | Carbonic anhydrase inhibitors. Biphenylsulfonamides with inhibitory action towards the transmembrane, tumor-associated isozymes IX possess cytotoxic activity against human colon, lung and breast cancer cell lines. |
| AID1796582 | CA Inhibition Assay from Article 10.1021/jm050483n: \\Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.\\ | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors. |
| AID1802983 | Enzyme Activity Assay from Article 10.3109/14756366.2010.491795: \\Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 26, Issue:2 | Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes. |
| AID1803185 | CA Activity Assay from Article 10.3109/14756366.2012.712516: \\Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors. |
| AID1803086 | hCA Activity Assay from Article 10.3109/14756366.2011.599029: \\Synthesis and characterization of novel dioxoacridine sulfonamide derivatives as new carbonic anhydrase inhibitors.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 27, Issue:4 | Synthesis and characterization of novel dioxoacridine sulfonamide derivatives as new carbonic anhydrase inhibitors. |
| AID1798596 | CA Inhibition Assay from Article 10.1016/j.bmcl.2008.06.105: \\Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.\\ | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID1798985 | CA Inhibition Assay from Article 10.1021/jm9000488: \\Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.\\ | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID1796980 | CA Inhibition Assay from Article 10.1021/jm060807n: \\Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide anal | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1799230 | CA Inhibition Assay from Article 10.1016/j.bmc.2009.09.003: \\Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II.\\ | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II. |
| AID1803150 | CO2 Hydration Assay from Article 10.3109/14756366.2012.658788: \\Secondary/tertiary benzenesulfonamides with inhibitory action against the cytosolic human carbonic anhydrase isoforms I and II.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Secondary/tertiary benzenesulfonamides with inhibitory action against the cytosolic human carbonic anhydrase isoforms I and II. |
| AID1796592 | CA Inhibition Assay from Article 10.1021/jm0600287: \\Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX.\\ | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
| AID1796552 | CA Inhibition Assay from Article 10.1021/jm0512600: \\Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.\\ | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. |
| AID1803186 | Esterase Activity Assay from Article 10.3109/14756366.2012.693919: \\Synthesis and characterization of phenolic Mannich bases and effects of these compounds on human carbonic anhydrase isozymes I and II.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Synthesis and characterization of phenolic Mannich bases and effects of these compounds on human carbonic anhydrase isozymes I and II. |
| AID1803487 | ChEMBL_158307 (CHEMBL763192) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1803392 | Thermal Shift Assay (TSA) from Article 10.3109/14756366.2012.757223: \\Benzenesulfonamides with benzimidazole moieties as inhibitors of carbonic anhydrases I, II, VII, XII and XIII.\\ | 2014 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 29, Issue:1 | Benzenesulfonamides with benzimidazole moieties as inhibitors of carbonic anhydrases I, II, VII, XII and XIII. |
| AID1803491 | ChEMBL_158311 (CHEMBL763368) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1798598 | CA Inhibition Assay from Article 10.1016/j.bmcl.2008.03.051: \\Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct.\\ | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID1799667 | Inhibition Assay from Article : \\Carbonic anhydrase activity modulators: synthesis of inhibitors and activators incorporating 2-substituted-thiazol-4-yl-methyl scaffolds.\\ | 2001 | Journal of enzyme inhibition, Oct, Volume: 16, Issue:4 | Carbonic anhydrase activity modulators: synthesis of inhibitors and activators incorporating 2-substituted-thiazol-4-yl-methyl scaffolds. |
| AID1797360 | CA Inhibition Assay from Article 10.1021/jm061320h: \\Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.\\ | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
| AID1802976 | Hydratase Activity Assay from Article 10.3109/14756361003733639: \\Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 26, Issue:1 | Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes. |
| AID1802576 | Esterase Activity Assay from Article 10.1016/j.bioorg.2016.12.001: \\Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4, | 2017 | Bioorganic chemistry, 02, Volume: 70 | Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives. |
| AID1803142 | Esterase Activity Assay from Article 10.3109/14756366.2011.617745: \\Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 27, Issue:6 | Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI. |
| AID1799861 | Inhibition Assay from Article 10.1021/bi802035f: \\Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer properties.\\ | 2009 | Biochemistry, Feb-17, Volume: 48, Issue:6 | Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer properties. |
| AID1803136 | CA Activity Assay from Article 10.3109/14756366.2011.621122: \\Carbonic anhydrase inhibitors: inhibition of human and bovine isoenzymes by benzenesulphonamides, cyclitols and phenolic compounds.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 27, Issue:6 | Carbonic anhydrase inhibitors: inhibition of human and bovine isoenzymes by benzenesulphonamides, cyclitols and phenolic compounds. |
| AID1802982 | Esterase Activity Assay from Article 10.3109/14756366.2010.491795: \\Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 26, Issue:2 | Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes. |
| AID1798769 | CA Inhibition Assay from Article 10.1021/jm801267c: \\Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.\\ | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID1803220 | Esterase Assay from Article 10.3109/14756366.2012.732071: \\Kinetic and in silico analysis of thiazolidin-based inhibitors of a-carbonic anhydrase isoenzymes.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Kinetic and in silico analysis of thiazolidin-based inhibitors of α-carbonic anhydrase isoenzymes. |
| AID1802977 | Esterase Activity Assay from Article 10.3109/14756361003733639: \\Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 26, Issue:1 | Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes. |
| AID1803187 | CA Activity Assay from Article 10.3109/14756366.2012.693919: \\Synthesis and characterization of phenolic Mannich bases and effects of these compounds on human carbonic anhydrase isozymes I and II.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Synthesis and characterization of phenolic Mannich bases and effects of these compounds on human carbonic anhydrase isozymes I and II. |
| AID1801944 | Carbonic Anhydrase (bCAII) Inhibition Assay from Article 10.1016/j.bioorg.2016.07.011: \\Synthesis of novel bisindolylmethanes: New carbonic anhydrase II inhibitors, docking, and 3D pharmacophore studies.\\ | 2016 | Bioorganic chemistry, 10, Volume: 68 | Synthesis of novel bisindolylmethanes: New carbonic anhydrase II inhibitors, docking, and 3D pharmacophore studies. |
| AID1803140 | Esterase Activity Assay from Article 10.3109/14756366.2011.643303: \\Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 28, Issue:2 | Carbonic anhydrase inhibitors: in vitro inhibition of α isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids. |
| AID1803441 | CA Inhibition Assay from Article 10.3109/14756366.2013.806497: \\Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae u00DF-carbonic anhydrase.\\ | 2014 | Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 29, Issue:4 | Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase. |
| AID1802981 | Hydratase Activity Assay from Article 10.3109/14756366.2010.491795: \\Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes.\\ | 2011 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 26, Issue:2 | Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes. |
| AID1796855 | CA Inhibition Assay from Article 10.1021/jm0494826: \\Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.\\ | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties. |
| AID1803489 | ChEMBL_158309 (CHEMBL763366) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1803139 | Esterase Activity Assay from Article 10.3109/14756366.2011.637202: \\Simple methanesulfonates are hydrolyzed by the sulfatase carbonic anhydrase activity.\\ | 2012 | Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 27, Issue:6 | Simple methanesulfonates are hydrolyzed by the sulfatase carbonic anhydrase activity. |
| AID1799602 | In Vitro Inhibtion Assay from Article 10.1111/j.1747-0285.2010.01036.x: \\An alternative purification method for human serum paraoxonase 1 and its interactions with sulfonamides.\\ | 2010 | Chemical biology & drug design, Dec, Volume: 76, Issue:6 | An alternative purification method for human serum paraoxonase 1 and its interactions with sulfonamides. |
| AID1796991 | Carbonic Anhydrase Enzyme Inhibition Assay from Article 10.1021/jm011112j: \\Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation.\\ | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
| AID1801567 | CA I and II Esterase Assay from Article 10.1111/cbdd.12695: \\Synthesis of 4-[2-(3,4-dimethoxybenzyl)cyclopentyl]-1,2-dimethoxybenzene Derivatives and Evaluations of Their Carbonic Anhydrase Isoenzymes Inhibitory Effects.\\ | 2016 | Chemical biology & drug design, Apr, Volume: 87, Issue:4 | Synthesis of 4-[2-(3,4-dimethoxybenzyl)cyclopentyl]-1,2-dimethoxybenzene Derivatives and Evaluations of Their Carbonic Anhydrase Isoenzymes Inhibitory Effects. |
| AID1803484 | ChEMBL_158304 (CHEMBL763189) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1803485 | ChEMBL_158305 (CHEMBL763190) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1803488 | ChEMBL_158308 (CHEMBL763365) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1803492 | ChEMBL_158312 (CHEMBL763369) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1803490 | ChEMBL_158310 (CHEMBL763367) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1799340 | CA Inhibition Assay from Article 10.1016/j.bmc.2009.01.048: \\Carbonic anhydrase inhibitors. The nematode alpha-carbonic anhydrase of Caenorhabditis elegans CAH-4b is highly inhibited by 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides.\\ | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Carbonic anhydrase inhibitors. The nematode alpha-carbonic anhydrase of Caenorhabditis elegans CAH-4b is highly inhibited by 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides. |
| AID1798982 | CA Inhibition Assay from Article 10.1021/jm9003126: \\Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.\\ | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. |
| AID1797276 | Esterase Assay from Article 10.1021/jm031079w: \\Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX.\\ | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1803486 | ChEMBL_158306 (CHEMBL763191) from Article 10.1016/j.bmc.2016.05.029: \\Anion inhibition profiles of a-, u00DF- and u00BF-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.\\ | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID396644 | Anticonvulsant activity in ip dosed OF1 mouse assessed as protection against maximal electroshock-induced seizures after 2 hrs | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. |
| AID1852048 | Selectivity index, ratio of Ki for inhibition of recombinant human CA2 to Ki for inhibition of recombinant human CA9 | |||
| AID1158136 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties. |
| AID1410858 | Inhibition of human CA12 assessed as enzyme inhibitor complex formation preincubated for 15 mins and measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Discovery of 4-Hydroxy-3-(3-(phenylureido)benzenesulfonamides as SLC-0111 Analogues for the Treatment of Hypoxic Tumors Overexpressing Carbonic Anhydrase IX. |
| AID1564416 | Inhibition of recombinant human CA9 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID243117 | Ratio of Kcat/Km against mouse carbonic anhydrase VII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1504708 | Inhibition of Candida glabrata Nce103 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study. |
| AID1336563 | Inhibition of human recombinant carbonic anhydrase-1 using CO2 as substrate preincubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors. |
| AID314833 | Inhibition of human carbonic anhydrase 9 in presence of 10 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1849592 | Binding affinity to human recombinant CA1 assessed as inhibition constant incubated for 10 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID780319 | Inhibition of human carbonic anhydrase14 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID1170164 | Inhibition of human carbonic anhydrase 1 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1357840 | Inhibition of human cytosolic carbonic anhydrase 1 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | 2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents. |
| AID1628038 | Inhibition of recombinant Plasmodium falciparum eta-carbonic anhydrase (181 to 538 residues) expressed in Escherichia coli artic express (DE3) preincubated for 15 mins by stop flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17 | Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum. |
| AID616474 | Inhibition of human carbonic anhydrase 7 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1240215 | Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1379158 | Inhibition of human transmembrane carbonic anhydrase 4 by stopped-flow CO2 hydrase assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino) benzenesulfonamides: Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular modelling studies. |
| AID1736567 | Inhibition of recombinant human CA1 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | |||
| AID272529 | Inhibition of human cloned CA14 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID47719 | Compound was evaluated for inhibition against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. |
| AID1161953 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID724719 | Inhibition of human recombinant CA10 mutant after 15 mins by stopped-flow CO2 hydration method | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Restoring catalytic activity to the human carbonic anhydrase (CA) related proteins VIII, X and XI affords isoforms with high catalytic efficiency and susceptibility to anion inhibition. |
| AID1256865 | Selectivity ratio, ratio of Ki for human carbonic anahydrase-2 to Ki for carbonic anhydrase-14 | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID48302 | Inhibitory activity against human carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX. |
| AID1466466 | Inhibition of recombinant human carbonic anhydrase-9 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII. |
| AID408476 | Selectivity for human cloned CA12 over human recombinant CA2 | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1704678 | Inhibition of human CA1 preincubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. |
| AID551579 | Inhibition of Mycobacterium tuberculosis recombinant beta-carbonic anhydrase Rv1284 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Inhibition of β-carbonic anhydrases with ureido-substituted benzenesulfonamides. |
| AID577530 | Inhibition of Brucella suis carbonic anhydrase II by spectrophotometry at pH 8.3 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID1206510 | Inhibition of human recombinant carbonic anhdydrase-12 expressed in Escherichia coli pre-incubated for 6 hrs by stopped-flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | 6-Substituted sulfocoumarins are selective carbonic anhdydrase IX and XII inhibitors with significant cytotoxicity against colorectal cancer cells. |
| AID1262264 | Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus. |
| AID342486 | Inhibition of mouse carbonic anhydrase 13 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1692095 | Inhibition of human erythrocyte CA2 using 4-nitrophenyl acetate as substrate by spectrophotometry | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate. |
| AID512004 | Inhibition of human cloned catalytic domain of CA12 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID512004 | Inhibition of human cloned catalytic domain of CA12 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID461088 | Inhibition of hydratase-activity of CA1 from human erythrocytes by CO2-hydration method | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. |
| AID1254158 | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22 | New natural product carbonic anhydrase inhibitors incorporating phenol moieties. |
| AID1053402 | Inhibition of recombinant human catalytic domain of carbonic anhydrase-12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates. |
| AID1254032 | Inhibition of Cryptococcus neoformans beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID166954 | In vitro transcorneal accession rate in rabbit corneal denuded epithelium | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID714403 | Inhibition of Sulfurihydrogenibium azorense alpha-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Anion inhibition studies of the fastest carbonic anhydrase (CA) known, the extremo-CA from the bacterium Sulfurihydrogenibium azorense. |
| AID1504710 | Inhibition of human carbonic anhydrase-2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study. |
| AID1312156 | Inhibition of Cryptococcus neoformans beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID603455 | Selectivity ratio of Ki for human full length cytosolic isoform of carbonic anhydrase 2 to Ki for human recombinant catalytic domain of carbonic anhydrase 12 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1849558 | Inhibition of human CA2 by spectrophotometer based analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1193928 | Inhibition of human recombinant CA-9 after 15 mins by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID1537862 | Inhibition of recombinant human carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID1175501 | Inhibition of human recombinant carbonic anhydrase 9 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1517547 | Inhibition of human carbonic anhydrase 1 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID758948 | Inhibition of Porphyromonas gingivalis recombinant CA by CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14 | A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules. |
| AID342466 | Inhibition of AQP4 expressed in rat FRT cells assessed as osmotic water permeability at 10 uM by stopped-flow light scattering method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID1183833 | Inhibition of recombinant human carbonic anhydrase 12 after 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Selective inhibition of human carbonic anhydrases by novel amide derivatives of probenecid: synthesis, biological evaluation and molecular modelling studies. |
| AID314771 | Inhibition of human carbonic anhydrase 2 in presence of 0.25 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID764719 | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety. |
| AID1879885 | Selectivity ratio of Ki for inhibition of human recombinant carbonic anhydrase 2 to Ki for inhibition of human recombinant carbonic anhydrase 12 | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID238987 | Inhibitory activity against human carbonic anhydrase IX at 0.09 uM | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID299231 | Activity of Helicobacter pylori alpha CA at pH 8.9 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID48303 | Inhibitory activity against human carbonic anhydrase IX (hCA IX) by using CO2 hydrase assay method | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design. |
| AID620786 | Inhibition of human recombinant CA9 by CO2 hydration based stopped flow assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1468989 | Binding affinity to human full length His-tagged CA2 (1 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as dissociation rate constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID616476 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1183268 | Inhibition of human cloned CA12 catalytic domain pre-incubated with enzyme for 15 mins by phenol red based CO2 hydration stopped-flow assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis of a new series of N⁴-substituted 4-(2-aminoethyl)benzenesulfonamides and their inhibitory effect on human carbonic anhydrase cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII. |
| AID47924 | Dissociation constant against Carbonic anhydrase II was reported in experiment 2 | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
| AID1170170 | Inhibition of human carbonic anhydrase 6 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1373173 | Binding affinity to recombinant human carbonic anhydrase 12 (1 to 260 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1564423 | Inhibition of recombinant human CA2 at 10'-8 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID271039 | Inhibition of human cloned CA9 catalytic domain by CO2 hydration assay | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors. |
| AID600083 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 7 | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors. |
| AID762171 | Inhibition of carbonic anhydrase 9 (unknown origin) preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design and synthesis of novel 4-(4-oxo-2-arylthiazolidin-3-yl)benzenesulfonamides as selective inhibitors of carbonic anhydrase IX over I and II with potential anticancer activity. |
| AID1273036 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1857415 | Inhibition of human recombinant CA5A assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID50355 | Inhibitory activity against human cloned carbonic anhydrase I (hCA I) | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. |
| AID588191 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 1 to Ki for Mycobacterium tuberculosis recombinant Rv1284 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1373170 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 6 expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID780925 | Binding affinity to human recombinant carbonic anhydrase 13 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Benzenesulfonamides with pyrimidine moiety as inhibitors of human carbonic anhydrases I, II, VI, VII, XII, and XIII. |
| AID697244 | Inhibition of full length human CA1 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. |
| AID281083 | Inhibition of human recombinant isozyme CA2 by CO2 hydration method | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
| AID1518943 | Inhibition of recombinant human carbonic anhydrase 9 at 1 nM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1277142 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 12 | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID238277 | Ki value against carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID766613 | Inhibition of recombinant human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18 | Synthesis of novel acridine and bis acridine sulfonamides with effective inhibitory activity against the cytosolic carbonic anhydrase isoforms II and VII. |
| AID1237884 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 2 to Ki for Cryptococcus neoformans var. grubii beta-carbonic anhydrase | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID382943 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.0302 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1408651 | Inhibition of recombinant human carbonic anhydrase 5b incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity. |
| AID757576 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1691504 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID437756 | Ratio of Kcat to Km full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID48305 | Inhibitory concentration against catalytic domain of human cloned carbonic anhydrase IX. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
| AID589729 | Inhibition of Cryptococcus neoformans Can2 beta-carbonic anhydrase by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. |
| AID1231560 | Inhibition of human carbonic anhydrase-2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay based Lineweaver-Burk plot method | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors. |
| AID1331201 | Inhibition of human recombinant carbonic anhydrase 4 expressed in Escherichia coli assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1 | Microwave assisted synthesis of novel tetrazole/sulfonamide derivatives based on octahydroacridine, xanthene and chromene skeletons as inhibitors of the carbonic anhydrases isoforms I, II, IV and VII. |
| AID386503 | Selectivity for human CA9 over human CA1 | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID468531 | Inhibition of human CA2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors; fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II. |
| AID1464258 | Inhibition of human recombinant carbonic anhydrase-2 preincubated for 10 mins by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID396643 | Anticonvulsant activity in OF1 mouse assessed as protection against maximal electroshock-induced seizures at 50 mg/kg, ip after 2 hrs | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. |
| AID1605090 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action. |
| AID315098 | Inhibition of mouse carbonic anhydrase 13 assessed as 4-nitrophenyl acetate hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID612732 | Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 2 at pH 8.3 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID166790 | Corneal penetration rate constant (k) for excised intact cornea of albino rabbit | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide. |
| AID428373 | Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1706619 | Inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID1435061 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 10 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5 | Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID1655389 | Inhibition of recombinant human carbonic anhydrase 5A preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1470980 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | Synthesis of new 3-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-benzenesulfonamides with strong inhibition properties against the tumor associated carbonic anhydrases IX and XII. |
| AID314822 | Inhibition of human carbonic anhydrase 2 in presence of 0.10 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID244399 | Selectivity ratio of Inhibitory constant against human carbonic anhydrase II to carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX. |
| AID484158 | Inhibition of full length human carbonic anhydrase 5a preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1360269 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents. |
| AID1453444 | Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells at 100 uM using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Repurposing of Proton Pump Inhibitors as first identified small molecule inhibitors of endo-β-N-acetylglucosaminidase (ENGase) for the treatment of NGLY1 deficiency, a rare genetic disease. |
| AID1183562 | Inhibition of human recombinant carbonic anhydrase 12 by stopped flow CO2 hydration method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Cyclic tertiary sulfamates: selective inhibition of the tumor-associated carbonic anhydrases IX and XII by N- and O-substituted acesulfame derivatives. |
| AID1769576 | Inhibition of recombinant human CA4 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold. |
| AID1723512 | Inhibition of carbonic anhydrase in Enterococcus faecium HM-965 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of 5% CO2 by CLSI protocol based broth microdilution assay | |||
| AID1758422 | Inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides. |
| AID1430528 | Inhibition of Burkholderia pseudomallei recombinant His-tagged carbonic anhydrase beta (256 residues) expressed in Escherichia coli BL21 (DE3) incubated for 15 mins prior to testing by stopped flow CO2 hydration method | |||
| AID1565764 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | From random to rational: A discovery approach to selective subnanomolar inhibitors of human carbonic anhydrase IV based on the Castagnoli-Cushman multicomponent reaction. |
| AID352789 | Inhibition of human CA9 catalytic domain by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Carbonic anhydrase inhibitors. Synthesis of 2,4,6-trimethylpyridinium derivatives of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides acting as potent inhibitors of the tumor-associated isoform IX and XII. |
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID387187 | Inhibition of human carbonic anhydrase 1 at 20 degC by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions. |
| AID1460764 | Inhibition of human CA1 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID587124 | Inhibition of human carbonic anhydrase 1 after 15 mins by Lineweaver-Burk plot | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID669117 | Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID486932 | Inhibition of human cloned carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID486932 | Inhibition of human cloned carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1782940 | Inhibition of recombinant human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID1585355 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID317579 | Inhibition of human cloned CA1 by CO2 hydration method | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. |
| AID239048 | Inhibitory activity against membrane bound tumor associated human carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates. |
| AID314817 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.01 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1188770 | Competitive inhibition of bovine erythrocyte carbonic anhydrase 2 using 4-nitrophenyl acetate substrate by photometric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Sulfamates of methyl triterpenoates are effective and competitive inhibitors of carbonic anhydrase II. |
| AID27788 | Calculated partition coefficient (clogP) (MlogP) | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
| AID1537866 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) to Ki for recombinant human carbonic anhydrase 9 expressed in Escherichia coli GOLD BL21 (DE3) | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID1268965 | Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA. |
| AID1757215 | Selectivity index, ratio of Ki for inhibition of human CA2 to Ki for inhibition of human CA9 | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID1303401 | Selectivity ratio, ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 12 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID1706629 | Selectivity index, ratio of Ki for inhibition of human CA2 to Ki for inhibition of human CA12 | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID1077019 | Inhibition of human carbonic anhydrase 1-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1070022 | Inhibition of Legionella pneumophila carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Anion inhibition studies of two new β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID1655393 | Inhibition of recombinant human carbonic anhydrase 7 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1877751 | Inhibition of carbonic anhydrase 1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Synthesis, carbonic anhydrase enzyme inhibition evaluations, and anticancer studies of sulfonamide based thiadiazole derivatives. |
| AID1453627 | Inhibition of recombinant human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Synthesis of novel acyl selenoureido benzensulfonamides as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID271038 | Inhibition of human cloned CA2 by CO2 hydration assay | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors. |
| AID414957 | Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID386504 | Selectivity for human CA9 over human CA2 | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID299238 | Ratio of kcat to Km of human CA12 | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID307888 | Inhibition of human CA5A by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID468534 | Selectivity ratio of Ki for human recombinant CA9 catalytic domain to Ki for human CA2 | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors; fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II. |
| AID367654 | Inhibition of human carbonic anhydrase 2 measured by CO2 hydration reaction assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Carbonic anhydrase inhibitors: inhibition studies of a coral secretory isoform with inorganic anions. |
| AID1237478 | Inhibition of human carbonic anhydrase-1 by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID1425990 | Binding affinity to recombinant human carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. |
| AID1360100 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and X-ray crystallography of selenides bearing benzenesulfonamide moiety with neuropathic pain modulating effects. |
| AID1565733 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration at 10'-7 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1306799 | Inhibition of human recombinant CA1 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Microwave assisted synthesis of novel acridine-acetazolamide conjugates and investigation of their inhibition effects on human carbonic anhydrase isoforms hCA I, II, IV and VII. |
| AID48120 | In vitro inhibitory activity against bovine carbonic anhydrase IV (CAIV) | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | Carbonic anhydrase inhibitors: synthesis and topical intraocular pressure lowering effects of fluorine-containing inhibitors devoid of enhanced reactivity. |
| AID1058183 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | A prodrug approach toward cancer-related carbonic anhydrase inhibition. |
| AID598729 | Inhibition of Brucella suis carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay at pH 8.3 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID496914 | Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1824505 | Inhibition of human CA12 preincubated for 15 mins by phenol red based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Synthesis, biological evaluation, and in silico studies of potential activators of apoptosis and carbonic anhydrase inhibitors on isatin-5-sulfonamide scaffold. |
| AID1189117 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydrase Assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Carbonic Anhydrase Inhibition with Benzenesulfonamides and Tetrafluorobenzenesulfonamides Obtained via Click Chemistry. |
| AID1427468 | Inhibition of recombinant human carbonic anhydrase-1 assessed as reduction in enzyme-catalyzed hydration activity using CO2 as substrate preincubated for 15 mins followed substrate addition measured after 10 to 100 sec by phenol red dye based stopped flow | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3- and 4-(hetero)arylisoxazol-5-amine scaffolds. |
| AID1419424 | Cytotoxicity against human HT-29 cells assessed as cell viability at 100 uM after 48 hrs under hypoxic conditions by MTT assay (Rvb = 100%) | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID238753 | Inhibitory activity against Carbonic anhydrase I | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties. |
| AID314827 | Inhibition of human carbonic anhydrase 9 in presence of 0.25 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1784929 | Inhibition of human CA2 measured after 15 mins by stopped flow carbon dioxide anhydrase assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Natural inspired piperine-based sulfonamides and carboxylic acids as carbonic anhydrase inhibitors: Design, synthesis and biological evaluation. |
| AID620686 | Inhibition of human carbonic anhydrase 2-catalyzed CO2 hydration activity by stopped flow assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID1461934 | Inhibition of human CA2 incubated for 15 mins by stopped-flow CO2 hydration assay | |||
| AID475900 | Inhibition of Brucella suis recombinant (6X)His tagged-beta carbonic anhydrase expressed in Escherichia coli BL21(DE3) after 15 mins by stopped flow carbon dioxide hydrase assay method | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides. |
| AID1060766 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors. |
| AID1464260 | Inhibition of human recombinant carbonic anhydrase-12 preincubated for 10 mins by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID299230 | Activity of human CA14 at pH 7.5 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID620656 | Reduction in CA9 protein level in ca9/ca12 double silenced human LS 174T cells under hypoxia at 60 uM after 48 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID577532 | Inhibition of Helicobacter pylori beta-carbonic anhydrase by spectrophotometry at pH 8.3 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID1274832 | Inhibition of human carbonic anhydrase 2 by Stopped-Flow CO2 Hydrase assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Thioxocoumarins Show an Alternative Carbonic Anhydrase Inhibition Mechanism Compared to Coumarins. |
| AID342478 | Inhibition of human carbonic anhydrase 4 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID646241 | Inhibition of human recombinant carbonic anhydrase 7 using carbon-dioxide as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID314820 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.05 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID411535 | Inhibition of human recombinant CA9 catalytic domain by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411535 | Inhibition of human recombinant CA9 catalytic domain by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1430526 | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition of CO2 hydration incubated for 15 mins prior to testing by stopped flow CO2 hydration method | |||
| AID1241135 | Inhibition of human carbonic anhydrase-1 incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Exploring new Probenecid-based carbonic anhydrase inhibitors: Synthesis, biological evaluation and docking studies. |
| AID1206508 | Inhibition of human recombinant carbonic anhdydrase-2 expressed in Escherichia coli pre-incubated for 6 hrs by stopped-flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | 6-Substituted sulfocoumarins are selective carbonic anhdydrase IX and XII inhibitors with significant cytotoxicity against colorectal cancer cells. |
| AID1303397 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 min to 72 hrs by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID1379912 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Discovery of New Selenoureido Analogues of 4-(4-Fluorophenylureido)benzenesulfonamide as Carbonic Anhydrase Inhibitors. |
| AID1607536 | Inhibition of human recombinant carbonic anhydrase 4 preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID316071 | Inhibition of human recombinant full length carbonic hydrase 14 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID578223 | Inhibition of human recombinant CA5A mitochondrial isoform by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | (R)-/(S)-10-camphorsulfonyl-substituted aromatic/heterocyclic sulfonamides selectively inhibit mitochondrial over cytosolic carbonic anhydrases. |
| AID1453412 | Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | |||
| AID1519743 | Inhibition of recombinant human carbonic anhydrase-1 incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID47728 | 50% inhibitory concentration against human carbonic anhydrase II (HCA II) after pre-incubation at 3 degree C | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma. |
| AID601814 | Inhibition of human carbonic anhydrase 2 preincubated with compound for 15 mins by carbon dioxide hydration assay | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV. |
| AID1256861 | Inhibition of human carbonic anhydrase-9 assessed as CO2 hydration activity by stopped-flow method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID474213 | Selectivity ratio of Ki for human recombinant CA2 to Ki for human recombinant CA9 | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID166758 | Variation of intraocular pressure in second day at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID1849572 | Binding affinity to human CA1 assessed as inhibition constant using 4-nitrophenylacetate as substrate by spectrophotometry based esterase assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1570387 | Inhibition of human carbonic anhydrase 4 incubated for 15 mins by phenol red staining-based stopped flow CO2 hydrase assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure. |
| AID1603058 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors. |
| AID20165 | In vitro susceptibility to nucleophilic attack by reduced glutathione at 37 degree C and at pH 7.4 | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide. |
| AID1446116 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 100 uM after 72 hrs under normoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1301278 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 12 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1373171 | Binding affinity to recombinant human N-terminal His-tagged carbonic anhydrase 7 (3 to 264 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1647461 | Cytotoxicity against human HEK293T cells assessed as reduction in cell viability at 5 to 200 uM incubated for 48 hrs by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID311023 | Inhibition of human carbonic anhydrase 1 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1274833 | Inhibition of human carbonic anhydrase 9 catalytic domain by Stopped-Flow CO2 Hydrase assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Thioxocoumarins Show an Alternative Carbonic Anhydrase Inhibition Mechanism Compared to Coumarins. |
| AID1273000 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 7 | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1449742 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant Malassezia globosa beta-carbonic anhydrase | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Inhibition of Malassezia globosa carbonic anhydrase with phenols. |
| AID299225 | Activity of human CA2 at pH 7.5 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID320305 | Inhibition of human recombinant full length carbonic hydrase 1 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID730890 | Intrinsic thermodynamic binding affinity to human recombinant carbonic anhydrase 12 expressed in Escherichia coli Rosetta (DE3) by isothermal titration calorimetry assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Characterization of human carbonic anhydrase XII stability and inhibitor binding. |
| AID315089 | Inhibition of human carbonic anhydrase 2 by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID1161951 | Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID1809975 | Selectivity ratio of IC50 for inhibition of recombinant human CA9 to IC50 for inhibition of recombinant CA2 using 4-nitrophenylacetate as substrate by esterase assay | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID1077018 | Inhibition of human carbonic anhydrase 2-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID441706 | Inhibition of human recombinant CA2 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1204091 | Inhibition of recombinant human transmembrane, tumor-associated form of carbonic anhydrase-12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1596534 | Inhibition of human carbonic anhydrase 1 assessed as inhibitory constant preincubated for 15 mins by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID428367 | Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1254155 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22 | New natural product carbonic anhydrase inhibitors incorporating phenol moieties. |
| AID238620 | Inhibitory activity against cytosolic human carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates. |
| AID1180164 | Inhibition of CA-12 (unknown origin) after 15 mins by CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors. |
| AID1849588 | Binding affinity to human recombinant CA9 assessed as inhibition constant incubated for 6 hrs prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID778726 | Inhibition of Methanobacterium thermoautotrophicum beta-carbonic anhydrase | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18 | Cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Leishmania donovani chagasi, the protozoan parasite responsible for leishmaniasis. |
| AID1519750 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase-2 to Ki for recombinant human carbonic anhydrase-12 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID254241 | Inhibitory activity against human cloned Carbonic anhydrase II by the CO2 hydration method | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides. |
| AID1168853 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Structural insights on carbonic anhydrase inhibitory action, isoform selectivity, and potency of sulfonamides and coumarins incorporating arylsulfonylureido groups. |
| AID371560 | Selectivity for full length human recombinant mitochondrial carbonic anhydrase 5B over human recombinant cytosolic carbonic anhydrase 2 | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID1243118 | Inhibition of human carbonic anhydrase 9 at 10'-7 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID327766 | Inhibition of human catalytic domain carbonic anhydrase 9 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1053401 | Selectivity ratio of Ki for full length human cytosolic carbonic anhydrase-2 to Ki for recombinant human catalytic domain of carbonic anhydrase-9 | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates. |
| AID1142836 | Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-1 assessed as CO2 hydrase activity by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11 | Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID1379911 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Discovery of New Selenoureido Analogues of 4-(4-Fluorophenylureido)benzenesulfonamide as Carbonic Anhydrase Inhibitors. |
| AID299544 | Inhibition of human CA6 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID646245 | Inhibition of human recombinant carbonic anhydrase 7 hydrolysis activity using 4-nitrophenyl acetate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID1689405 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay to Ki for recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1873563 | Inhibition of human carbonic anhydrase 1 by stopped flow CO2 assay | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors. |
| AID539001 | Inhibition of Saccharomyces cerevisiae CTS1 | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Acetazolamide-based fungal chitinase inhibitors. |
| AID1194027 | Inhibition of recombinant Porphyromonas gingivalis gamma-carbonic anhydrase by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune. |
| AID1257050 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Interaction of carbonic anhydrase isozymes I, II, and IX with some pyridine and phenol hydrazinecarbothioamide derivatives. |
| AID271173 | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
| AID47900 | Inhibition constant evaluated for the inhibition of human CA II (Carbonic anhydrase II) | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID47940 | Inhibitory activity against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered. |
| AID1596536 | Inhibition of human carbonic anhydrase 9 assessed as inhibitory constant preincubated for 15 mins by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID339677 | Inhibition of human recombinant carbonic anhydrase 14 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1251957 | Inhibition of recombinant human carbonic anhydrase 1 expressed in Escherichia coli incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII. |
| AID299245 | Inhibition of human carbonic anhydrase 5A by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID328980 | Inhibition of human full length carbonic anhydrase 6 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID1245673 | Inhibition of carbonic anhydrase-9 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1731967 | Inhibition of human CA1 incubated for 15 mins by stopped-flow CO2 hydration kinetic assay based Cheng-Prusoff equation analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II. |
| AID1504976 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases. |
| AID238300 | Ki value against human carbonic anhydrase II (hCA II) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? |
| AID1238807 | Inhibition of human recombinant CA12 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID1603062 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 9 | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors. |
| AID1655388 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1446105 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1686872 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 9 to Ki for Ki for inhibition of recombinant human carbonic anhydrase 7 | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID526860 | Binding affinity to human recombinant carbonic anhydrase 1 by isothermal titration calorimetry assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID382963 | Solubility in water in presence of 0.0226 mol/l hydroxypropyl-beta-cyclodextrin and 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID365979 | Inhibition of human cloned CA2 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID300868 | Inhibition of human cloned CA2 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety. |
| AID1504046 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Lucky Switcheroo: Dramatic Potency and Selectivity Improvement of Imidazoline Inhibitors of Human Carbonic Anhydrase VII. |
| AID1518917 | Inhibition of recombinant human carbonic anhydrase 1 assessed as residual activity at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID382957 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.0302 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1433066 | Inhibition of human CA9 by stopped-flow CO2 hydration method | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and carbonic anhydrase isoenzymes I, II, IX, and XII inhibitory effects of dimethoxybromophenol derivatives incorporating cyclopropane moieties. |
| AID48092 | Inhibition of human carbonic anhydrase II | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
| AID1234502 | Inhibition of human carbonic anhydrase 12 by by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design and synthesis of benzothiazole-6-sulfonamides acting as highly potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1469003 | Binding affinity to human N-terminal full length His-tagged CA13 (1 to 262 residues) expressed in Escherichia coli BL21(DE3) assessed as thermodynamic equilibrium constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1435062 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 10 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5 | Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID1596535 | Inhibition of human carbonic anhydrase 2 assessed as inhibitory constant preincubated for 15 mins by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID382958 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.0604 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1194029 | Inhibition of Coleofasciculus chthonoplastes beta-carbonic anhydrase by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune. |
| AID1469000 | Binding affinity to human full length His-tagged CA2 (1 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic thermodynamic equilibrium constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1726063 | Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae alpha carbonic anhydrase | |||
| AID26307 | Compound was evaluated for Octanol/pH 7.2 phosphate buffer distribution coefficient | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. |
| AID295289 | Inhibition of human recombinant CA1 after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID327759 | Inhibition of human full length carbonic anhydrase 2 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID446438 | Inhibition of full length human recombinant carbonic anhydrase 9 expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors. |
| AID315090 | Inhibition of human carbonic anhydrase 3 by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID415829 | Inhibition of human CA1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors. |
| AID90255 | Relative salidiuretic efficacy was scored in human; weak | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID1656165 | Inhibition of human CA1 preincubated for 15 mins by stopped-flow CO2 hydration kinetic assay based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action. |
| AID1755845 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID1686879 | Anticonvulsant activity in Swiss Albino mouse assessed as protection against seizure at 100 mg/kg, ip measured after 0.5 hrs by sc-PTZ seizure test relative to control | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID739942 | Inhibition of human carbonic anhydrase-2 cytosolic isoform after 15 mins by Stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Structural effect of phenyl ring compared to thiadiazole based adamantyl-sulfonamides on carbonic anhydrase inhibition. |
| AID300755 | Inhibition of human recombinant CA2 by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID1754560 | Inhibition of recombinant human CA9 preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity. |
| AID1275627 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms. |
| AID281082 | Inhibition of human recombinant isozyme CA1 by CO2 hydration method | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
| AID339668 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1077013 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1238808 | Selectivity ratio of Ki for human recombinant CA1 to Ki for human recombinant CA9 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID307890 | Inhibition of human CA6 by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID757567 | Inhibition of carbonic anhydrase 9 protein expression in human U373 cells under normoxic conditions by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID408472 | Inhibition of human cloned CA12 catalytic domain by stopped flow CO2 hydration assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1849566 | Binding affinity to human CA1 assessed as inhibition constant using 4-nitrophenylacetate as substrate by spectrophotometrical analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1352818 | Inhibition of human CA12 after 15 mins by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Structural investigations on coumarins leading to chromeno[4,3-c]pyrazol-4-ones and pyrano[4,3-c]pyrazol-4-ones: New scaffolds for the design of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID764499 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Inhibition of tumor-associated human carbonic anhydrase isozymes IX and XII by a new class of substituted-phenylacetamido aromatic sulfonamides. |
| AID299228 | Activity at human CA5B at pH 7.5 by CO2 hydration | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1873566 | Inhibition of human carbonic anhydrase 12 by stopped flow CO2 assay | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors. |
| AID612728 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 at pH 8.3 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID1678136 | Inhibition of recombinant human CA9 expressed in Escherichia coli BL21 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Structural Basis of Nanomolar Inhibition of Tumor-Associated Carbonic Anhydrase IX: X-Ray Crystallographic and Inhibition Study of Lipophilic Inhibitors with Acetazolamide Backbone. |
| AID1180161 | Inhibition of CA-2 (unknown origin) after 15 mins by CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors. |
| AID320312 | Inhibition of human recombinant full length carbonic hydrase 7 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID1453628 | Inhibition of recombinant human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Synthesis of novel acyl selenoureido benzensulfonamides as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID1301277 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID612731 | Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 1 at pH 8.3 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID1277136 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins prior to testing by CO2 hydration-based stopped flow assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID1060764 | Inhibition of human catalytic domain of carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors. |
| AID1570355 | Inhibition of recombinant human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Carbonic anhydrase inhibitors based on sorafenib scaffold: Design, synthesis, crystallographic investigation and effects on primary breast cancer cells. |
| AID1564430 | Inhibition of recombinant human CA12 at at 10'-9 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1723532 | Antibacterial activity against Enterococcus faecium NR-31972 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1726064 | Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae beta carbonic anhydrase | |||
| AID1373183 | Binding affinity to recombinant human N-terminal His-tagged carbonic anhydrase 7 (3 to 264 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID301574 | Ratio of Kcat to Km of human recombinant CA 2 | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID321160 | Selectivity for human CA9 over human CA1 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID421537 | Inhibition of human erythrocytes carbonic anhydrase 2 by CO2 hydration assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Carbonic anhydrase-encoded dynamic constitutional libraries: toward the discovery of isozyme-specific inhibitors. |
| AID1058392 | Inhibition of Candida albicans carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID1278406 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID295295 | Inhibition of human recombinant CA14 after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID1753390 | Selectivity index, ratio of Ki for inhibition of human CA1 to Ki for inhibition of human CA9 | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities. |
| AID778725 | Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18 | Cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Leishmania donovani chagasi, the protozoan parasite responsible for leishmaniasis. |
| AID365983 | Inhibition of human cloned CA5B by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID1633345 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1564592 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity. |
| AID616470 | Inhibition of human carbonic anhydrase 4 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1408647 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity. |
| AID1474292 | Inhibition of recombinant human cytosolic carbonic anhydrase 1 pretreated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Evaluation of selenide, diselenide and selenoheterocycle derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors. |
| AID1172691 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Carbonic anhydrase inhibitory activity of sulfonamides and carboxylic acids incorporating cyclic imide scaffolds. |
| AID1857411 | Inhibition of human recombinant DPP4 using H-Gly-Pro-AMC as substrate incubated for 30 mins by fluorescence based microplate reader assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID1564427 | Inhibition of recombinant human CA9 at 10'-8 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1277140 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID1240210 | Inhibition of human carbonic anhydrase-2 by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1723493 | Antibacterial activity against Enterococcus faecium NR-31903 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID780951 | Inhibition of human recombinant carbonic anhydrase3 cytosolic isoform expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Inhibition of human carbonic anhydrase isoforms I-XIV with sulfonamides incorporating fluorine and 1,3,5-triazine moieties. |
| AID1633342 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1723492 | Antibacterial activity against Enterococcus faecium NR-28978 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1534903 | Inhibition of recombinant full length human carbonic anhydrase-7 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID620687 | Inhibition of human carbonic anhydrase 9-catalyzed CO2 hydration activity by stopped flow assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID1379904 | Inhibition of recombinant human full-length carbonic anhydrase 2 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. |
| AID1565732 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration at 10'-8 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1312152 | Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID315091 | Inhibition of human carbonic anhydrase 13 by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID486933 | Inhibition of human cloned carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID486933 | Inhibition of human cloned carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID587130 | Inhibition of human carbonic anhydrase 1 after 15 mins by CO2 hydrase assay at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID1188138 | Inhibition of Porphyromonas gingivalis Gamma-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID1422964 | Inhibition of recombinant human CA3 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1660020 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID300756 | Inhibition of human CA9 catalytic domain by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID1306528 | Inhibition of Porphyromonas gingivalis beta carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID239240 | Inhibitory potency against human cloned Carbonic anhydrase II expressed in Escherichia coli strain BL21 | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX. |
| AID1193925 | Inhibition of human recombinant CA-1 after 15 mins by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID1757216 | Selectivity index, ratio of Ki for inhibition of human CA1 to Ki for inhibition of human CA12 | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID295294 | Inhibition of human recombinant CA9 after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID1356462 | Binding affinity to human carbonic anhydrase 2 by stopped flow CO2 hydration method | 2018 | ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7 | Targeting Tumor Associated Carbonic Anhydrases IX and XII: Highly Isozyme Selective Coumarin and Psoralen Inhibitors. |
| AID1511297 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID614108 | Inhibition of human cloned carbonic anhydrase 12 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Carbonic anhydrase inhibitors. Synthesis, molecular structures, and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with novel 3-pyridinesulfonamide derivatives. |
| AID1439685 | Inhibition of recombinant human cytosolic carbonic anhydrase 1 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. |
| AID1419420 | Cytotoxicity against human HT-29 cells assessed as cell viability at 30 uM after 48 hrs under normoxic conditions by MTT assay (Rvb = 100%) | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID537655 | Inhibition of human carbonic anhydrase 2 hydratase activity by spectrophotometry | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide. |
| AID1061041 | Inhibition of human CA1 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1238806 | Inhibition of human recombinant CA9 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID187643 | Relative salidiuretic efficacy was scored in Rat; weak | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID588190 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 1 to Ki for Mycobacterium tuberculosis recombinant Rv3273 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID610541 | Inhibition of human recombinant carbonic anhydrase 5a preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID275811 | Inhibition of human cytosolic isozyme CA III | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID1183831 | Inhibition of recombinant human carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Selective inhibition of human carbonic anhydrases by novel amide derivatives of probenecid: synthesis, biological evaluation and molecular modelling studies. |
| AID20925 | Compound was evaluated for its solubility in water | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors. |
| AID272527 | Inhibition of catalytic domain of human cloned CA12 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1170159 | Inhibition of human CA-9 by stopped flow CO2 hydrase assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | A class of 4-sulfamoylphenyl-ω-aminoalkyl ethers with effective carbonic anhydrase inhibitory action and antiglaucoma effects. |
| AID1190064 | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum. |
| AID1251974 | Inhibition of human carbonic anhydrase 9 incubated for 6 hrs by stopped flow carbon-di-oxide hydrase assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Click-tailed coumarins with potent and selective inhibitory action against the tumor-associated carbonic anhydrases IX and XII. |
| AID195091 | Inhibitor level was measured in red blood cells at 30 min after exposure of 10 mL of blood to solutions by enzymatic method (EI) | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID1655627 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII. |
| AID1193751 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID1133321 | Anticonvulsant activity in po dosed mouse assessed as protection against electroshock-induced maximal seizure effect administered via gavage 2 hrs prior to electroshock stimulation | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides. |
| AID1314077 | Inhibition of human CA12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis 4-[2-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-ethyl]-benzenesulfonamides with subnanomolar carbonic anhydrase II and XII inhibitory properties. |
| AID1336987 | Inhibition of recombinant human erythrocyte cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID382946 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.1132 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1784930 | Inhibition of human CA9 measured after 15 mins by stopped flow carbon dioxide anhydrase assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Natural inspired piperine-based sulfonamides and carboxylic acids as carbonic anhydrase inhibitors: Design, synthesis and biological evaluation. |
| AID314794 | Inhibition of human carbonic anhydrase 9 in presence of 1.00 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1879879 | Inhibition of human recombinant carbonic anhydrase 2 assessed as inhibition constant incubated for 10 mins by phenol red dye based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID1753387 | Inhibition of recombinant human CA2 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities. |
| AID23533 | Compound was tested for solubility in pH buffer, at 25 degree C. | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring? |
| AID441708 | Inhibition of human recombinant CA4 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1238449 | Inhibition of human carbonic anhydrase-9 incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1517548 | Inhibition of human carbonic anhydrase 2 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1274834 | Inhibition of human carbonic anhydrase 12 catalytic domain by Stopped-Flow CO2 Hydrase assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Thioxocoumarins Show an Alternative Carbonic Anhydrase Inhibition Mechanism Compared to Coumarins. |
| AID1375666 | Inhibition of recombinant human carbonic anhydrase-1 incubated for 15 mins by stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis. |
| AID271711 | Inhibition of human cloned CA2 by CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". |
| AID616480 | Inhibition of human carbonic anhydrase 13 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1173861 | Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | 4-Functionalized 1,3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of carbonic anhydrase isoforms hCA I, II, IX and XII. |
| AID314777 | Inhibition of human carbonic anhydrase 2 in presence of 10 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID599953 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors. |
| AID238597 | Inhibitory activity against bovine carbonic anhydrase IV (bCAIV) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. |
| AID1204092 | Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-1 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-9 | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII. |
| AID314806 | Inhibition of human carbonic anhydrase 9 in presence of 0.10 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID382951 | Solubility in water in presence of 0.0604 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID272523 | Inhibition of human cloned CA5A by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1888317 | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition constant preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain. |
| AID47736 | In vitro inhibition of human Carbonic Anhydrase II | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide. |
| AID1852044 | Inhibition of recombinant human CA12 pre-incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID600082 | Inhibition of human recombinant carbonic anhydrase 7 by stopped flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors. |
| AID1357961 | Cytotoxicity against human MDA-MB-231 cells after 96 hrs under normoxic condition by MTT assay | |||
| AID327764 | Inhibition of human full length carbonic anhydrase 6 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1426788 | Inhibition of recombinant human CA7 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis. |
| AID238770 | Inhibitory activity against human carbonic anhydrase I expressed in Escherichia coli BL21 | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties. |
| AID589728 | Inhibition of human cytosolic carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. |
| AID441209 | Inhibition of human cloned CA12 catalytic domain by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID50189 | Inhibition concentration by inhibition of carbonic anhydrase from brain in Rat | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8 | Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives. |
| AID757587 | Inhibition of carbonic anhydrase 9 protein expression in human U87MG cells under hypoxic conditions at 4000 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1274831 | Inhibition of human carbonic anhydrase 1 by Stopped-Flow CO2 Hydrase assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Thioxocoumarins Show an Alternative Carbonic Anhydrase Inhibition Mechanism Compared to Coumarins. |
| AID263637 | Inhibition of human recombinant CA2 | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori. |
| AID1603059 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors. |
| AID1330453 | Inhibition of human full length carbonic anhydrase 1 | |||
| AID603069 | Inhibition of human recombinant cytosolic carbonic anhydrase 3 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Conformational variability of different sulfonamide inhibitors with thienyl-acetamido moieties attributes to differential binding in the active site of cytosolic human carbonic anhydrase isoforms. |
| AID1751408 | Inhibition of human CA1 measured by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies. |
| AID1272998 | Inhibition of recombinant human carbonic anhydrase 14 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1193929 | Inhibition of human recombinant CA-12 after 15 mins by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID438006 | Inhibition of human full length carbonic anhydrase 6 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1565731 | Inhibition of human carbonic anhydrase 12 assessed as inhibitory constant incubated for 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1726065 | Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae gamma carbonic anhydrase | |||
| AID731404 | Inhibition of human carbonic anhydrase 2 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | New selective carbonic anhydrase IX inhibitors: synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides. |
| AID1194929 | Reduction in intraocular pressure in patient with open-angle glaucoma | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of a new series of dithiocarbamates with effective human carbonic anhydrase inhibitory activity and antiglaucoma action. |
| AID1256860 | Inhibition of human carbonic anhydrase-2 assessed as CO2 hydration activity by stopped-flow method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID1336562 | Inhibition of Burkholderia pseudomallei recombinant His-tagged carbonic anhydrase gamma expressed in Escherichia coli BL21 (DE3) assessed as inhibition of CO2 hydration preincubated for 15 mins by Lineweaver-burk plot method | |||
| AID677270 | Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 alpha-carbonic anhydrase-catalyzed CO2 hydration reaction preincubated for 15 mins by stopped flow CO2 hydrase assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Anion inhibition studies of an α-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1. |
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| AID1518946 | Inhibition of recombinant human carbonic anhydrase 2 assessed as residual activity at 1 nM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1707346 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors. |
| AID1902654 | Inhibition of recombinant human CA 9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID732712 | Binding affinity to human recombinant CA2 at 37 degC and pH 7.0 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | 4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII. |
| AID1570402 | Inhibition of recombinant human carbonic anhydrase12 preincubated for 10 mins followed by CO2 solution addition by phenol red dye based stopped flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Synthesis and exploration of 2-morpholino-4-phenylthiazol-5-yl acrylamide derivatives for their effects against carbonic anhydrase I, II, IX and XII isoforms as a non-sulfonamide class of inhibitors. |
| AID1170179 | Inhibition of human carbonic anhydrase 2 at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1303394 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 min to 72 hrs by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID1852388 | Inhibition of Carbonic anhydrase (unknown origin) | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
| AID1275557 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1170166 | Inhibition of human carbonic anhydrase 3 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID301575 | Ratio of Kcat to Km of human recombinant CA 3 | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID1231559 | Inhibition of human carbonic anhydrase-1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay based Lineweaver-Burk plot method | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors. |
| AID1394918 | Inhibition of transmembrane human carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID644088 | Inhibition of bovine carbonic anhydrase 3 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID315092 | Inhibition of mouse carbonic anhydrase 13 by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID1206509 | Inhibition of human recombinant carbonic anhdydrase-9 expressed in Escherichia coli pre-incubated for 6 hrs by stopped-flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | 6-Substituted sulfocoumarins are selective carbonic anhdydrase IX and XII inhibitors with significant cytotoxicity against colorectal cancer cells. |
| AID1659548 | Selectivity index, ratio of IC50 for human carbonic anhydrase 2 using p-nitrophenyl acetate as substrate to IC50 for human carbonic anhydrase 5A using p-nitrophenyl acetate as substrate by | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX. |
| AID300759 | Selectivity for human CA9 over human CA2 | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID646249 | Inhibition of human recombinant carbonic anhydrase 7 phosphatase activity using 4-nitrophenyl phosphate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID244539 | Inhibition constant against human recombinant carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumo |
| AID620787 | Inhibition of human recombinant CA12 by CO2 hydration based stopped flow assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1373166 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1419422 | Cytotoxicity against human HT-29 cells assessed as cell viability at 200 uM after 48 hrs under normoxic conditions by MTT assay (Rvb = 100%) | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID301522 | Inhibition of human cloned carbonic anhydrase2 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2-thione derivatives with carbonic anhydrase inhibitory activity. |
| AID239250 | Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID1585356 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 12 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID299541 | Inhibition of human CA4 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID492421 | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain preincubated for 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Coumarinyl-substituted sulfonamides strongly inhibit several human carbonic anhydrase isoforms: solution and crystallographic investigations. |
| AID321158 | Inhibition of human recombinant CA9 by CO2 hydration stopped flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID1446119 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 100 uM after 72 hrs under hypoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1278994 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6 | Development of 3-(4-aminosulphonyl)-phenyl-2-mercapto-3H-quinazolin-4-ones as inhibitors of carbonic anhydrase isoforms involved in tumorigenesis and glaucoma. |
| AID47929 | Inhibition of human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. |
| AID1504901 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors. |
| AID1058080 | Inhibition of human recombinant carbonic anhydrase 12-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Salen and tetrahydrosalen derivatives act as effective inhibitors of the tumor-associated carbonic anhydrase XII--a new scaffold for designing isoform-selective inhibitors. |
| AID1422967 | Inhibition of recombinant human CA5b preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1537863 | Inhibition of recombinant human carbonic anhydrase 2 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID314772 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.25 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1373174 | Binding affinity to recombinant human full length N-terminal His-tagged carbonic anhydrase 13 (1 to 262 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1422968 | Inhibition of recombinant human CA6 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1058083 | Inhibition of human recombinant carbonic anhydrase 1-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Salen and tetrahydrosalen derivatives act as effective inhibitors of the tumor-associated carbonic anhydrase XII--a new scaffold for designing isoform-selective inhibitors. |
| AID254243 | Inhibitory activity against human Carbonic anhydrase II (hCA II) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. |
| AID1240211 | Inhibition of Coleofasciculus chthonoplastes beta carbonic anhydrase by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID331499 | Inhibition of human recombinant carbonic anhydrase 2 by CO2 hydration stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes. |
| AID396642 | Inhibition of human carbonic anhydrase 7 by CO2 hydration assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. |
| AID1692096 | Inhibition of human erythrocyte CA1 b using 4-nitrophenyl acetate as substrate by Lineweaver-Burk plot analysis | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate. |
| AID243110 | Ratio of Kcat/Km against human carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1723515 | Bacteriostatic activity against Enterococcus faecium ATCC 700221 assessed as reduction in bacterial burden at 5 times MIC preincubated for 24 hrs followed by replating on soya agar plates and measured after 16 hrs by time-kill assay | |||
| AID1126609 | Inhibition of bovine erythrocyte carbonic anhydrase 2 using p-nitrophenyl acetate as substrate at 1 mM preincubated for 10 mins before substrate addition measured after 30 mins by spectrophotometric analysis | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | New aminobenzenesulfonamide-thiourea conjugates: synthesis and carbonic anhydrase inhibition and docking studies. |
| AID1655625 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII. |
| AID427131 | Selectivity ratio of Ki for Candida albicans recombinant Nce103 to Ki for Cryptococcus neoformans recombinant Can2 | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID552131 | Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. |
| AID195094 | Inhibitor level was measured in red blood cells at 60 min after exposure of 10 mL of blood to solutions by enzymatic method (EI) | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID1446117 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 300 uM after 72 hrs under normoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1058394 | Inhibition of Cryptococcus neoformans carbonic anhydrase Can2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID1692244 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII. |
| AID438009 | Inhibition of human membrane-bound carbonic anhydrase 12 catalytic domain after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID314795 | Inhibition of human carbonic anhydrase 2 in presence of 10 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1410856 | Inhibition of human CA2 assessed as enzyme inhibitor complex formation preincubated for 15 mins and measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Discovery of 4-Hydroxy-3-(3-(phenylureido)benzenesulfonamides as SLC-0111 Analogues for the Treatment of Hypoxic Tumors Overexpressing Carbonic Anhydrase IX. |
| AID1849562 | Binding affinity to human CA1 assessed as inhibition constant by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1312158 | Inhibition of Mycobacterium tuberculosis beta-carbonic anhydrase Rv3273 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID1464263 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase-1 to Ki for human recombinant carbonic anhydrase-12 | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID1660016 | Inhibition of human carbonic anhydrase 9 assessed as inhibitory constant incubated for 6 hrs by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID320313 | Inhibition of human catalytic domain carbonic hydrase 9 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID300757 | Inhibition of human CA12 catalytic domain by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID314769 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.10 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID493886 | Inhibition of human recombinant carbonic anhydrase 4 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1607541 | Inhibition of human recombinant carbonic anhydrase 12 preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID493887 | Inhibition of human recombinant carbonic anhydrase 5a after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID21067 | Corneal permeability coefficient was determined | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. |
| AID1607534 | Inhibition of human recombinant carbonic anhydrase 1 preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID1425992 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 12 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. |
| AID484160 | Inhibition of human carbonic anhydrase 6 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1596537 | Inhibition of human carbonic anhydrase 12 assessed as inhibitory constant preincubated for 15 mins by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID1180159 | Inhibition of CA-1 (unknown origin) after 15 mins by CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors. |
| AID1818555 | Inhibition of human CA1 incubated for 15 mins prior to testing by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | 2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity. |
| AID1427470 | Inhibition of recombinant human carbonic anhydrase-4 assessed as reduction in enzyme-catalyzed hydration activity using CO2 as substrate preincubated for 15 mins followed substrate addition measured after 10 to 100 sec by phenol red dye based stopped flow | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3- and 4-(hetero)arylisoxazol-5-amine scaffolds. |
| AID1818558 | Inhibition of human CA9 incubated for 15 mins prior to testing by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | 2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity. |
| AID367617 | Inhibition of human recombinant CA12 catalytic domain by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367617 | Inhibition of human recombinant CA12 catalytic domain by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID646250 | Inhibition of human recombinant carbonic anhydrase 7 C183S/C217S mutant phosphatase activity using 4-nitrophenyl phosphate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID293812 | Inhibition of human recombinant CA2 by stopped flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties. |
| AID1170177 | Inhibition of human carbonic anhydrase 14 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1348313 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases. |
| AID623073 | Selectivity ratio of Ki for carbonic anhydrase 1 to Ki for carbonic anhydrase 9 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis of glycoconjugate carbonic anhydrase inhibitors by ruthenium-catalysed azide-alkyne 1,3-dipolar cycloaddition. |
| AID1555962 | Inhibition of human carbonic anhydrase 3 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID314767 | Inhibition of human carbonic anhydrase 9 in presence of 0.05 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID733808 | Selectivity ratio of IC50 for recombinant human carbonic anhydrase 2 to IC50 for recombinant human carbonic anhydrase 9 | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship. |
| AID1238810 | Selectivity ratio of Ki for human recombinant CA1 to Ki for human recombinant CA12 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID1555960 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID1872738 | Binding affinity to carbonic anhydrase 1 (unknown origin) assessed as inhibition constant | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy. |
| AID50175 | Compound was evaluated for the inhibition of Carbonic anhydrase (Non competitive) | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. |
| AID272526 | Inhibition of catalytic domain of human cloned CA9 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1565738 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration at 10'-7 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1570354 | Inhibition of recombinant human CA7 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Carbonic anhydrase inhibitors based on sorafenib scaffold: Design, synthesis, crystallographic investigation and effects on primary breast cancer cells. |
| AID382962 | Solubility in water in presence of 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1202646 | Inhibition of human membrane associated form of carbonic anhydrase-12 assessed as CO2 hydration activity incubated for 15 mins prior to testing by stopped flow method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis, carbonic anhydrase inhibition and cytotoxic activity of novel chromone-based sulfonamide derivatives. |
| AID1256867 | Selectivity ratio, ratio of Ki for human carbonic anahydrase-12 to Ki for carbonic anhydrase-14 | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID382959 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.0755 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID607496 | Inhibition of human CA6 using 4-nitrophenylacetate substrate by esterase assay | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | In vitro inhibition of α-carbonic anhydrase isozymes by some phenolic compounds. |
| AID271714 | Selectivity for human CA9 over CA2 | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". |
| AID1154447 | Inhibition of human cloned transmembrane tumor-associated catalytic domain of carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Carbonic anhydrase inhibitors. Synthesis of a novel series of 5-substituted 2,4-dichlorobenzenesulfonamides and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII. |
| AID1518933 | Inhibition of recombinant human carbonic anhydrase 9 assessed as residual activity at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1517566 | Inhibition of human carbonic anhydrase 9 at 10'-7 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1723514 | Inhibition of carbonic anhydrase in Enterococcus faecium ATCC 700221 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of 5% CO2 by CLSI protocol based broth microdilution assay | |||
| AID1666824 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID1720900 | Inhibition of recombinant human carbonic anhydrase 12 assessed as inhibition constant preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | New coumarin/sulfocoumarin linked phenylacrylamides as selective transmembrane carbonic anhydrase inhibitors: Synthesis and in-vitro biological evaluation. |
| AID1726062 | Inhibition of human carbonic anhydrase 2 incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1188141 | Inhibition of Legionella pneumophilia Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID1768059 | Inhibition of human carbonic anhydrase 12 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
| AID1183265 | Inhibition of human cloned CA1 pre-incubated with enzyme for 15 mins by phenol red based CO2 hydration stopped-flow assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis of a new series of N⁴-substituted 4-(2-aminoethyl)benzenesulfonamides and their inhibitory effect on human carbonic anhydrase cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII. |
| AID1857414 | Inhibition of human recombinant CA4 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID339672 | Inhibition of human recombinant carbonic anhydrase 5A by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID743512 | Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 recombinant carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides. |
| AID612730 | Inhibition of Brucella suis recombinant carbonic anhydrase 2 at pH 8.3 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID1245675 | Inhibition of carbonic anhydrase-14 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1277135 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing by CO2 hydration-based stopped flow assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID314811 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 1.00 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1360270 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents. |
| AID342480 | Inhibition of human carbonic anhydrase 5B by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1468995 | Binding affinity to human CA9 catalytic domain expressed in mammalian expression system assessed as intrinsic thermodynamic equilibrium constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1292254 | Inhibition of human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate by Lineweaver-Burk plot analysis | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. |
| AID226919 | Anticonvulsant potency in mice relative to compound UK-12130 (ED50 of compound 24/compound) | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides. |
| AID1753405 | Inhibition of recombinant human CA2 pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Insertion of metal carbenes into the anilinic N-H bond of unprotected aminobenzenesulfonamides delivers low nanomolar inhibitors of human carbonic anhydrase IX and XII isoforms. |
| AID1460768 | Inhibition of human CA5A by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1660015 | Inhibition of human carbonic anhydrase 1 assessed as inhibitory constant incubated for 6 hrs by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID1689399 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1193680 | Inhibition of human tumor-associated carbonic anhydrase 12 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Synthesis of 6-aryl-substituted sulfocoumarins and investigation of their carbonic anhydrase inhibitory action. |
| AID1565744 | Inhibition of human carbonic anhydrase 12 assessed as reduction in CO2 hydration at 10'-9 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1058391 | Inhibition of Flaveria bidentis carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID371557 | Inhibition of full length human recombinant mitochondrial carbonic anhydrase 5A pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID307891 | Inhibition of human CA9 catalytic domain by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID421536 | Inhibition of human erythrocytes carbonic anhydrase 1 by CO2 hydration assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Carbonic anhydrase-encoded dynamic constitutional libraries: toward the discovery of isozyme-specific inhibitors. |
| AID1243108 | Inhibition of human carbonic anhydrase 1 at 10'-9 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1461805 | Inhibition of human CA12 | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | 1,3-Oxazole-based selective picomolar inhibitors of cytosolic human carbonic anhydrase II alleviate ocular hypertension in rabbits: Potency is supported by X-ray crystallography of two leads. |
| AID1727540 | Inhibition of recombinant human carbonic anhydrase 7 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion. |
| AID371556 | Inhibition of truncated human cloned membrane-associated carbonic anhydrase 4 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID1565743 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration at 10'-6 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1818405 | Inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors. |
| AID1689406 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay to Ki for recombinant human carbonic anhydrase 12 preincubated with enzyme for 15 mins by | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1560580 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID281085 | Selectivity ratio of human CA9 over human CA1 | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
| AID1172693 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Carbonic anhydrase inhibitory activity of sulfonamides and carboxylic acids incorporating cyclic imide scaffolds. |
| AID1446111 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 300 uM after 48 hrs under normoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1534904 | Inhibition of human carbonic anhydrase-9 catalytic domain assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID1873665 | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition constant incubated for 1 hr prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry, 08-01, Volume: 67 | Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation. |
| AID411528 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411528 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1301276 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 9 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1067262 | Inhibition of human recombinant transmembrane carbonic anhydrase 9 after 6 hrs by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Synthesis of 6-tetrazolyl-substituted sulfocoumarins acting as highly potent and selective inhibitors of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1291095 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 expressed in Escherichia coli to Ki for recombinant Candida glabrata beta carbonic anhydrase NCE103 expressed in Escherichia coli | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID424443 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. |
| AID1238455 | Selectivity ratio of Ki for human carbonic anhydrase-2 to Ki for human carbonic anhydrase-12 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID311031 | Inhibition of human carbonic anhydrase 9 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID47751 | Inhibitory activity towards Carbonic anhydrase II | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
| AID50351 | In vitro inhibitory activity against human carbonic anhydrase I (hCAI) | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | Carbonic anhydrase inhibitors: synthesis and topical intraocular pressure lowering effects of fluorine-containing inhibitors devoid of enhanced reactivity. |
| AID1379157 | Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino) benzenesulfonamides: Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular modelling studies. |
| AID301573 | Ratio of Kcat to Km of human recombinant CA 1 | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID48296 | Inhibitory activity against human tumor-associated transmembrane carbonic anhydrase IX. | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Carbonic anhydrase inhibitors: the first QSAR study on inhibition of tumor-associated isoenzyme IX with aromatic and heterocyclic sulfonamides. |
| AID437749 | Inhibition of human recombinant CA2 by stopped-flow hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID50371 | Inhibitory activity against human cloned carbonic anhydrase isozyme I by esterase assay method. | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides. |
| AID1879882 | Selectivity ratio of Ki for inhibition of human recombinant carbonic anhydrase 1 to Ki for inhibition of human recombinant carbonic anhydrase 9 | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID1273003 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 14 to Ki for recombinant human carbonic anhydrase 7 | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1442654 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip administered 0.5 hrs prior to 50 mA current induction | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID484213 | Inhibition of human carbonic anhydrase 1 | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors. |
| AID441705 | Inhibition of human recombinant CA1 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID382955 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1454026 | Inhibition of recombinant human cytosolic carbonic anhydrase 1 expressed in Escherichia coli pretreated for 15 mins prior to testing by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases. |
| AID1726081 | Inhibition of Vibrio cholerae gamma carbonic anhydrase pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in |
| AID365978 | Inhibition of human cloned CA1 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID603451 | Inhibition of human recombinant catalytic domain of carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1162894 | Selectivity ratio of Ki for Vibrio cholerae alpha-carbonic anhydrase to Ki for human carbonic anhydrase 2 | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | Quinazoline-sulfonamides with potent inhibitory activity against the α-carbonic anhydrase from Vibrio cholerae. |
| AID1519755 | Inhibition of recombinant human carbonic anhydrase-2 at 1 nM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1453411 | Inhibition of Burkholderia pseudomallei beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | |||
| AID295298 | Selectivity ratio of human CA4 over human CA2 | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID48299 | Inhibition constant determined against catalytic domain of human cloned carbonic anhydrase IX | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
| AID496918 | Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1067264 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 after 6 hrs by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Synthesis of 6-tetrazolyl-substituted sulfocoumarins acting as highly potent and selective inhibitors of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1578356 | Inhibition of recombinant human CA9 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors. |
| AID1824501 | Inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Synthesis, biological evaluation, and in silico studies of potential activators of apoptosis and carbonic anhydrase inhibitors on isatin-5-sulfonamide scaffold. |
| AID1242662 | Inhibition of full length human carbonic anhydrase-2 by stopped-flow CO2 hydration assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. |
| AID237404 | Compound level in Red Blood Cells at 48 h, after exposure of 10 mL of Blood to compound solution by HPLC method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID382948 | Solubility in water | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1520071 | Binding affinity to recombinant human carbonic anhydrase 5a expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1563829 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis. |
| AID47747 | In vitro inhibition of purified human erythrocyte carbonic anhydrase II | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase. |
| AID1306526 | Inhibition of Vibrio cholerae alpha carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1256864 | Selectivity ratio, ratio of Ki for human carbonic anahydrase-1 to Ki for carbonic anhydrase-14 | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID1278562 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow carbon dioxide hydrase assay | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII. |
| AID365989 | Inhibition of human cloned CA14 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID1604489 | Inhibition of COX2 in mouse RAW264.7 cells assessed as reduction in LPS-induced inflammation by measuring PGE2 level at 1 uM treated 1 hr after LPS stimulation and measured after 18 hrs by ELISA (Rvb = (2437 +/- 93.17 pg/mL) | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID1161931 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Discovery of a new family of carbonic anhydrases in the malaria pathogen Plasmodium falciparum--the η-carbonic anhydrases. |
| AID327767 | Inhibition of human catalytic domain carbonic anhydrase 12 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID732025 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Carbonic anhydrase inhibitors: benzenesulfonamides incorporating cyanoacrylamide moieties are low nanomolar/subnanomolar inhibitors of the tumor-associated isoforms IX and XII. |
| AID612726 | Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID238467 | Inhibition constant against human carbonic anhydrase XII | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes. |
| AID1235245 | Inhibition of Pseudoalteromonas haloplanktis gamma-CA after 15 mins by stopped-flow/Co2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Cloning, characterization and anion inhibition studies of a new γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID496915 | Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1339400 | Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties. |
| AID669116 | Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID770585 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. |
| AID1071786 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Substituted benzene sulfonamides incorporating 1,3,5-triazinyl moieties potently inhibit human carbonic anhydrases II, IX and XII. |
| AID1498921 | Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration by stopped flow assay | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery. |
| AID238208 | Inhibitory constant against human Carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX. |
| AID411536 | Inhibition of human recombinant CA12 catalytic domain by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411536 | Inhibition of human recombinant CA12 catalytic domain by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1348314 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases. |
| AID1812657 | Inhibition of recombinant Schistosoma manson carbonic anhydrase pre-incubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Structural Insights into |
| AID1446115 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 30 uM after 72 hrs under normoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID299235 | Ratio of kcat to Km of human CA3 | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1655936 | Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer. |
| AID1570400 | Inhibition of recombinant human carbonic anhydrase1 preincubated for 10 mins followed by CO2 solution addition by phenol red dye based stopped flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Synthesis and exploration of 2-morpholino-4-phenylthiazol-5-yl acrylamide derivatives for their effects against carbonic anhydrase I, II, IX and XII isoforms as a non-sulfonamide class of inhibitors. |
| AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1161933 | Inhibition of Cryptococcus neoformans beta-carbonic anhydrase | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Discovery of a new family of carbonic anhydrases in the malaria pathogen Plasmodium falciparum--the η-carbonic anhydrases. |
| AID448553 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides. |
| AID327765 | Inhibition of human full length carbonic anhydrase 7 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1474383 | Cytotoxicity against human HT-29 cells assessed as cell viability at 100 uM after 72 hrs under hypoxic condition condition by MTT assay relative to control | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. |
| AID1731030 | Inhibition of human CAH14 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID724721 | Inhibition of human recombinant wild type CA2 by stopped-flow CO2 hydration method | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Restoring catalytic activity to the human carbonic anhydrase (CA) related proteins VIII, X and XI affords isoforms with high catalytic efficiency and susceptibility to anion inhibition. |
| AID1555966 | Inhibition of human carbonic anhydrase 6 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID382947 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.1660mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1292251 | Inhibition of human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. |
| AID1818307 | Inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID258729 | Inhibitory activity against cloned human CA1 | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib. |
| AID1072631 | Inhibition of human cytosolic carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID1235242 | Inhibition of archaeon Methanosarcina thermophila gamma-CA after 15 mins by stopped-flow/Co2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Cloning, characterization and anion inhibition studies of a new γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1303399 | Selectivity ratio, ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 12 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID588182 | Inhibition of Mycobacterium tuberculosis recombinant Rv3273 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID757566 | Inhibition of carbonic anhydrase 9 protein expression in human U251 cells under normoxic conditions by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID50336 | Inhibition concentration by inhibition of carbonic anhydrase from synaptosomes in Rat | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8 | Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives. |
| AID305490 | Inhibition of human recombinant CA12 catalytic domain by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions. |
| AID1237875 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 2 to Ki for Leishmania donovani chagasi beta-carbonic anhydrase | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1768057 | Inhibition of human carbonic anhydrase 2 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
| AID1809973 | Inhibition of recombinant human CA9 using 4-nitrophenylacetate as substrate by esterase assay | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID660366 | Inhibition of human CA2 pre-incubated for 15 mins by stopped-flow CO2 hydration method | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo. |
| AID1309027 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | N-Nitrosulfonamides: A new chemotype for carbonic anhydrase inhibition. |
| AID238247 | Ki value against human carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1809977 | Cytotoxicity against HCEC cells assessed as cell viability at 1% by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID195092 | Inhibitor level was measured in red blood cells at 60 min after exposure of 10 mL of blood to solutions by HPLC method | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID314826 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.25 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1408652 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity. |
| AID757584 | Inhibition of carbonic anhydrase 9 mRNA expression in human GaMG cells under hypoxic conditions at 4000 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by RT-PCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1193749 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID1755143 | Inhibition of recombinant human CA2 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII. |
| AID1373187 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 14 (20 to 280 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1723494 | Antibacterial activity against Enterococcus faecium NR-32065 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1170165 | Inhibition of human carbonic anhydrase 2 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID616473 | Inhibition of human carbonic anhydrase 6 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID238850 | Inhibitory activity against human carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma. |
| AID1633343 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1723507 | Inhibition of carbonic anhydrase in Enterococcus faecium HM-965 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of ambient air by CLSI protocol based broth microdilution assay | |||
| AID1753389 | Inhibition of recombinant human CA12 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities. |
| AID452820 | Inhibition of human recombinant CA12 catalytic domain expressed in Sf9 cells by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II. |
| AID1140122 | Inhibition of human carbonic anhydrase 12-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity. |
| AID1358715 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID1518941 | Inhibition of recombinant human carbonic anhydrase 12 at 1 nM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID644087 | Inhibition of human carbonic anhydrase 6 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID1061893 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Inhibition of carbonic anhydrases from the extremophilic bacteria Sulfurihydrogenibium yellostonense (SspCA) and S. azorense (SazCA) with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophe |
| AID1272996 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1691505 | Selectivity ratio of Ki for inhibition of recombinant human CA1 to Ki for inhibition of recombinant human CA9 | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID1753404 | Inhibition of recombinant human CA1 pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Insertion of metal carbenes into the anilinic N-H bond of unprotected aminobenzenesulfonamides delivers low nanomolar inhibitors of human carbonic anhydrase IX and XII isoforms. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1243119 | Inhibition of human carbonic anhydrase 9 at 10'-6 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1461938 | Inhibition of recombinant His6-tagged Francisella tularensis beta-CA (227 residues) expressed in Escherichia coli BL21(DE3) incubated for 15 mins by stopped-flow CO2 hydration assay | |||
| AID1394915 | Inhibition of cytosolic human carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID711212 | Inhibition of recombinant Vibrio cholerae carbonic anhydrase expressed in Escherichia coli (DE3) preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae. |
| AID1849565 | Binding affinity to human CA12 assessed as inhibition constant by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1354959 | Inhibition of human carbonic anhydrase 9 after 15 mins by stopped flow carbon dioxide hydration assay | 2018 | ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5 | Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology. |
| AID1245665 | Inhibition of carbonic anhydrase-2 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID311034 | Inhibition of human carbonic anhydrase 14 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID597963 | Inhibition of human CA2 by CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and crystallographic analysis of new sulfonamides incorporating NO-donating moieties with potent antiglaucoma action. |
| AID50352 | Inhibition constant evaluated for the inhibition of human CA I (Carbonic anhydrase I) | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1237482 | Inhibition of Coleofasciculus chthonoplastes carbonic anhydrase by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID257066 | Selectivity ratio for inhibiting CA VA over CA II | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID301576 | Inhibition of human recombinant CA 1 assessed as CO2 hydration by stopped flow kinetic assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID1170181 | Inhibition of human carbonic anhydrase 9 at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID616469 | Inhibition of human carbonic anhydrase 3 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID342475 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1422974 | Inhibition of recombinant Helicobacter pylori alpha carbonic anhydrase preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1237873 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 2 to Ki for Brucella suis beta-carbonic anhydrase 1 | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1563831 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis. |
| AID1422963 | Inhibition of recombinant human CA2 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1461937 | Inhibition of Helicobacter pylori beta-CA incubated for 15 mins by stopped-flow CO2 hydration assay | |||
| AID315100 | Inhibition of human carbonic anhydrase 2 assessed as 4-nitrophenyl phosphate hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID19197 | Partition coefficient (logP) | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides. |
| AID1439687 | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. |
| AID1556936 | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID316067 | Inhibition of human recombinant full length carbonic hydrase 7 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID484155 | Inhibition of full length human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1308828 | Inhibition of human recombinant carbonic anhydrase 9 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID93582 | Level in red blood cells after incubation of human erythrocytes for 60 min, was determined by EI method | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1824504 | Inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Synthesis, biological evaluation, and in silico studies of potential activators of apoptosis and carbonic anhydrase inhibitors on isatin-5-sulfonamide scaffold. |
| AID428374 | Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1809104 | Inhibition of recombinant human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis. |
| AID1454027 | Inhibition of recombinant human cytosolic carbonic anhydrase 2 expressed in Escherichia coli pretreated for 15 mins prior to testing by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases. |
| AID367615 | Inhibition of human recombinant full length CA7 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367615 | Inhibition of human recombinant full length CA7 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1757217 | Selectivity index, ratio of Ki for inhibition of human CA2 to Ki for inhibition of human CA12 | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID1335042 | Inhibition of human erythrocyte carbonic anhydrase 1 preincubated for 15 mins prior to testing by bromothymol blue-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Dithiocarbamates effectively inhibit the β-carbonic anhydrase from the dandruff-producing fungus Malassezia globosa. |
| AID762170 | Inhibition of cytosolic carbonic anhydrase 2 (unknown origin) preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design and synthesis of novel 4-(4-oxo-2-arylthiazolidin-3-yl)benzenesulfonamides as selective inhibitors of carbonic anhydrase IX over I and II with potential anticancer activity. |
| AID1373186 | Binding affinity to recombinant human full length N-terminal His-tagged carbonic anhydrase 13 (1 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID446440 | Inhibition of human recombinant carbonic anhydrase 14 expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors. |
| AID1859985 | Inhibition of human carbonic anhydrase 9 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide derivatives utilizing tail/dual-tail approaches as novel carbonic anhydrase inhibitors. |
| AID275807 | Inhibition of human recombinant cytosolic isozyme CA I by stopped-flow CO2 hydrase method | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID1312154 | Inhibition of Candida albicans beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID314760 | Inhibition of human carbonic anhydrase 9 catalytic domain | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID48132 | Inhibition constant against bovine Carbonic anhydrase IV, isolated from lung microsomes | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
| AID1518930 | Inhibition of recombinant human carbonic anhydrase 2 at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1439690 | Inhibition of recombinant human tumor-associated carbonic anhydrase 9 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. |
| AID300803 | Inhibition of human recombinant carbonic anhydrase 1 by CO2 hydration stopped-flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I and II, and extracellular isoforms IV, IX, and XII with sulfamides incorporating sugar moieties. |
| AID446437 | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors. |
| AID47902 | Inhibitory activity against human recombinant carbonic anhydrase II (CA2) | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
| AID589732 | Selectivity ratio of Ki for human cytosolic carbonic anhydrase 2 to Ki for Candida albicans Nce103 beta-carbonic anhydrase | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. |
| AID1272999 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 7 | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID367613 | Inhibition of human recombinant full length CA5B by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367613 | Inhibition of human recombinant full length CA5B by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1782944 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 1 to Ki for inhibition of recombinant human carbonic anhydrase 2 | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1461803 | Inhibition of human CA2 | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | 1,3-Oxazole-based selective picomolar inhibitors of cytosolic human carbonic anhydrase II alleviate ocular hypertension in rabbits: Potency is supported by X-ray crystallography of two leads. |
| AID238223 | Inhibitory constant against human Carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds. |
| AID328975 | Inhibition of human full length carbonic anhydrase 2 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID371554 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID758953 | Inhibition of human recombinant CA1 by CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14 | A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules. |
| AID1520082 | Binding affinity to recombinant human carbonic anhydrase 4 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID780930 | Binding affinity to human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Benzenesulfonamides with pyrimidine moiety as inhibitors of human carbonic anhydrases I, II, VI, VII, XII, and XIII. |
| AID231407 | Anticonvulsant potency ratio expressed as ratio ED50 of UK-12130 to that of compound during separate electroshock experiments | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides. |
| AID1306801 | Inhibition of human recombinant CA4 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Microwave assisted synthesis of novel acridine-acetazolamide conjugates and investigation of their inhibition effects on human carbonic anhydrase isoforms hCA I, II, IV and VII. |
| AID238084 | Inhibition constant against human (cloned) isozyme (hCA II) by CO2 hydration method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1304443 | Inhibition of human recombinant CA2 preincubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Synthesis of 4-(thiazol-2-ylamino)-benzenesulfonamides with carbonic anhydrase I, II and IX inhibitory activity and cytotoxic effects against breast cancer cell lines. |
| AID1565765 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | From random to rational: A discovery approach to selective subnanomolar inhibitors of human carbonic anhydrase IV based on the Castagnoli-Cushman multicomponent reaction. |
| AID1818313 | Selectivity index, ratio of Ki for inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration ass | |||
| AID50357 | Inhibitory effect on human carbonic anhydrase I | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. |
| AID725592 | Inhibition of human CA9 by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors. |
| AID1336993 | Selectivity ratio of Ki for human erythrocyte cytosolic carbonic anhydrase 2 to Ki for human membrane bound carbonic anhydrase 12 | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID1849533 | Binding affinity to human CA1 assessed as inhibition constant by SDS-PAGE analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID295292 | Inhibition of human recombinant CA5A after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID1188135 | Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID1821396 | Inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes. |
| AID1555963 | Inhibition of human carbonic anhydrase 4 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID1449743 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Synthesis and carbonic anhydrase inhibition of a series of SLC-0111 analogs. |
| AID1238072 | Inhibition of human erythrocytes CA1 using 4-nitrophenylacetate as substrate by esterase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Synthesis and carbonic anhydrase inhibitory properties of novel uracil derivatives. |
| AID353230 | Inhibition of human recombinant CA9 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties. |
| AID1238454 | Selectivity ratio of Ki for human carbonic anhydrase-1 to Ki for human carbonic anhydrase-12 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1703322 | Inhibition of human CA2 incubated for 15 mins by stopped- flow CO2 hydrase assay method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Discovery of first-in-class multi-target adenosine A |
| AID301570 | Activity of human recombinant CA 1 assessed as CO2 hydration | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID1548130 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID438008 | Inhibition of human membrane-bound carbonic anhydrase 9 catalytic domain after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1312218 | Inhibition of Plasmodium falciparum full length recombinant His-fused Eta-carbonic anhydrase domain preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Anion inhibition profiles of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum. |
| AID598731 | Inhibition of Salmonella Typhimurium carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay at pH 8.3 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID238787 | Inhibitory activity against human carbonic anhydrase II expressed in Escherichia coli BL21 | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties. |
| AID646243 | Inhibition of S-glutathionylated form of human recombinant carbonic anhydrase 7 using carbon-dioxide as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID727279 | Inhibition of full length human recombinant CA1 cytosolic isoform after 6 hrs by stopped-flow CO2 hydration method | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases. |
| AID331498 | Inhibition of human recombinant carbonic anhydrase 1 by CO2 hydration stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes. |
| AID1170183 | Inhibition of human carbonic anhydrase 12 at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1755146 | Inhibition of full length human CA12 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII. |
| AID314813 | Inhibition of human carbonic anhydrase 2 in presence of 10 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID484154 | Inhibition of full length human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1077014 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 12 | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1195031 | Inhibition of human CA-1 using p-nitro-phenylacetate as substrate by Lineweaver-Burk plot analysis | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II. |
| AID1076059 | Inhibition of human recombinant carbonic anhydrase 12-mediated CO2 hydration after 6 hrs by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | 6-Triazolyl-substituted sulfocoumarins are potent, selective inhibitors of the tumor-associated carbonic anhydrases IX and XII. |
| AID616475 | Inhibition of human carbonic anhydrase 9 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1446103 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1759812 | Inhibition of Vibrio cholerae gamma carbonic anhydrase preincubated with enzyme for 15 mins by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1162891 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | Quinazoline-sulfonamides with potent inhibitory activity against the α-carbonic anhydrase from Vibrio cholerae. |
| AID1238075 | Inhibition of human carbonic anhydrase-1 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII. |
| AID1766624 | Inhibition of recombinant human CA7 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Discovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations. |
| AID1849585 | Binding affinity to human recombinant CA5A assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1129145 | Inhibition of human recombinant cytosolic human carbonic anhydrase-2 incubated for 15 mins prior to testing by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7 | Synthesis and carbonic anhydrase I, II, IX and XII inhibition studies of 4-N,N-disubstituted sulfanilamides incorporating 4,4,4-trifluoro-3-oxo-but-1-enyl, phenacylthiourea and imidazol-2(3H)-one/thione moieties. |
| AID1277138 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins prior to testing by CO2 hydration-based stopped flow assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID1564387 | Inhibition of recombinant human carbonic anhydrase VA preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitors. |
| AID1175497 | Inhibition of human recombinant carbonic anhydrase 4 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID644086 | Inhibition of human carbonic anhydrase 4 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID1688231 | Inhibition of recombinant human carbonic anhydrase 2 measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID732028 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Carbonic anhydrase inhibitors: benzenesulfonamides incorporating cyanoacrylamide moieties are low nanomolar/subnanomolar inhibitors of the tumor-associated isoforms IX and XII. |
| AID299226 | Activity of human CA3 at pH 7.5 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID598727 | Inhibition of recombinant Mycobacterium tuberculosis Rv3273 carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay at pH 7.5 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID1266231 | Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped flow CO2 dehydration assay | 2016 | Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1 | Inhibition of carbonic anhydrase isoforms I, II, IV, VII and XII with carboxylates and sulfonamides incorporating phthalimide/phthalic anhydride scaffolds. |
| AID299250 | Inhibition of Helicobacter pylori beta carbonic anhydrase by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID311032 | Inhibition of human carbonic anhydrase 12 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1809972 | Inhibition of recombinant human CA2 using 4-nitrophenylacetate as substrate by esterase assay | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID48130 | Compound was evaluated for inhibition against bovine carbonic anhydrase IV | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. |
| AID1237870 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 1 to Ki for Brucella suis beta-carbonic anhydrase 2 | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1686868 | Inhibition of recombinant human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID1357841 | Inhibition of human cytosolic carbonic anhydrase 2 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | 2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents. |
| AID411533 | Inhibition of human recombinant CA6 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411533 | Inhibition of human recombinant CA6 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID50185 | Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors. |
| AID1170174 | Inhibition of human carbonic anhydrase 12 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1273033 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1460766 | Inhibition of human CA3 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID610539 | Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID739943 | Inhibition of human carbonic anhydrase-1 cytosolic isoform after 15 mins by Stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Structural effect of phenyl ring compared to thiadiazole based adamantyl-sulfonamides on carbonic anhydrase inhibition. |
| AID1543083 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped flow CO2 hydrase assay | |||
| AID1278412 | Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID749803 | Inhibition of human carbonic anhydrase-14 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID388307 | Ex vivo inhibition of Plasmodium falciparum growth in cultured cells after 48hrs as [3H]hypoxanthine uptake | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Carbonic anhydrase inhibitors: inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides-in vitro and in vivo studies. |
| AID387188 | Inhibition of human carbonic anhydrase 2 at 20 degC by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions. |
| AID1334827 | Inhibition of human recombinant carbonic anhydrase-1 preincubated for 6 hrs by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity. |
| AID1449738 | Inhibition of Malassezia globosa recombinant beta-carbonic anhydrase preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Inhibition of Malassezia globosa carbonic anhydrase with phenols. |
| AID1202645 | Inhibition of human membrane associated form of carbonic anhydrase-9 assessed as CO2 hydration activity incubated for 15 mins prior to testing by stopped flow method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis, carbonic anhydrase inhibition and cytotoxic activity of novel chromone-based sulfonamide derivatives. |
| AID50356 | Inhibitory activity against human cloned isoenzyme carbonic anhydrase I (hCA I), by esterase method. | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives. |
| AID408470 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID365980 | Inhibition of human cloned CA3 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID446436 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors. |
| AID758949 | Inhibition of Flaveria bidentis recombinant CA by CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14 | A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules. |
| AID1517564 | Inhibition of human carbonic anhydrase 2 at 10'-9 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID299229 | Activity of human CA12 at pH 7.5 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID293814 | Selectivity for human recombinant CA9 over human recombinant CA2 | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties. |
| AID367619 | Inhibition of human recombinant full length CA14 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367619 | Inhibition of human recombinant full length CA14 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID497128 | Inhibition of human recombinant carbonic anhydrase 1 Phe91Asn mutant expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors. |
| AID1061170 | Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis. |
| AID1666828 | Selectivity index, ratio of Ki for human carbonic anhydrase 12 to Ki for human carbonic anhydrase 2 | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID352788 | Inhibition of human recombinant CA2 by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Carbonic anhydrase inhibitors. Synthesis of 2,4,6-trimethylpyridinium derivatives of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides acting as potent inhibitors of the tumor-associated isoform IX and XII. |
| AID314798 | Inhibition of human carbonic anhydrase 2 in presence of 0.01 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1491569 | Inhibition of recombinant human carbonic anhydrase 12 assessed as reduction in CO2 hydration pretreated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | |
| AID1238076 | Inhibition of human carbonic anhydrase-2 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII. |
| AID1373169 | Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5B (40 to 317 residues) expressed in Escherichia coli Rosetta 2 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1387631 | Inhibition of recombinant human carbonic anhydrase 1 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines. |
| AID1688235 | Selectivity index, ratio of Ki for inhibition of recombinant human carbonic anhydrase 2 to inhibition of recombinant human carbonic anhydrase 12 | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID1061069 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii. |
| AID1352815 | Inhibition of human CA1 after 15 mins by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Structural investigations on coumarins leading to chromeno[4,3-c]pyrazol-4-ones and pyrano[4,3-c]pyrazol-4-ones: New scaffolds for the design of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1809108 | Solubility of the compound | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis. |
| AID1243107 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID314766 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.05 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1360264 | Inhibition of human carbonic anhydrase 9 expressed in Escherichia coli BL21 D3 strain using p-nitrophenyl acetate as substrate by UV/visible spectrophotometry | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents. |
| AID349605 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. |
| AID759697 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for Trypanosoma cruzi carbonic anhydrase | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | A class of sulfonamides with strong inhibitory action against the α-carbonic anhydrase from Trypanosoma cruzi. |
| AID726600 | Permeability across human Caco2 cells | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4 | A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma. |
| AID1287520 | Inhibition of recombinant Enterobacter sp. B13 beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13. |
| AID1655934 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer. |
| AID1173862 | Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | 4-Functionalized 1,3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of carbonic anhydrase isoforms hCA I, II, IX and XII. |
| AID1692372 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID1859984 | Inhibition of human carbonic anhydrase 2 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide derivatives utilizing tail/dual-tail approaches as novel carbonic anhydrase inhibitors. |
| AID320314 | Inhibition of human catalytic domain carbonic hydrase 12 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID311033 | Inhibition of mouse carbonic anhydrase 13 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID408474 | Selectivity for human cloned CA9 over human recombinant CA2 | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1308822 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID314803 | Inhibition of human carbonic anhydrase 9 in presence of 0.05 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID757565 | Inhibition of carbonic anhydrase 9 protein expression in human GaMG cells under hypoxic conditions at 4000 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1170178 | Inhibition of human carbonic anhydrase 1 at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID610547 | Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1446109 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 30 uM after 48 hrs under normoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1240209 | Inhibition of human carbonic anhydrase-1 by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID305486 | Inhibition of human recombinant CA2 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions. |
| AID166976 | Tested for level of sulfonamide in red blood cells of albino rabbits at 60 min post-administration of 50 mg/kg sulfonamides | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
| AID1692245 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII. |
| AID1266248 | Inhibition of human carbonic anhydrase-14 preincubated for 15 mins by stopped flow CO2 dehydration method | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies. |
| AID47903 | Inhibitory activity against human cloned carbonic anhydrase II (hCA II) | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. |
| AID648179 | Inhibition of human wild type carbonic anhydrase 2 Asn67Ile mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors. |
| AID1655395 | Inhibition of recombinant human carbonic anhydrase 12 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1733130 | Inhibition of recombinant human carbonic anhydrase 2 pre-incubated for 10 mins by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 39 | Synthesis and biological evaluation of novel 4,7-disubstituted coumarins as selective tumor-associated carbonic anhydrase IX and XII inhibitors. |
| AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1067225 | Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 12 | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. |
| AID1731021 | Inhibition of human CAH3 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1607537 | Inhibition of human recombinant carbonic anhydrase 5A preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID1474293 | Inhibition of recombinant human cytosolic carbonic anhydrase 2 pretreated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Evaluation of selenide, diselenide and selenoheterocycle derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors. |
| AID165488 | Reduction in maximum Intra ocular pressure in the rabbit model of ocular hypertension, when treated with a minimum effective oral dose of 1.25 mg/kg | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity. |
| AID1878297 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides. |
| AID1585352 | Inhibition of recombinant human carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID438010 | Inhibition of mouse full length cytosolic carbonic anhydrase 13 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1406818 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel hydrazido benzenesulfonamides-isatin conjugates: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID127482 | Ability to bind to monoclonal antibody IgE (Lb4), expressed as association constant (LogKA) | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Comparative molecular field analysis of haptens docked to the multispecific antibody IgE(Lb4) |
| AID1072632 | Inhibition of human cytosolic carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID731405 | Inhibition of human carbonic anhydrase 1 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | New selective carbonic anhydrase IX inhibitors: synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides. |
| AID1182978 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Synthesis of sulfonamides with effective inhibitory action against Porphyromonas gingivalis γ-carbonic anhydrase. |
| AID452819 | Inhibition of human recombinant CA9 catalytic domain expressed in Sf9 cells by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II. |
| AID1238447 | Inhibition of human carbonic anhydrase-1 incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID314819 | Inhibition of human carbonic anhydrase 2 in presence of 0.05 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1763379 | Inhibition of human CA2 by stopped-flow assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Developments of small molecules as inhibitors for carbonic anhydrase isoforms. |
| AID396640 | Inhibition of human carbonic anhydrase 12 by CO2 hydration assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. |
| AID299551 | Inhibition of Helicobacter pylori beta CA | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID620788 | Selectivity ratio of IC50 for human recombinant CA2 to IC50 for human recombinant CA9 | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1517242 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration incubated for 1 hr by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID1195081 | Inhibition of bovine carbonic anhydrase 2 assessed as hydrolysis of p-nitrophenyl acetate after 30 mins by spectrophotometric method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Diarylsulfonamides and their bioisosteres as dual inhibitors of alkaline phosphatase and carbonic anhydrase: Structure activity relationship and molecular modelling studies. |
| AID436751 | Selectivity ratio of Ki for human recombinant cytosolic carbonic anhydrase 2 to Ki for human recombinant full length mitochondrial carbonic anhydrase 5B | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
| AID732024 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 12 | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Carbonic anhydrase inhibitors: benzenesulfonamides incorporating cyanoacrylamide moieties are low nanomolar/subnanomolar inhibitors of the tumor-associated isoforms IX and XII. |
| AID620688 | Inhibition of human carbonic anhydrase 12-catalyzed CO2 hydration activity by stopped flow assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID669485 | Inhibition of human recombinant full length CA7-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, structure-activity relationship studies, and X-ray crystallographic analysis of arylsulfonamides as potent carbonic anhydrase inhibitors. |
| AID1703324 | Inhibition of human CA12 incubated for 15 mins by stopped- flow CO2 hydrase assay method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Discovery of first-in-class multi-target adenosine A |
| AID47745 | Compound was tested for inhibition of human carbonic anhydrase (hCA II) | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II. |
| AID620785 | Inhibition of human recombinant CA2 by CO2 hydration based stopped flow assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID382975 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.2 M hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1659545 | Inhibition of human carbonic anhydrase 9 using p-nitrophenyl acetate as substrate by UV-VIS spectrophotometric analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX. |
| AID1766622 | Inhibition of recombinant human CA1 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Discovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations. |
| AID1604481 | Inhibition of human CA4 pre-incubated for 6 hrs by stopped- flow CO2 hydrase assay method based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID25800 | The compound was evaluated for in Vitro corneal permeability at cornea intact | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route. |
| AID1356461 | Binding affinity to human carbonic anhydrase 1 by stopped flow CO2 hydration method | 2018 | ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7 | Targeting Tumor Associated Carbonic Anhydrases IX and XII: Highly Isozyme Selective Coumarin and Psoralen Inhibitors. |
| AID780927 | Binding affinity to human recombinant carbonic anhydrase 7 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Benzenesulfonamides with pyrimidine moiety as inhibitors of human carbonic anhydrases I, II, VI, VII, XII, and XIII. |
| AID753464 | Inhibition of full length carbonic anhydrase-2 in human erythrocytes | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening. |
| AID1607550 | Antinociceptive activity in CD-1 albino mouse model of oxaliplatin-induced neuropathic pain assessed as decrease in pain-related behaviour measured as licking latency at 100 mg/kg, po treated on day 15 post oxaliplatin treatment and measured after 15 mins | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID1753407 | Inhibition of recombinant human CA12 pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Insertion of metal carbenes into the anilinic N-H bond of unprotected aminobenzenesulfonamides delivers low nanomolar inhibitors of human carbonic anhydrase IX and XII isoforms. |
| AID411531 | Inhibition of human recombinant CA5A by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411531 | Inhibition of human recombinant CA5A by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID237411 | Compound level in Red Blood Cells at 60 min, after exposure of 10 mL of Blood to compound solution by electronic spectroscopic method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID238083 | Inhibition constant against human cloned isozyme (hCA IX) by CO2 hydration method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID1170182 | Inhibition of chimeric carbonic anhydrase 9 (unknown origin) expressing with full length CA2 (1 to 260) at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID452821 | Selectivity index, ratio of Kinact for human cloned full length CA2 to Kinact for human recombinant CA9 catalytic domain | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II. |
| AID1237477 | Inhibition of Pseudomonas aeruginosa PAO1 type-2 beta-carbonic anhydrase psCA3 expressed in Escherichia coli Tuner BL21 (DE3) cells pre-incubated for 15 mins at pH 8.3 and 293K by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID1427469 | Inhibition of recombinant human carbonic anhydrase-2 assessed as reduction in enzyme-catalyzed hydration activity using CO2 as substrate preincubated for 15 mins followed substrate addition measured after 10 to 100 sec by phenol red dye based stopped flow | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3- and 4-(hetero)arylisoxazol-5-amine scaffolds. |
| AID299543 | Inhibition of human CA5B | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID1195029 | Inhibition of human CA-1 using p-nitro-phenylacetate as substrate after 3 mins by UV-Vis spectrophotometry | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II. |
| AID1278997 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6 | Development of 3-(4-aminosulphonyl)-phenyl-2-mercapto-3H-quinazolin-4-ones as inhibitors of carbonic anhydrase isoforms involved in tumorigenesis and glaucoma. |
| AID1053404 | Inhibition of full length human cytosolic carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates. |
| AID1426787 | Inhibition of recombinant human CA4 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis. |
| AID497129 | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors. |
| AID1517570 | Inhibition of human carbonic anhydrase 12 at 10'-7 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1520079 | Binding affinity to recombinant human carbonic anhydrase 1 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID433253 | Inhibition of Candida glabrata carbonic anhydrase by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the pathogenic yeast Candida glabrata with anions. |
| AID1849545 | Binding affinity to human recombinant CA1 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID766612 | Inhibition of recombinant human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18 | Synthesis of novel acridine and bis acridine sulfonamides with effective inhibitory activity against the cytosolic carbonic anhydrase isoforms II and VII. |
| AID537653 | Inhibition of human carbonic anhydrase 2 esterase activity by spectrophotometry | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide. |
| AID603071 | Inhibition of human recombinant cytosolic carbonic anhydrase 13 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Conformational variability of different sulfonamide inhibitors with thienyl-acetamido moieties attributes to differential binding in the active site of cytosolic human carbonic anhydrase isoforms. |
| AID1723491 | Antibacterial activity against Enterococcus faecium HM968 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1655150 | Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors. |
| AID1518929 | Inhibition of recombinant human carbonic anhydrase 2 at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1565729 | Inhibition of human carbonic anhydrase 2 assessed as inhibitory constant incubated for 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID242842 | Kcat value against human carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1278995 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6 | Development of 3-(4-aminosulphonyl)-phenyl-2-mercapto-3H-quinazolin-4-ones as inhibitors of carbonic anhydrase isoforms involved in tumorigenesis and glaucoma. |
| AID1520072 | Binding affinity to recombinant human carbonic anhydrase 5b expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1565747 | Inhibition of human carbonic anhydrase 12 assessed as reduction in CO2 hydration at 10'-6 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID15233 | Distribution coefficient (D %) between octanol and buffer of pH 7.4 | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID314779 | Inhibition of human carbonic anhydrase 9 in presence of 10 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1520090 | Binding affinity to recombinant human carbonic anhydrase 14 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID409601 | Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Inhibition of aquaporin 4 by antiepileptic drugs. |
| AID1245666 | Inhibition of carbonic anhydrase-3 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1166970 | Inhibition of human CA-12 after 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Inhibition of carbonic anhydrase isoforms I, II, IX and XII with novel Schiff bases: identification of selective inhibitors for the tumor-associated isoforms over the cytosolic ones. |
| AID1626027 | Inhibition of human carbonic anhydrase 9 catalytic domain preincubated for 15 mins by CO2 hydration stopped-flow assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma. |
| AID1519758 | Inhibition of recombinant human carbonic anhydrase-2 at 1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1354954 | Inhibition of human carbonic anhydrase 1 after 15 mins by stopped flow carbon dioxide hydration assay | 2018 | ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5 | Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology. |
| AID1287517 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13. |
| AID1757214 | Selectivity index, ratio of Ki for inhibition of human CA1 to Ki for inhibition of human CA9 | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID1336561 | Inhibition of Pseudoalteromonas haloplanktis recombinant carbonic anhydrase gamma assessed as inhibition of CO2 hydration preincubated for 15 mins by Lineweaver-burk plot method | |||
| AID1373179 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 4 expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID514212 | Inhibition of human recombinant carbonic anhydrase 9 after 15 mins by stopped flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity. |
| AID244308 | Percent of mice protected against seizures induced by a maximal electroshock (50mA,0.2s) after 30 mg/kg compound was injected intraperitoneally; Not tested | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties. |
| AID1058390 | Inhibition of Saccharomyces cerevisiae carbonic anhydrase SceCA preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID1430529 | Inhibition of recombinant human carbonic anhydrase 1 assessed as inhibition of CO2 hydration incubated for 15 mins prior to testing by stopped flow CO2 hydration method | |||
| AID1478800 | Inhibition of human carbonic anhydrase 1 incubated for 10 mins by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Synthesis and biological evaluation of novel aromatic and heterocyclic bis-sulfonamide Schiff bases as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID47942 | Inhibitory activity against human carbonic anhydrase II | 2003 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17 | Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide. |
| AID1193678 | Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Synthesis of 6-aryl-substituted sulfocoumarins and investigation of their carbonic anhydrase inhibitory action. |
| AID1373177 | Binding affinity to recombinant human full length N-terminal His-tagged carbonic anhydrase 2 (1 to 260 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID414955 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID487850 | Inhibition of esterase activity of human carbonic anhydrase 2 by Lineweaver-Burke plot analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | A novel and one-pot synthesis of new 1-tosyl pyrrol-2-one derivatives and analysis of carbonic anhydrase inhibitory potencies. |
| AID415676 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for Caenorhabditis elegans carbonic anhydrase 4b | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Carbonic anhydrase inhibitors. The nematode alpha-carbonic anhydrase of Caenorhabditis elegans CAH-4b is highly inhibited by 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides. |
| AID1603061 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors. |
| AID644037 | Inhibition of human carbonic anhydrase 1 esterase activity using 4-nitrophenylacetate as substrate | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives. |
| AID114172 | Effective dose of perorally administered, that gives protection against max electroshock in mice | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides. |
| AID1071785 | Inhibition of human transmembrane carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Substituted benzene sulfonamides incorporating 1,3,5-triazinyl moieties potently inhibit human carbonic anhydrases II, IX and XII. |
| AID264314 | Selectivity for human CA9 over CA2 | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
| AID1570399 | Inhibition of recombinant human carbonic anhydrase2 preincubated for 10 mins followed by CO2 solution addition by phenol red dye based stopped flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Synthesis and exploration of 2-morpholino-4-phenylthiazol-5-yl acrylamide derivatives for their effects against carbonic anhydrase I, II, IX and XII isoforms as a non-sulfonamide class of inhibitors. |
| AID48298 | Inhibition against human carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase. |
| AID1453369 | Inhibition of carbonic anhydrase-2 in human erythrocyte membranes assessed as reduction in H+ release using CO2 as substrate by bromine thymol blue indicator based assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives. |
| AID314759 | Inhibition of human carbonic anhydrase 2 | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID464215 | Inhibition of bovine carbonic anhydrase assessed as conversion of 4-nitrophenyl acetate to 4-nitrophnolate after 5 mins | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Synthesis and investigation of inhibition effect of fluorinated sulfonamide derivatives on carbonic anhydrase. |
| AID1878298 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides. |
| AID669486 | Inhibition of human recombinant CA9 catalytic domain-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, structure-activity relationship studies, and X-ray crystallographic analysis of arylsulfonamides as potent carbonic anhydrase inhibitors. |
| AID1468991 | Binding affinity to human CA9 catalytic domain expressed in mammalian expression system assessed as dissociation rate constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID314776 | Inhibition of human carbonic anhydrase 9 in presence of 1.00 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID526866 | Binding affinity to human recombinant carbonic anhydrase 13 by isothermal titration calorimetry assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID314812 | Inhibition of human carbonic anhydrase 9 in presence of 1.00 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID496920 | Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1303396 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 min to 72 hrs by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID1061037 | Inhibition of human CA4 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID238255 | Ki value against human carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1565728 | Inhibition of human carbonic anhydrase 1 assessed as inhibitory constant incubated for 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID347431 | Selectivity ratio of Ki human CA1 to Ki human CA9 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. |
| AID408475 | Selectivity for human cloned CA12 over human recombinant CA1 | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1548133 | Inhibition of Vibrio cholerae alpha carbonic anhydrase incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID603068 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Conformational variability of different sulfonamide inhibitors with thienyl-acetamido moieties attributes to differential binding in the active site of cytosolic human carbonic anhydrase isoforms. |
| AID166974 | Tested for level of sulfonamide in red blood cells of albino rabbits at 120 min post-administration of 50 mg/kg sulfonamides | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
| AID667535 | Inhibition of human CA4 using 4NPA as substrate for 3 mins by Lineweaver burk plot analysis | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols and their derivatives including natural products: vidalol B. |
| AID1504903 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors. |
| AID20926 | Solubility, pH 7.2 phosphate buffer at 32 degree C | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. |
| AID1518949 | Inhibition of recombinant human carbonic anhydrase 9 at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1564594 | Inhibition of recombinant human carbonic anhydrase 4 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity. |
| AID552130 | Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. |
| AID237410 | Compound level in Red Blood Cells at 30 min, after exposure of 10 mL of Blood to compound solution by electronic spectroscopic method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID1336566 | Inhibition of human recombinant carbonic anhydrase-7 using CO2 as substrate preincubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors. |
| AID762168 | Selectivity ratio of Ki for cytosolic carbonic anhydrase 2 (unknown origin) to Ki for carbonic anhydrase 9 (unknown origin) | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design and synthesis of novel 4-(4-oxo-2-arylthiazolidin-3-yl)benzenesulfonamides as selective inhibitors of carbonic anhydrase IX over I and II with potential anticancer activity. |
| AID1570401 | Inhibition of recombinant human carbonic anhydrase9 preincubated for 10 mins followed by CO2 solution addition by phenol red dye based stopped flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Synthesis and exploration of 2-morpholino-4-phenylthiazol-5-yl acrylamide derivatives for their effects against carbonic anhydrase I, II, IX and XII isoforms as a non-sulfonamide class of inhibitors. |
| AID411537 | Inhibition of mouse recombinant CA13 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411537 | Inhibition of mouse recombinant CA13 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1422972 | Inhibition of recombinant human CA13 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID299545 | Inhibition of human CA7 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID1757210 | Inhibition of human CA1 by stopped- flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID587132 | Inhibition of Leptonychotes weddellii alpha-carbonic anhydrase after 15 mins by CO2 hydrase assay at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID242851 | Kcat value against mouse carbonic anhydrase VII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1812658 | Selectivity ratio of Ki for inhibition of recombinant human carbonic anhydrase 2 to Ki for inhibition of recombinant Schistosoma manson carbonic anhydrase | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Structural Insights into |
| AID1442867 | Inhibition of recombinant human Carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action. |
| AID1752206 | Inhibition of recombinant human carbonic anhydrase 12 by stopped-flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1154446 | Inhibition of human cloned cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Carbonic anhydrase inhibitors. Synthesis of a novel series of 5-substituted 2,4-dichlorobenzenesulfonamides and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII. |
| AID315101 | Inhibition of mouse carbonic anhydrase 13 assessed as 4-nitrophenyl phosphate hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID314799 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.01 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1387634 | Inhibition of recombinant human carbonic anhydrase 12 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines. |
| AID1379902 | Inhibition of recombinant human full-length carbonic anhydrase 1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. |
| AID775831 | Inhibition of HDAC2 (unknown origin)-mediated deacetylation at 10 uM preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID1175498 | Inhibition of human recombinant carbonic anhydrase 5A pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1623427 | Inhibition of human carbonic anhydrase 12 assessed as reduction in CO2 hydration after 15 mins by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment. |
| AID342476 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1275630 | Inhibition of human carbonic anhydrase 9 for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Kinetic and X-ray crystallographic investigations on carbonic anhydrase isoforms I, II, IX and XII of a thioureido analog of SLC-0111. |
| AID1292250 | Inhibition of human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. |
| AID1689401 | Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1125514 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 | Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII. |
| AID320315 | Inhibition of mouse recombinant full length carbonic hydrase 13 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID620790 | Cytotoxicity against CA9-deficient chinese hamster PS120 cells assessed as cell viability at 30 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID597964 | Inhibition of human CA4 by CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and crystallographic analysis of new sulfonamides incorporating NO-donating moieties with potent antiglaucoma action. |
| AID1189118 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydrase Assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Carbonic Anhydrase Inhibition with Benzenesulfonamides and Tetrafluorobenzenesulfonamides Obtained via Click Chemistry. |
| AID1193679 | Inhibition of human tumor-associated carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Synthesis of 6-aryl-substituted sulfocoumarins and investigation of their carbonic anhydrase inhibitory action. |
| AID1230149 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies. |
| AID601813 | Inhibition of human carbonic anhydrase 1 preincubated with compound for 15 mins by carbon dioxide hydration assay | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV. |
| AID1239228 | Inhibition of human recombinant carbonic anhydrase-9 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties. |
| AID314792 | Inhibition of human carbonic anhydrase 2 in presence of 1.00 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1202644 | Inhibition of human cytosolic form of carbonic anhydrase-2 assessed as CO2 hydration activity incubated for 15 mins prior to testing by stopped flow method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis, carbonic anhydrase inhibition and cytotoxic activity of novel chromone-based sulfonamide derivatives. |
| AID1373164 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 1 (3 to 261 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID597962 | Inhibition of human CA1 by CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and crystallographic analysis of new sulfonamides incorporating NO-donating moieties with potent antiglaucoma action. |
| AID239126 | Inhibitory constant against catalytic domain of human carbonic anhydrase XII | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. |
| AID1067227 | Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. |
| AID1306837 | Inhibition of human carbonic anhydrase 2 preincubated for 6 hrs at 4 degC measured for 10 to 100 secs by stopped-flow carbon dioxide hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1,6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors. |
| AID417830 | Inhibition of human recombinant full length CA5B by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1423029 | Inhibition of human CA2 by Lineweaver-Burk plot analysis | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides. |
| AID299243 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1140816 | Inhibition of human carbonic anhydrase 2-catalyzed CO2 hydration preincubated for 10 mins by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of human cytosolic isoforms I and II with (reduced) Schiff's bases incorporating sulfonamide, carboxylate and carboxymethyl moieties. |
| AID589731 | Selectivity ratio of Ki for human cytosolic carbonic anhydrase 2 to Ki for Cryptococcus neoformans Can2 beta-carbonic anhydrase | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. |
| AID1256862 | Inhibition of human carbonic anhydrase-12 assessed as CO2 hydration activity by stopped-flow method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID1626028 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma. |
| AID411530 | Inhibition of human recombinant CA4 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411530 | Inhibition of human recombinant CA4 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1768058 | Inhibition of human carbonic anhydrase 9 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1347713 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | |||
| AID1442650 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip administered 3 hrs prior to 50 mA current induction | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID1593065 | Inhibition of full length human CA 1 | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines. |
| AID1469005 | Binding affinity to human N-terminal full length His-tagged CA13 (1 to 262 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic dissociation rate constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID50365 | Inhibition against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase. |
| AID1468997 | Binding affinity to human full length His-tagged CA2 (1 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as thermodynamic equilibrium constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1902652 | Inhibition of recombinant human CA 1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID1565746 | Inhibition of human carbonic anhydrase 12 assessed as reduction in CO2 hydration at 10'-7 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1709149 | Inhibition of recombinant human carbonic anhydrase 13 by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | 3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation. |
| AID317583 | Selectivity for human CA9 over human CA2 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. |
| AID1731023 | Inhibition of human CAH5A expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID620644 | Cytotoxicity against chinese hamster PS120 cells expressing CA9 assessed as cell viability at 100 uM and pH 6.4 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID678518 | Inhibition of human CA12 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors. |
| AID417831 | Inhibition of human recombinant full length CA6 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID644084 | Inhibition of human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID1204095 | Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-2 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-12 | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII. |
| AID614105 | Inhibition of human cloned carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Carbonic anhydrase inhibitors. Synthesis, molecular structures, and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with novel 3-pyridinesulfonamide derivatives. |
| AID1308831 | Inhibition of human recombinant carbonic anhydrase 14 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID427122 | Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID387189 | Inhibition of Methanobacterium thermoautotrophicum Cab at 20 degC by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions. |
| AID1379156 | Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino) benzenesulfonamides: Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular modelling studies. |
| AID1474381 | Inhibition of recombinant human carbonic anhydrase 9 using 4-nitrophenylacetate as substrate pretreated for 15 mins prior to test by spectrophotometric method | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. |
| AID1717283 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Sulfonamide/sulfamate switch with a series of piperazinylureido derivatives: Synthesis, kinetic and in silico evaluation as carbonic anhydrase isoforms I, II, IV, and IX inhibitors. |
| AID1067230 | Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. |
| AID1688237 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID1520087 | Binding affinity to recombinant human carbonic anhydrase 9 expressed in mammalian cell expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID620691 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 9 catalytic domain | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID1691503 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID352790 | Inhibition of human CA12 catalytic domain by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Carbonic anhydrase inhibitors. Synthesis of 2,4,6-trimethylpyridinium derivatives of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides acting as potent inhibitors of the tumor-associated isoform IX and XII. |
| AID1468990 | Binding affinity to human CA9 catalytic domain expressed in mammalian expression system assessed as association rate constant after 60 secs at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID287699 | Inhibition of human recombinant carbonic anhydrase 2 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates. |
| AID623070 | Inhibition of recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis of glycoconjugate carbonic anhydrase inhibitors by ruthenium-catalysed azide-alkyne 1,3-dipolar cycloaddition. |
| AID1727541 | Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion. |
| AID1166265 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel sulfonamides bearing pyrrole and pyrrolopyrimidine moieties as carbonic anhydrase inhibitors: Synthesis, cytotoxic activity and molecular modeling. |
| AID255389 | Selectivity is measured as ratio of Ki value of Carbonic anhydrase II to that of Carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides. |
| AID1596541 | Selectivity index, ratio of Ki of human carbonic anhydrase 2 to Ki of human carbonic anhydrase 12 | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID396641 | Inhibition of human carbonic anhydrase 14 by CO2 hydration assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. |
| AID1442870 | Inhibition of recombinant human Carbonic anhydrase 9 assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action. |
| AID222125 | Inhibition of cloned isozyme, human carbonic anhydrase I | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Carbonic anhydrase inhibitors: synthesis of sulfonamides incorporating dtpa tails and of their zinc complexes with powerful topical antiglaucoma properties. |
| AID1571211 | Selectivity ratio of IC50 for recombinant human carbonic anhydrase-2 expressed in Escherichia coli to IC50 for human carbonic anhydrase-9 | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies. |
| AID1166268 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 12 | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel sulfonamides bearing pyrrole and pyrrolopyrimidine moieties as carbonic anhydrase inhibitors: Synthesis, cytotoxic activity and molecular modeling. |
| AID1469001 | Binding affinity to human N-terminal full length His-tagged CA13 (1 to 262 residues) expressed in Escherichia coli BL21(DE3) assessed as association rate constant after 60 secs at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID620685 | Inhibition of human carbonic anhydrase 1-catalyzed CO2 hydration activity by stopped flow assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID327761 | Inhibition of human full length carbonic anhydrase 4 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID493891 | Inhibition of human recombinant carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1231561 | Inhibition of human carbonic anhydrase-9 pre-incubated for 15 mins by stopped-flow CO2 hydration assay based Lineweaver-Burk plot method | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors. |
| AID764498 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Inhibition of tumor-associated human carbonic anhydrase isozymes IX and XII by a new class of substituted-phenylacetamido aromatic sulfonamides. |
| AID1720898 | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition constant preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | New coumarin/sulfocoumarin linked phenylacrylamides as selective transmembrane carbonic anhydrase inhibitors: Synthesis and in-vitro biological evaluation. |
| AID1254157 | Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22 | New natural product carbonic anhydrase inhibitors incorporating phenol moieties. |
| AID733595 | Inhibition of human recombinant carbonic anhydrase-12-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | o-Benzenedisulfonimido-sulfonamides are potent inhibitors of the tumor-associated carbonic anhydrase isoforms CA IX and CA XII. |
| AID1277137 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by CO2 hydration-based stopped flow assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID300804 | Inhibition of human recombinant carbonic anhydrase 2 by CO2 hydration stopped-flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I and II, and extracellular isoforms IV, IX, and XII with sulfamides incorporating sugar moieties. |
| AID757570 | Inhibition of carbonic anhydrase 9 protein expression in human U251 cells under hypoxic conditions treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1355471 | Inhibition of recombinant human CA2 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | 4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors. |
| AID314781 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.01 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID586999 | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 min by CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis. |
| AID1373172 | Binding affinity to recombinant human carbonic anhydrase 9 (1 to 260 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1170188 | Inhibition of chimeric carbonic anhydrase 9 (unknown origin) expressing with full length CA2 (1 to 260) at pH7 and 25 degC by stopped-flow kinetic inhibition assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID93583 | Level in red blood cells after incubation of human erythrocytes for 60 min, was determined by ES method | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1061068 | Inhibition of Leishmania donovani chagasi recombinant beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii. |
| AID1422965 | Inhibition of recombinant human CA4 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1243106 | Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID660368 | Inhibition of human CA12 pre-incubated for 15 mins by stopped-flow CO2 hydration method | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo. |
| AID1275565 | Selectivity ratio, ratio of Ki for human carbonic anhydrase-1 to Ki for human carbonic anhydrase-2 | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID50344 | Inhibitory activity of compound against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. |
| AID1170160 | Inhibition of human CA-12 by stopped flow CO2 hydrase assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | A class of 4-sulfamoylphenyl-ω-aminoalkyl ethers with effective carbonic anhydrase inhibitory action and antiglaucoma effects. |
| AID1736570 | Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | |||
| AID1241138 | Inhibition of human carbonic anhydrase-12 incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Exploring new Probenecid-based carbonic anhydrase inhibitors: Synthesis, biological evaluation and docking studies. |
| AID1689404 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay to Ki for recombinant human carbonic anhydrase 12 preincubated with enzyme for 15 mins by | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1872739 | Binding affinity to carbonic anhydrase 2 (unknown origin) assessed as inhibition constant | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy. |
| AID314788 | Inhibition of human carbonic anhydrase 9 in presence of 0.10 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID515780 | Intrinsic solubility of the compound in water | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19 | QSAR-based solubility model for drug-like compounds. |
| AID1058182 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | A prodrug approach toward cancer-related carbonic anhydrase inhibition. |
| AID1543084 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins by stopped flow CO2 hydrase assay | |||
| AID166750 | Variation of intraocular pressure in fifth day at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID238315 | Ki value against human carbonic anhydrase VII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID598014 | Inhibition of human recombinant CA9 catalytic domain by CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and crystallographic analysis of new sulfonamides incorporating NO-donating moieties with potent antiglaucoma action. |
| AID1686880 | Anticonvulsant activity in Swiss Albino mouse assessed as protection against seizure at 100 mg/kg, ip measured after 3 hrs by sc-PTZ seizure test relative to control | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID244541 | Inhibition constant against human recombinant carbonic anhydrase IX catalytic domain | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumo |
| AID1275911 | Inhibition of Vibrio cholerae alpha-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae. |
| AID1570386 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by phenol red staining-based stopped flow CO2 hydrase assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure. |
| AID365986 | Inhibition of human cloned CA9 catalytic domain by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID1755142 | Inhibition of recombinant human CA1 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII. |
| AID1245667 | Inhibition of carbonic anhydrase-5A (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1818407 | Inhibition of human CA12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors. |
| AID299547 | Inhibition of human CA12 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID486934 | Inhibition of human cloned carbonic anhydrase 9 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID486934 | Inhibition of human cloned carbonic anhydrase 9 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1520068 | Binding affinity to recombinant human carbonic anhydrase 2 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID780323 | Inhibition of human carbonic anhydrase7 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID1660018 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID1782943 | Inhibition of recombinant human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID314770 | Inhibition of human carbonic anhydrase 9 in presence of 0.10 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1517572 | Inhibition of human carbonic anhydrase 12 at 10'-5 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1818311 | Selectivity index, ratio of Ki for inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration ass | |||
| AID1275559 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 9 | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1731965 | Inhibition of MMP2 (unknown origin) using Mca-Lys-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 5 min followed by substrate addition and measured for 30 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II. |
| AID382941 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1237475 | Inhibition of human carbonic anhydrase-2 by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID1142833 | Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11 | Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID275809 | Inhibition of catalytic domain of human recombinant CA IX | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID587000 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 min by CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis. |
| AID1350477 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
| AID1237869 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 1 to Ki for Brucella suis beta-carbonic anhydrase 1 | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1468993 | Binding affinity to human CA9 catalytic domain expressed in mammalian expression system assessed as intrinsic dissociation rate constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID342483 | Inhibition of human carbonic anhydrase 9 catalytic domain by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1873664 | Inhibition of recombinant human carbonic anhydrase 1 assessed as inhibition constant incubated for 1 hr prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry, 08-01, Volume: 67 | Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation. |
| AID484166 | Inhibition of full length mouse carbonic anhydrase 15 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1578355 | Inhibition of recombinant human CA7 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors. |
| AID1659546 | Inhibition of human carbonic anhydrase 5A using p-nitrophenyl acetate as substrate by UV-VIS spectrophotometric analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX. |
| AID367608 | Inhibition of human recombinant full length CA1 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367608 | Inhibition of human recombinant full length CA1 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID275806 | Inhibition of full length human recombinant CA VI | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID1347712 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | |||
| AID1449746 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Synthesis and carbonic anhydrase inhibition of a series of SLC-0111 analogs. |
| AID727276 | Inhibition of human recombinant transmembrane CA12 catalytic domain after 6 hrs by stopped-flow CO2 hydration method | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases. |
| AID623074 | Selectivity ratio of Ki for carbonic anhydrase 2 to Ki for carbonic anhydrase 9 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis of glycoconjugate carbonic anhydrase inhibitors by ruthenium-catalysed azide-alkyne 1,3-dipolar cycloaddition. |
| AID1275628 | Inhibition of human carbonic anhydrase 1 for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Kinetic and X-ray crystallographic investigations on carbonic anhydrase isoforms I, II, IX and XII of a thioureido analog of SLC-0111. |
| AID526859 | Binding affinity to human recombinant carbonic anhydrase 1 by thermal shift assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID743515 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID441717 | Inhibition of mouse recombinant CA15 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1077016 | Inhibition of human carbonic anhydrase 12-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1517571 | Inhibition of human carbonic anhydrase 12 at 10'-6 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1652404 | Inhibition of human CA5B pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID353231 | Inhibition of human recombinant CA12 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties. |
| AID1707345 | Inhibition of recombinant human carbonic anhydrase 7 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors. |
| AID1556938 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 1 expressed in Escherichia coli to Ki for human recombinant carbonic anhydrase 12 expressed in Escherichia coli | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID48297 | Compound was evaluated for inhibition against human carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. |
| AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1278563 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow carbon dioxide hydrase assay | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII. |
| AID577529 | Inhibition of human carbonic anhydrase XII by spectrophotometry at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID1474385 | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability at 100 uM after 72 hrs under hypoxic condition by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. |
| AID1478801 | Inhibition of human carbonic anhydrase 2 incubated for 10 mins by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Synthesis and biological evaluation of novel aromatic and heterocyclic bis-sulfonamide Schiff bases as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID382950 | Solubility in water in presence of 0.0302 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID299239 | Ratio of kcat to Km of human CA14 | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID314785 | Inhibition of human carbonic anhydrase 9 in presence of 0.05 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID314782 | Inhibition of human carbonic anhydrase 9 in presence of 0.01 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1158139 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties. |
| AID1061036 | Inhibition of human CA6 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID752643 | Selectivity ratio of Ki for Sachcharomyces cerevisiae beta carbonic anhydrase to Ki for human carbonic anhydrase-2 | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Carbonic anhydrase inhibitors. Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase. |
| AID1520088 | Binding affinity to recombinant human carbonic anhydrase 12 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID48309 | Inhibition of murine mitochondrial isozyme Carbonic anhydrase V at 20 degrees C | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
| AID1517546 | Inhibition of human carbonic anhydrase 12 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1460769 | Inhibition of human CA5B by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1518932 | Inhibition of recombinant human carbonic anhydrase 9 assessed as residual activity at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID369273 | Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID512003 | Inhibition of human cloned catalytic domain of CA9 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID512003 | Inhibition of human cloned catalytic domain of CA9 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1251958 | Inhibition of recombinant human carbonic anhydrase 2 expressed in Escherichia coli incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII. |
| AID195090 | Inhibitor level was measured in red blood cells at 30 min after exposure of 10 mL of blood to solutions by electronic spectroscopic (ES) method | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID293194 | Inhibition of human recombinant CA14 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides. |
| AID314774 | Inhibition of human carbonic anhydrase 2 in presence of 1.00 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID299548 | Inhibition of mouse CA13 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID1254159 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22 | New natural product carbonic anhydrase inhibitors incorporating phenol moieties. |
| AID1633350 | Inhibition of Cryptococcus neoformans carbonic anhydrase preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID757562 | Inhibition of carbonic anhydrase 9 protein expression in human U373 cells under hypoxic conditions at 4000 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID382968 | Solubility in water in presence of 0.1660mol/l hydroxypropyl-beta-cyclodextrin and 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID367618 | Inhibition of mouse recombinant full length CA13 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367618 | Inhibition of mouse recombinant full length CA13 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1237883 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 1 to Ki for Cryptococcus neoformans var. grubii beta-carbonic anhydrase | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1756970 | Inhibition of human carbonic anhydrase 9 using p-nitrophenyl acetate as substrate by UV-VIS spectrophotometric analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
| AID299249 | Inhibition of Helicobacter pylori alpha carbonic anhydrase by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID577531 | Inhibition of Brucella suis carbonic anhydrase I by spectrophotometry at pH 8.3 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID747807 | Inhibition of recombinant human CA9 transmembrane isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID1751410 | Inhibition of human CA9 measured by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies. |
| AID1158137 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties. |
| AID757564 | Inhibition of carbonic anhydrase 9 protein expression in human GaMG cells under normoxic conditions by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID603449 | Inhibition of human full length cytosolic isoform of carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1560582 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID416126 | Inhibition of human erythrocyte CA2 esterase activity using 4-nitrophenyl acetate substrate | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols. |
| AID47923 | Dissociation constant against Carbonic anhydrase II was reported in experiment 1 | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
| AID365988 | Inhibition of mouse CA13 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID493893 | Inhibition of human recombinant carbonic anhydrase 13 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1162893 | Selectivity ratio of Ki for Vibrio cholerae alpha-carbonic anhydrase to Ki for human carbonic anhydrase 1 | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | Quinazoline-sulfonamides with potent inhibitory activity against the α-carbonic anhydrase from Vibrio cholerae. |
| AID1652403 | Inhibition of human CA5A pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID1731968 | Inhibition of human CA2 incubated for 15 mins by stopped-flow CO2 hydration kinetic assay based Cheng-Prusoff equation analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II. |
| AID339676 | Inhibition of human recombinant carbonic anhydrase 12 catalytic domain by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID299237 | Ratio of kcat to Km of human CA5B | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1478803 | Inhibition of human carbonic anhydrase 9 incubated for 10 mins by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Synthesis and biological evaluation of novel aromatic and heterocyclic bis-sulfonamide Schiff bases as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID1723519 | Apparent permeability across basolateral to apical side in human Caco2 cells | |||
| AID588183 | Inhibition of Mycobacterium tuberculosis recombinant Rv1284 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID772920 | Inhibition of human carbonic anhydrase-12 by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20 | Effect of incorporating a thiophene tail in the scaffold of acetazolamide on the inhibition of human carbonic anhydrase isoforms I, II, IX and XII. |
| AID257062 | Inhibition of recombinant human cytosolic isozyme CA I | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID367653 | Inhibition of human carbonic anhydrase 1 measured by CO2 hydration reaction assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Carbonic anhydrase inhibitors: inhibition studies of a coral secretory isoform with inorganic anions. |
| AID1427077 | Inhibition of human recombinant carbonic anhydrase 4 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies. |
| AID314778 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 10 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID314787 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.10 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID411538 | Inhibition of human recombinant CA14 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411538 | Inhibition of human recombinant CA14 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1888316 | Inhibition of recombinant human carbonic anhydrase 1 assessed as inhibition constant preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain. |
| AID496921 | Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1266244 | Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped flow CO2 dehydration method | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies. |
| AID441716 | Inhibition of human recombinant CA14 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1129147 | Inhibition of human recombinant transmembrane tumor associated carbonic anhydrase-12 incubated for 15 mins prior to testing by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7 | Synthesis and carbonic anhydrase I, II, IX and XII inhibition studies of 4-N,N-disubstituted sulfanilamides incorporating 4,4,4-trifluoro-3-oxo-but-1-enyl, phenacylthiourea and imidazol-2(3H)-one/thione moieties. |
| AID1360102 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and X-ray crystallography of selenides bearing benzenesulfonamide moiety with neuropathic pain modulating effects. |
| AID1278410 | Inhibition of Porphyromonas gingivalis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID1449741 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant Malassezia globosa beta-carbonic anhydrase | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Inhibition of Malassezia globosa carbonic anhydrase with phenols. |
| AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1459106 | Selectivity ratio of IC50 for human erythrocyte carbonic anhydrase-1 to IC50 for human erythrocyte carbonic anhydrase-2 | |||
| AID1731026 | Inhibition of human CAH7 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID350900 | Inhibition of CO2-hydratase activity of human carbonic anhydrase 2 by CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Effects of new 5-amino-1,3,4-thiadiazole-2-sulfonamide derivatives on human carbonic anhydrase isozymes. |
| AID1460772 | Inhibition of human CA9 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1852041 | Inhibition of recombinant human CA2 pre-incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1170176 | Inhibition of human carbonic anhydrase 13 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1688232 | Inhibition of recombinant human carbonic anhydrase 9 measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID353228 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties. |
| AID1782941 | Inhibition of recombinant human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID243112 | Ratio of Kcat/Km against human carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1275556 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1519766 | Inhibition of recombinant human carbonic anhydrase-12 at 1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1534902 | Inhibition of recombinant full length human carbonic anhydrase-2 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID1655148 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors. |
| AID725593 | Inhibition of human CA12 by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors. |
| AID1304442 | Inhibition of human recombinant CA1 preincubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Synthesis of 4-(thiazol-2-ylamino)-benzenesulfonamides with carbonic anhydrase I, II and IX inhibitory activity and cytotoxic effects against breast cancer cell lines. |
| AID1491568 | Inhibition of recombinant human carbonic anhydrase 9 assessed as reduction in CO2 hydration pretreated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | |
| AID316069 | Inhibition of human catalytic domain carbonic hydrase 12 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1519751 | Inhibition of recombinant human carbonic anhydrase-1 at 0.01 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID382953 | Solubility in water in presence of 0.1132 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID441711 | Inhibition of human recombinant CA6 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID238323 | Inhibitory activity against human Carbonic anhydrase II | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Carbonic anhydrase inhibitors: the first on-resin screening of a 4-sulfamoylphenylthiourea library. |
| AID462276 | Inhibition of human CA6 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1405949 | Inhibition of human recombinant carbonic anhydrase 1 assessed as CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye-based stopped-flow assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal. |
| AID1723496 | Antibacterial activity against Enterococcus faecium NR-31916 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID437836 | Inhibition of human full length membrane-bound carbonic anhydrase 4 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1859983 | Inhibition of human carbonic anhydrase 1 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide derivatives utilizing tail/dual-tail approaches as novel carbonic anhydrase inhibitors. |
| AID1556934 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID1723500 | Antibacterial activity against Enterococcus faecalis HM-334 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1564417 | Inhibition of recombinant human CA12 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1519745 | Inhibition of recombinant human carbonic anhydrase-9 incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID414956 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID650297 | Inhibition of human carbonic anhydrase 12 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases. |
| AID327769 | Inhibition of human full length carbonic anhydrase 14 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID730874 | Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | An α-carbonic anhydrase from the thermophilic bacterium Sulphurihydrogenibium azorense is the fastest enzyme known for the CO2 hydration reaction. |
| AID314810 | Inhibition of human carbonic anhydrase 2 in presence of 1.00 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1548132 | Inhibition of Sulfurihydrogenibium yellowstonense alpha carbonic anhydrase incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID350902 | Inhibition of esterase activity of human carbonic anhydrase 2 by CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Effects of new 5-amino-1,3,4-thiadiazole-2-sulfonamide derivatives on human carbonic anhydrase isozymes. |
| AID1563833 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis. |
| AID758950 | Inhibition of Methanosarcina thermophila recombinant gamma-CA by CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14 | A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules. |
| AID1752202 | Inhibition of recombinant human carbonic anhydrase 5A by stopped-flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors. |
| AID307887 | Inhibition of human CA2 by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID1185163 | Inhibition of Vibrio cholerae cytosolic carbonic anhydrase by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae. |
| AID1375667 | Inhibition of recombinant human carbonic anhydrase-2 incubated for 15 mins by stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis. |
| AID539002 | Inhibition of Aspergillus fumigatus ChiA1 expressed in Pichia pastoris after 70 mins | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Acetazolamide-based fungal chitinase inhibitors. |
| AID1731024 | Inhibition of human CAH5B expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1339402 | Inhibition of recombinant human carbonic anhydrase 4 assessed as reduction in CO2 hydration preincubated for 15 mins by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties. |
| AID172512 | Renal excretion of bicarbonate after administration of 10 mg/kg in rats. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID1375669 | Inhibition of recombinant human carbonic anhydrase-9 catalytic domain incubated for 15 mins by stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis. |
| AID1678135 | Inhibition of recombinant human CA4 expressed in Escherichia coli BL21 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Structural Basis of Nanomolar Inhibition of Tumor-Associated Carbonic Anhydrase IX: X-Ray Crystallographic and Inhibition Study of Lipophilic Inhibitors with Acetazolamide Backbone. |
| AID646248 | Inhibition of human recombinant carbonic anhydrase 3 phosphatase activity using 4-nitrophenyl phosphate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID1520069 | Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1061894 | Inhibition of human carbonic anhydrase 1 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Inhibition of carbonic anhydrases from the extremophilic bacteria Sulfurihydrogenibium yellostonense (SspCA) and S. azorense (SazCA) with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophe |
| AID1287519 | Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13. |
| AID1358716 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 4 to Ki for recombinant human carbonic anhydrase 9 | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID113959 | Anticonvulsant activity following p.o. administration by standard maximal electroshock test in mice. | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Anticonvulsant O-alkyl sulfamates. 2,3:4,5-Bis-O-(1-methylethylidene)-beta-D-fructopyranose sulfamate and related compounds. |
| AID1504706 | Inhibition of Malassezia globosa beta-carbonic anhydrase incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study. |
| AID256964 | Inhibitory activity against human recombinant mitochondrial isozyme CA VA | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors. |
| AID1125518 | Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 | Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII. |
| AID1731025 | Inhibition of human CAH6 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1185165 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for Vibrio cholerae cytosolic carbonic anhydrase | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae. |
| AID382976 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.2 M hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID243098 | Ratio of inhibitory activity of human cytosolic carbonic anhydrase II to tumor associated carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates. |
| AID475902 | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow carbon dioxide hydrase assay method | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides. |
| AID496925 | Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1238809 | Selectivity ratio of Ki for human recombinant CA2 to Ki for human recombinant CA9 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID17874 | Evaluated for first order rate constant (Kin) for transcorneal penetration in anesthetized rabbits | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors. |
| AID299552 | Inhibition of Methanosarcina thermophila gamma CA | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID321163 | Selectivity for human CA12 over human CA2 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID1564421 | Inhibition of recombinant human CA1 at 10'-5 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1878299 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides. |
| AID1537868 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 expressed in Escherichia coli BL21 (DE3) to Ki for recombinant human carbonic anhydrase 9 expressed in Escherichia coli GOLD BL21 (DE3) | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID371555 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID598725 | Inhibition of recombinant Mycobacterium tuberculosis Rv1284 carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay at pH 7.5 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID1686869 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 1 to Ki for Ki for inhibition of recombinant human carbonic anhydrase 2 | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID271175 | Selectivity for human recombinant carbonic anhydrase 9 over carbonic anhydrase 2 | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
| AID1322632 | Inhibition of human carbonic anhydrase 12 pre-incubated for 15 mins by stopped flow carbon dioxide hydrase assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure Lowering Investigations. |
| AID552783 | Inhibition of Methanothermobacter thermautotrophicus carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Inhibition of the β-carbonic anhydrase from Streptococcus pneumoniae by inorganic anions and small molecules: Toward innovative drug design of antiinfectives? |
| AID762172 | Inhibition of cytosolic carbonic anhydrase 1 (unknown origin) preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design and synthesis of novel 4-(4-oxo-2-arylthiazolidin-3-yl)benzenesulfonamides as selective inhibitors of carbonic anhydrase IX over I and II with potential anticancer activity. |
| AID1336559 | Inhibition of Porphyromonas gingivalis recombinant carbonic anhydrase gamma assessed as inhibition of CO2 hydration preincubated for 15 mins by Lineweaver-burk plot method | |||
| AID316070 | Inhibition of mouse recombinant full length carbonic hydrase 13 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1446120 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 300 uM after 72 hrs under hypoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1354956 | Inhibition of human carbonic anhydrase 5A after 15 mins by stopped flow carbon dioxide hydration assay | 2018 | ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5 | Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology. |
| AID484216 | Selectivity ratio of Ki for human carbonic anhydrase 9 to human carbonic anhydrase 2 | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors. |
| AID725594 | Inhibition of human CA2 by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors. |
| AID93580 | Level in red blood cells after incubation of human erythrocytes for 30 min, was determined by ES method | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID305487 | Inhibition of human recombinant CA5A by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions. |
| AID386506 | Selectivity for human CA12 over human CA2 | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID598732 | Inhibition of Salmonella Typhimurium carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay at pH 8.3 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID726232 | Inhibition of Trypanosoma cruzi CL Brener recombinant alpha-carbonic anhydrase expressed in insect Sf9 cell Baculovirus system by stopped flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4 | Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease. |
| AID770583 | Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. |
| AID757583 | Inhibition of carbonic anhydrase 9 mRNA expression in human U87MG cells under hypoxic conditions at 5000 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by RT-PCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID50353 | Inhibitory activity against Human carbonic anhydrase I | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties. |
| AID496923 | Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID342482 | Inhibition of human carbonic anhydrase 7 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID598726 | Inhibition of recombinant human carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay at pH 8.3 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID437750 | Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID1070020 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Anion inhibition studies of two new β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID299246 | Inhibition of human carbonic anhydrase 5B by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID305488 | Inhibition of full length human recombinant full length CA6 expressed in Escherichia coli BL21 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions. |
| AID316060 | Inhibition of human recombinant full length carbonic hydrase 1 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1757212 | Inhibition of human CA9 by stopped- flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID475174 | inhibition of Cryptococcus neoformans recombinant Can2 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | Carbonic anhydrase inhibitors. The beta-carbonic anhydrases from the fungal pathogens Cryptococcus neoformans and Candida albicans are strongly inhibited by substituted-phenyl-1H-indole-5-sulfonamides. |
| AID733596 | Inhibition of human recombinant carbonic anhydrase-9-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | o-Benzenedisulfonimido-sulfonamides are potent inhibitors of the tumor-associated carbonic anhydrase isoforms CA IX and CA XII. |
| AID730371 | Inhibition of Cryptococcus neoformans beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Kinetic and anion inhibition studies of a β-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis. |
| AID679485 | TP_TRANSPORTER: uptake in Xenopus laevis oocytes | 2000 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1 | Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1. |
| AID1335044 | Inhibition of Malassezia globosa beta-carbonic anhydrase preincubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Dithiocarbamates effectively inhibit the β-carbonic anhydrase from the dandruff-producing fungus Malassezia globosa. |
| AID382960 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.1132 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1072625 | Selectivity ratio of Ki for human cytosolic carbonic anhydrase 2 to Ki for human transmembrane carbonic anhydrase 12 | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID1058389 | Inhibition of Clostridium perfringens carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID415832 | Selectivity ratio of Ki for human CA1 to Ki for human recombinant CA9 | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors. |
| AID1519761 | Inhibition of recombinant human carbonic anhydrase-9 at 0.1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID382973 | Solubility in water in presence of 0.2335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID436749 | Inhibition of human recombinant full length mitochondrial carbonic anhydrase 5B by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
| AID50177 | In vitro inhibition of carbonic anhydrase was determined using enzyme prepared from mouse erythrocytes | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides. |
| AID1238450 | Inhibition of human carbonic anhydrase-12 incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID757569 | Inhibition of carbonic anhydrase 9 protein expression in human GaMG cells under hypoxic conditions treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID780322 | Inhibition of human carbonic anhydrase9 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID1336991 | Selectivity ratio of Ki for human erythrocyte cytosolic carbonic anhydrase 2 to Ki for human membrane bound carbonic anhydrase 9 | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID320308 | Inhibition of human recombinant full length carbonic hydrase 4 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID349608 | Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 3 expressed in Escherichia coli BL21 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. |
| AID1717281 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Sulfonamide/sulfamate switch with a series of piperazinylureido derivatives: Synthesis, kinetic and in silico evaluation as carbonic anhydrase isoforms I, II, IV, and IX inhibitors. |
| AID300807 | Inhibition of cloned catalytic domani of human carbonic anhydrase 11 by CO2 hydration stopped-flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I and II, and extracellular isoforms IV, IX, and XII with sulfamides incorporating sugar moieties. |
| AID342471 | Inhibition of AQP4 in wild type mouse brain gilial cells assessed as reduction of osmotic equilibrium rate at 10 to 100 uM after 15 mins by calcein quenching assay relative to water permeability | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID238768 | Inhibitory activity against Carbonic anhydrase II | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties. |
| AID271713 | Selectivity for human CA9 over CA1 | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". |
| AID1692371 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID1821397 | Inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes. |
| AID1453368 | Inhibition of carbonic anhydrase-1 in human erythrocyte membranes assessed as reduction in H+ release using CO2 as substrate by bromine thymol blue indicator based assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives. |
| AID1809107 | Selectivity ratio of IC50 for recombinant human carbonic anhydrase 9 using 4-nitrophenylacetate as substrate to IC50 for recombinant human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis. |
| AID258730 | Inhibitory activity against cloned human CA2 | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib. |
| AID328978 | Inhibition of human full length carbonic anhydrase 5A | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID382969 | Solubility in water in presence of 0.2 M hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID588192 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 1 to Ki for Candida albicans recombinant Nce103 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1564420 | Inhibition of recombinant human CA1 at 10'-6 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1771797 | Inhibition of recombinant human CA9 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action. |
| AID1142835 | Inhibition of Cryptococcus neoformans Can2 assessed as CO2 hydrase activity by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11 | Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID281086 | Selectivity ratio of human CA9 over human CA2 | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
| AID1076061 | Inhibition of human recombinant carbonic anhydrase 2-mediated CO2 hydration after 6 hrs by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | 6-Triazolyl-substituted sulfocoumarins are potent, selective inhibitors of the tumor-associated carbonic anhydrases IX and XII. |
| AID475904 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for Brucella suis recombinant (6X)His tagged-beta carbonic anhydrase | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides. |
| AID314832 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 10 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1707347 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors. |
| AID459696 | Inhibition of Brucella suis CA1 expressed in Escherichia coli BL21(DE3) by stopped-flow CO2-hydration assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis. |
| AID1731019 | Inhibition of human CAH1 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1723509 | Inhibition of carbonic anhydrase in Enterococcus faecium ATCC 700221 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of ambient air by CLSI protocol based broth microdilution assay | |||
| AID1460770 | Inhibition of human CA6 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1453409 | Inhibition of Burkholderia pseudomallei beta-carbonic anhydrase | |||
| AID1188134 | Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID1275561 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 12 | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1543085 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins by stopped flow CO2 hydrase assay | |||
| AID1688236 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs under normaxia condition by MTT assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID607497 | Inhibition of Dicentrarchus labrax CA using 4-nitrophenylacetate substrate by esterase assay | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | In vitro inhibition of α-carbonic anhydrase isozymes by some phenolic compounds. |
| AID1242665 | Selectivity index, ratio of Ki for full length human carbonic anhydrase-2 to Ki for human recombinant carbonic anhydrase-9 catalytic domain | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. |
| AID614109 | Inhibition of human cloned full length carbonic anhydrase 14 preincubated for 15 mins by stopped flow CO2 hydration assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Carbonic anhydrase inhibitors. Synthesis, molecular structures, and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with novel 3-pyridinesulfonamide derivatives. |
| AID317582 | Selectivity for human CA9 over human CA1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. |
| AID1652405 | Inhibition of human CA7 pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID367655 | Inhibition of human secreted carbonic anhydrase 4 measured by CO2 hydration reaction assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Carbonic anhydrase inhibitors: inhibition studies of a coral secretory isoform with inorganic anions. |
| AID437753 | Activity at full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID599955 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 7 | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors. |
| AID1585353 | Inhibition of recombinant human carbonic anhydrase 12 by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID1821399 | Selectivity index, ratio of Ki for inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assa | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes. |
| AID342477 | Inhibition of human carbonic anhydrase 3 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1518924 | Inhibition of recombinant human carbonic anhydrase 2 assessed as residual activity at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1422971 | Inhibition of recombinant human CA12 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1918141 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 10 mins and measured by phenol red based stopped-flow CO2 hydration assay | |||
| AID48107 | Ex Vivo evaluation for the ability to penetrate the rabbit eye and inhibit carbonic anhydrase in a homogenate of the iris ciliary body | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides. |
| AID1565737 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration at 10'-8 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID264313 | Selectivity for human CA9 over CA1 | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
| AID314808 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.25 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1686865 | Inhibition of recombinant human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID314807 | Inhibition of human carbonic anhydrase 2 in presence of 0.25 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID770586 | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. |
| AID1194927 | Inhibition of human recombinant carbonic anhydrase 9 expressed in Escherichia coli pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of a new series of dithiocarbamates with effective human carbonic anhydrase inhibitory activity and antiglaucoma action. |
| AID1633349 | Inhibition of Malassezia globosa carbonic anhydrase preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1692373 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID1691507 | Selectivity ratio of Ki for inhibition of recombinant human CA1 to Ki for inhibition of recombinant human CA12 | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID314830 | Inhibition of human carbonic anhydrase 9 in presence of 1.00 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID47936 | Inhibition of human carbonic anhydrase II | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides. |
| AID257064 | Inhibition of recombinant human mitochondrial isozyme CA VA | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID1520084 | Binding affinity to recombinant human carbonic anhydrase 5b expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1873565 | Inhibition of human carbonic anhydrase 9 by stopped flow CO2 assay | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors. |
| AID320307 | Inhibition of human recombinant full length carbonic hydrase 3 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID47904 | Inhibitory activity against human cloned isoenzyme carbonic anhydrase II (hCA II), by esterase method. | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives. |
| AID603452 | Selectivity ratio of Ki for human full length cytosolic isoform of carbonic anhydrase 1 to Ki for human recombinant catalytic domain of carbonic anhydrase 9 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID386499 | Inhibition of human cloned CA2 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID331500 | Inhibition of human cloned carbonic anhydrase 9 by CO2 hydration stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes. |
| AID311025 | Inhibition of human carbonic anhydrase 3 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1188136 | Inhibition of Helicobacter pylori Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID295293 | Inhibition of human recombinant CA7 after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID757581 | Inhibition of carbonic anhydrase 9 mRNA expression in human U373 cells under hypoxic conditions at 4500 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by RT-PCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1183267 | Inhibition of human cloned CA9 catalytic domain pre-incubated with enzyme for 15 mins by phenol red based CO2 hydration stopped-flow assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis of a new series of N⁴-substituted 4-(2-aminoethyl)benzenesulfonamides and their inhibitory effect on human carbonic anhydrase cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII. |
| AID1419425 | Cytotoxicity against human HT-29 cells assessed as cell viability at 200 uM after 48 hrs under hypoxic conditions by MTT assay (Rvb = 100%) | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID588195 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 2 to Ki for Mycobacterium tuberculosis recombinant Rv1284 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID299227 | Activity of human CA5A at pH 7.5 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1070021 | Inhibition of Legionella pneumophila carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Anion inhibition studies of two new β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID314818 | Inhibition of human carbonic anhydrase 9 in presence of 0.01 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1354958 | Inhibition of human carbonic anhydrase 7 after 15 mins by stopped flow carbon dioxide hydration assay | 2018 | ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5 | Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology. |
| AID1759811 | Inhibition of Vibrio cholerae beta carbonic anhydrase preincubated with enzyme for 15 mins by phenol red-based stopped-flow CO2 hydration assay | |||
| AID764564 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | 5-Substituted-(1,2,3-triazol-4-yl)thiophene-2-sulfonamides strongly inhibit human carbonic anhydrases I, II, IX and XII: solution and X-ray crystallographic studies. |
| AID1518938 | Inhibition of recombinant human carbonic anhydrase 12 at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID620692 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 12 catalytic domain | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID371704 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 by by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273. |
| AID427125 | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID281084 | Inhibition of catalytic domain of human recombinant isozyme CA9 by CO2 hydration method | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. |
| AID1077017 | Inhibition of human carbonic anhydrase 9-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID261579 | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. |
| AID1517569 | Inhibition of human carbonic anhydrase 12 at 10'-8 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID382945 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.0755 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1076062 | Inhibition of human recombinant carbonic anhydrase 1-mediated CO2 hydration after 6 hrs by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | 6-Triazolyl-substituted sulfocoumarins are potent, selective inhibitors of the tumor-associated carbonic anhydrases IX and XII. |
| AID321159 | Inhibition of human recombinant CA12 by CO2 hydration stopped flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID1245671 | Inhibition of carbonic anhydrase-4 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1519747 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase-1 to Ki for recombinant human carbonic anhydrase-9 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID316068 | Inhibition of human catalytic domain carbonic hydrase 9 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1419399 | Inhibition of carbonic anhydrase 12 (unknown origin) preincubated for 15 mins by stopped flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID1060765 | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors. |
| AID1689402 | Inhibition of recombinant human carbonic anhydrase 12 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1308824 | Inhibition of human recombinant carbonic anhydrase 4 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID258733 | Inhibitory activity against cloned human CA12 | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib. |
| AID1504978 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases. |
| AID1756999 | Downregulation of carbonic anhydrase in human NCI-H1975 cells at 2 uM incubated for 24 hrs in hypoxic condition by Western blot analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
| AID299538 | Inhibition of human CA1 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
| AID1188142 | Inhibition of Legionella pneumophilia Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID1466467 | Inhibition of recombinant human carbonic anhydrase-12 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII. |
| AID1462737 | Inhibition of human CA12 pre-incubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Synthesis and carbonic anhydrase inhibition of polycyclic imides incorporating N-benzenesulfonamide moieties. |
| AID1175496 | Inhibition of human recombinant carbonic anhydrase 3 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID724718 | Inhibition of human recombinant CA11 mutant after 15 mins by stopped-flow CO2 hydration method | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Restoring catalytic activity to the human carbonic anhydrase (CA) related proteins VIII, X and XI affords isoforms with high catalytic efficiency and susceptibility to anion inhibition. |
| AID761443 | Inhibition of human recombinant CA9 using 4-nitrophenylacetate as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Sulfonamides containing coumarin moieties selectively and potently inhibit carbonic anhydrases II and IX: design, synthesis, inhibitory activity and 3D-QSAR analysis. |
| AID1273035 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1585357 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 12 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID612727 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 at pH 8.3 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID1379914 | Inhibition of recombinant human carbonic anhydrase 9 catalytic domain preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Discovery of New Selenoureido Analogues of 4-(4-Fluorophenylureido)benzenesulfonamide as Carbonic Anhydrase Inhibitors. |
| AID382974 | Solubility in water in presence of 0.3360 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1655935 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer. |
| AID1678133 | Inhibition of recombinant human CA1 expressed in Escherichia coli BL21 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Structural Basis of Nanomolar Inhibition of Tumor-Associated Carbonic Anhydrase IX: X-Ray Crystallographic and Inhibition Study of Lipophilic Inhibitors with Acetazolamide Backbone. |
| AID1736571 | Selectivity index, ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 12 | |||
| AID50380 | Inhibitory activity against human carbonic anhydrase I. | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates. |
| AID1461933 | Inhibition of human CA1 incubated for 15 mins by stopped-flow CO2 hydration assay | |||
| AID441211 | Selectivity for human cloned CA9 over human cloned CA2 | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID729570 | Inhibition of Drosophila melanogaster recombinant carbonic anhydrase-1 expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Characterization, bioinformatic analysis and dithiocarbamate inhibition studies of two new α-carbonic anhydrases, CAH1 and CAH2, from the fruit fly Drosophila melanogaster. |
| AID1354957 | Inhibition of human carbonic anhydrase 5B after 15 mins by stopped flow carbon dioxide hydration assay | 2018 | ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5 | Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology. |
| AID166654 | Tested in vitro for transcorneal accession rates (corneal permeability) against intact cornea | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID1723508 | Inhibition of carbonic anhydrase in Enterococcus faecalis HM-334 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of ambient air by CLSI protocol based broth microdilution assay | |||
| AID321156 | Inhibition of human recombinant CA1 by CO2 hydration stopped flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID1277139 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 9 | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID1771795 | Inhibition of recombinant human CA4 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action. |
| AID371705 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273. |
| AID1426789 | Inhibition of recombinant human CA9 catalytic domain preincubated for 15 mins by stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis. |
| AID1692247 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII. |
| AID1175500 | Inhibition of human recombinant carbonic anhydrase 7 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1193926 | Inhibition of human recombinant CA-2 after 15 mins by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID1204094 | Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-1 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-12 | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1818556 | Inhibition of human CA2 incubated for 15 mins prior to testing by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | 2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity. |
| AID1291360 | Inhibition of recombinant Sulfurihydrogenibium azorense alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1474384 | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability at 100 uM after 72 hrs under normoxic condition by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. |
| AID414959 | Inhibition of human mitochondrial carbonic anhydrase 5B by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID437751 | Activity at human recombinant CA1 by stopped-flow hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID1373181 | Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5B (40 to 317 residues) expressed in Escherichia coli Rosetta 2 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent t | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1312157 | Inhibition of Malassezia globosa beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID239287 | Mean inhibitory constant towards human carbonic anhydrase V determined by spectrophotometric dansylamide binding assay | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. |
| AID601816 | Inhibition of human carbonic anhydrase 14 preincubated with compound for 15 mins by carbon dioxide hydration assay | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV. |
| AID1518947 | Inhibition of recombinant human carbonic anhydrase 2 at 1 nM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID411532 | Inhibition of human recombinant CA5B by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411532 | Inhibition of human recombinant CA5B by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1771794 | Inhibition of recombinant human CA2 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action. |
| AID1235241 | Inhibition of human CA2 after 15 mins by stopped-flow/Co2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Cloning, characterization and anion inhibition studies of a new γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1405950 | Inhibition of human recombinant carbonic anhydrase 2 assessed as CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye-based stopped-flow assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal. |
| AID437835 | Inhibition of human full length cytosolic carbonic anhydrase 3 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1301274 | Inhibition of human carbonic anhydrase 9 using saturated CO2 as substrate incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1423030 | Inhibition of human CA9 by Lineweaver-Burk plot analysis | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides. |
| AID1449744 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Synthesis and carbonic anhydrase inhibition of a series of SLC-0111 analogs. |
| AID487851 | Inhibition of esterase activity of human carbonic anhydrase 1 by Lineweaver-Burke plot analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | A novel and one-pot synthesis of new 1-tosyl pyrrol-2-one derivatives and analysis of carbonic anhydrase inhibitory potencies. |
| AID644035 | Inhibition of human carbonic anhydrase 2 esterase activity using 4-nitrophenylacetate as substrate | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives. |
| AID587002 | Inhibition of tumor-associated human carbonic anhydrase 12 preincubated for 15 min by CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis. |
| AID1849601 | Inhibition of human CA9 using 4-nitrophenylacetate as substrate incubated for 10 mins prior to testing by spectrophotometry based esterase assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID238986 | Inhibitory activity against human carbonic anhydrase II at 0.01 uM | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID1626025 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma. |
| AID761310 | Inhibition of human transmembrane carbonic anhydrase 9 after 6 hrs by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | 7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors. |
| AID1649851 | Inhibition of human CA2 preincubated for 15 mins by stopped-flow carbon dioxide hydration assay | |||
| AID1808984 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID1849534 | Binding affinity to human CA2 assessed as inhibition constant by SDS-PAGE analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1306523 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1873667 | Inhibition of recombinant human carbonic anhydrase 12 assessed as inhibition constant incubated for 1 hr prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry, 08-01, Volume: 67 | Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation. |
| AID1354955 | Inhibition of human carbonic anhydrase 2 after 15 mins by stopped flow carbon dioxide hydration assay | 2018 | ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5 | Design, Synthesis, and X-ray of Selenides as New Class of Agents for Prevention of Diabetic Cerebrovascular Pathology. |
| AID347428 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. |
| AID1423031 | Inhibition of human CA12 by Lineweaver-Burk plot analysis | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides. |
| AID1766625 | Inhibition of recombinant human CA12 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Discovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations. |
| AID26762 | Partition coefficient (logD) (chloroform/buffer) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route. |
| AID1731043 | Inhibition of CAH9 in human T47D cells at 1 uM by membrane inlet for mass spectrometry | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1254028 | Inhibition of Trypanosoma cruzi alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID1878300 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides. |
| AID1277141 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 12 | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | 4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies. |
| AID612725 | Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID1166263 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel sulfonamides bearing pyrrole and pyrrolopyrimidine moieties as carbonic anhydrase inhibitors: Synthesis, cytotoxic activity and molecular modeling. |
| AID417837 | Inhibition of Caenorhabditis elegans CAH-4b by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1306527 | Inhibition of Flaveria bidentis carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID747806 | Inhibition of recombinant human CA12 transmembrane isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID436563 | Inhibition of human recombinant CA1 by stopped-flow CO2 assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. |
| AID1727537 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion. |
| AID1426790 | Inhibition of recombinant human CA12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis. |
| AID238774 | Binding affinity towards human cloned carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. |
| AID1188139 | Inhibition of Brucella suis Carbonic anhydrase (219 amino acids) compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID1570352 | Inhibition of recombinant human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Carbonic anhydrase inhibitors based on sorafenib scaffold: Design, synthesis, crystallographic investigation and effects on primary breast cancer cells. |
| AID1243123 | Inhibition of human carbonic anhydrase 12 at 10'-6 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1759813 | Inhibition of Burkholderia pseudomallei beta carbonic anhydrase preincubated with enzyme for 15 mins by phenol red-based stopped-flow CO2 hydration assay | |||
| AID331501 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for human cloned carbonic anhydrase 9 | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes. |
| AID551577 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Inhibition of β-carbonic anhydrases with ureido-substituted benzenesulfonamides. |
| AID1238804 | Inhibition of human recombinant CA1 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID365985 | Inhibition of human cloned CA7 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID261580 | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. |
| AID50350 | Inhibition of cloned human cytosolic isozyme Carbonic anhydrase I | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
| AID311029 | Inhibition of human carbonic anhydrase 6 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID299549 | Inhibition of human CA14 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID669121 | Antimicrobial activity against Malassezia dermatis CBS 9145 after 7 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1061031 | Inhibition of human CA14 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1518907 | Inhibition of recombinant human carbonic anhydrase 12 assessed as residual activity at 1 nM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1238452 | Selectivity ratio of Ki for human carbonic anhydrase-1 to Ki for human carbonic anhydrase-9 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID254242 | Inhibitory activity against human Carbonic anhydrase I (hCA I) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. |
| AID299244 | Inhibition of human carbonic anhydrase 3 by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID727278 | Inhibition of full length human recombinant CA2 cytosolic isoform after 6 hrs by stopped-flow CO2 hydration method | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases. |
| AID48310 | Inhibitory activity against murine carbonic anhydrase XIII (mCA XIII) by using CO2 hydrase assay method | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design. |
| AID620794 | Cytotoxicity against CA9-deficient chinese hamster PS120 cells assessed as cell viability at 100 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1310848 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | PEGylated Bis-Sulfonamide Carbonic Anhydrase Inhibitors Can Efficiently Control the Growth of Several Carbonic Anhydrase IX-Expressing Carcinomas. |
| AID48286 | Inhibitory activity against Carbonic anhydrase IV isolated from bovine lung | 2003 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17 | Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide. |
| AID462272 | Inhibition of human CA3 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID724720 | Inhibition of human recombinant CA8 mutant after 15 mins by stopped-flow CO2 hydration method | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Restoring catalytic activity to the human carbonic anhydrase (CA) related proteins VIII, X and XI affords isoforms with high catalytic efficiency and susceptibility to anion inhibition. |
| AID1666823 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID462278 | Inhibition of human CA9 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1306836 | Inhibition of human carbonic anhydrase 1 preincubated for 6 hrs at 4 degC measured for 10 to 100 secs by stopped-flow carbon dioxide hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1,6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors. |
| AID770582 | Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. |
| AID1358713 | Inhibition of recombinant human carbonic anhydrase 9 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID1581513 | Inhibition of recombinant human carbonic anhydrase 7 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID317580 | Inhibition of human cloned CA2 by CO2 hydration method | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID290101 | Inhibition of human AQP4b-mediated water transport in Xenopus oocytes | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5 | Identification of arylsulfonamides as Aquaporin 4 inhibitors. |
| AID1183561 | Inhibition of human recombinant carbonic anhydrase 9 by stopped flow CO2 hydration method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Cyclic tertiary sulfamates: selective inhibition of the tumor-associated carbonic anhydrases IX and XII by N- and O-substituted acesulfame derivatives. |
| AID1555965 | Inhibition of human carbonic anhydrase 5B incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID764566 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | 5-Substituted-(1,2,3-triazol-4-yl)thiophene-2-sulfonamides strongly inhibit human carbonic anhydrases I, II, IX and XII: solution and X-ray crystallographic studies. |
| AID1193677 | Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Synthesis of 6-aryl-substituted sulfocoumarins and investigation of their carbonic anhydrase inhibitory action. |
| AID734185 | Inhibition of recombinant human carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship. |
| AID1243110 | Inhibition of human carbonic anhydrase 1 at 10'-7 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID764567 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | 5-Substituted-(1,2,3-triazol-4-yl)thiophene-2-sulfonamides strongly inhibit human carbonic anhydrases I, II, IX and XII: solution and X-ray crystallographic studies. |
| AID417834 | Inhibition of human recombinant CA12 catalytic domain by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID496924 | Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID493889 | Inhibition of human recombinant carbonic anhydrase 6 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID616472 | Inhibition of human carbonic anhydrase 5B preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID620795 | Cytotoxicity against CA9 expressing chinese hamster PS120 cells assessed as cell viability at 100 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1605088 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action. |
| AID1427076 | Inhibition of human recombinant carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies. |
| AID339671 | Inhibition of human recombinant carbonic anhydrase 4 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1275626 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms. |
| AID1520070 | Binding affinity to recombinant human carbonic anhydrase 4 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1520083 | Binding affinity to recombinant human carbonic anhydrase 5a expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1170169 | Inhibition of human carbonic anhydrase 5B at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID331292 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols. |
| AID1504047 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Lucky Switcheroo: Dramatic Potency and Selectivity Improvement of Imidazoline Inhibitors of Human Carbonic Anhydrase VII. |
| AID1754557 | Inhibition of recombinant human CA2 preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity. |
| AID1520067 | Binding affinity to recombinant human carbonic anhydrase 1 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID752641 | Antifungal activity against wild type Saccharomyces cerevisiae BY4742 assessed as growth inhibition after 48 hrs by microplate spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Carbonic anhydrase inhibitors. Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase. |
| AID732709 | Binding affinity to human recombinant CA13 at 37 degC and pH 7.0 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | 4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII. |
| AID1175502 | Inhibition of human recombinant carbonic anhydrase 12 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1564595 | Inhibition of recombinant human carbonic anhydrase 7 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity. |
| AID1308830 | Inhibition of human recombinant carbonic anhydrase 13 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID1655390 | Inhibition of recombinant human carbonic anhydrase 4 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID342472 | Inhibition of AQP4 in mouse erythrocytes assessed as inhibition of osmotic water permeability at 100 uM after 15 mins by stopped-flow light scattering method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID1278407 | Inhibition of Coleofasciculus chthonoplastes beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID1733132 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 10 mins by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 39 | Synthesis and biological evaluation of novel 4,7-disubstituted coumarins as selective tumor-associated carbonic anhydrase IX and XII inhibitors. |
| AID616471 | Inhibition of human carbonic anhydrase 5A preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID314793 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 1.00 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1560583 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID239223 | Inhibitory potency against human cloned Carbonic anhydrase I expressed in Escherichia coli strain BL21 | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX. |
| AID331293 | Inhibition of mouse recombinant carbonic anhydrase 15 by stopped-flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols. |
| AID1688230 | Inhibition of recombinant human carbonic anhydrase 1 measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID1234858 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | 5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII. |
| AID166755 | Variation of intraocular pressure in fourth day at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID93584 | Level in red blood cells after incubation of human erythrocytes for 60 min, was determined by HPLC method | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1235244 | Inhibition of Nostoc commune CA after 15 mins by stopped-flow/Co2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Cloning, characterization and anion inhibition studies of a new γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID724722 | Inhibition of human recombinant wild type CA1 by stopped-flow CO2 hydration method | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Restoring catalytic activity to the human carbonic anhydrase (CA) related proteins VIII, X and XI affords isoforms with high catalytic efficiency and susceptibility to anion inhibition. |
| AID1449745 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Synthesis and carbonic anhydrase inhibition of a series of SLC-0111 analogs. |
| AID1133343 | Inhibition of carbonic anhydrase (unknown origin) preincubated with enzyme for 10 mins prior to substrate addition by colorimetric method | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides. |
| AID1808981 | Inhibition of human carbonic anhydrase 5A by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID300805 | Inhibition of human truncated recombinant carbonic anhydrase 4 by CO2 hydration stopped-flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I and II, and extracellular isoforms IV, IX, and XII with sulfamides incorporating sugar moieties. |
| AID1597786 | Inhibition of human recombinant N-HA--tagged carbonic anhydrase 12 expressed in HEK293T cells using p-nitrophenyl acetate as substrate measured after 30 mins by colorimetric analysis | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17 | Sulfonate and sulfamate derivatives possessing benzofuran or benzothiophene nucleus as potent carbonic anhydrase II/IX/XII inhibitors. |
| AID1470977 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | Synthesis of new 3-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-benzenesulfonamides with strong inhibition properties against the tumor associated carbonic anhydrases IX and XII. |
| AID388109 | Cytotoxicity against human KB cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Carbonic anhydrase inhibitors: inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides-in vitro and in vivo studies. |
| AID1564431 | Inhibition of recombinant human CA12 at at 10'-8 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID464121 | Inhibition of human recombinant CA14 by stopped-flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies. |
| AID484159 | Inhibition of full length human carbonic anhydrase 5b preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID382972 | Solubility in water in presence of 0.1668 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID552785 | Inhibition of Streptococcus pneumoniae beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Inhibition of the β-carbonic anhydrase from Streptococcus pneumoniae by inorganic anions and small molecules: Toward innovative drug design of antiinfectives? |
| AID328983 | Inhibition of human catalytic domain carbonic anhydrase 12 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID757582 | Inhibition of carbonic anhydrase 9 mRNA expression in human U251 cells under hypoxic conditions at 4500 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by RT-PCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID50364 | Inhibition of human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. |
| AID1511293 | Inhibition of human carbonic anhydrase 4 assessed as reduction in CO2 hydration preincubated for 15 mins to 2 hrs by phenol red dye based stopped flow CO2 hydrase assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID50375 | Inhibitory activity against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered. |
| AID1849575 | Inhibition of human recombinant CA1 incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID770584 | Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. |
| AID195093 | Inhibitor level was measured in red blood cells at 60 min after exposure of 10 mL of blood to solutions by electronic spectroscopic (ES) method | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID1379906 | Inhibition of recombinant human carbonic anhydrase 12 catalytic domain preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. |
| AID238635 | Inhibitory activity against cytosolic human carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates. |
| AID603450 | Inhibition of human recombinant catalytic domain of carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID587128 | Inhibition of Struthio camelus carbonic anhydrase after 15 mins by Lineweaver-Burk plot | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID648181 | Inhibition of human wild type carbonic anhydrase 2 Leu204Ser mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors. |
| AID427128 | Inhibition of human carbonic anhydrase 5A by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID1564385 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitors. |
| AID646242 | Inhibition of human recombinant carbonic anhydrase 7 C183S/C217S mutant using carbon-dioxide as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID762169 | Selectivity ratio of Ki for cytosolic carbonic anhydrase 1 (unknown origin) to Ki for carbonic anhydrase 9 (unknown origin) | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design and synthesis of novel 4-(4-oxo-2-arylthiazolidin-3-yl)benzenesulfonamides as selective inhibitors of carbonic anhydrase IX over I and II with potential anticancer activity. |
| AID1126610 | Inhibition of bovine erythrocyte carbonic anhydrase 2 using p-nitrophenyl acetate as substrate preincubated for 10 mins before substrate addition measured after 30 mins by spectrophotometric analysis | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | New aminobenzenesulfonamide-thiourea conjugates: synthesis and carbonic anhydrase inhibition and docking studies. |
| AID1564433 | Inhibition of recombinant human CA12 at at 10'-6 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1348312 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases. |
| AID409951 | Inhibition of human liver MAOB | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1268963 | Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA. |
| AID1754561 | Selectivity ratio, ratio of Ki of recombinant human CA2 to Ki of recombinant human CA9 | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity. |
| AID367820 | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates. |
| AID1754558 | Inhibition of recombinant human CA4 preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity. |
| AID611567 | Inhibition of bovine carbonic anhydrase assessed as formation of p-nitrophenol from p-nitrophenyl acetate substrate at 0.5 mM after 30 mins by spectrophotometric method | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Discovery of new chromone containing sulfonamides as potent inhibitors of bovine cytosolic carbonic anhydrase. |
| AID436565 | Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. |
| AID275813 | Inhibition of human mitochondrail isozyme CA VB | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID512002 | Inhibition of human cloned CA2 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID512002 | Inhibition of human cloned CA2 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1422975 | Inhibition of recombinant Helicobacter pylori beta carbonic anhydrase preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID327768 | Inhibition of mouse full length carbonic anhydrase 13 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1334830 | Inhibition of human recombinant carbonic anhydrase-12 preincubated for 6 hrs by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity. |
| AID1140119 | Inhibition of human carbonic anhydrase 1-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity. |
| AID408469 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1237874 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 2 to Ki for Brucella suis beta-carbonic anhydrase 2 | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1061040 | Inhibition of human CA2 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1254031 | Inhibition of Porphyromonas gingivalis beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID301577 | Inhibition of human recombinant CA 2 assessed as CO2 hydration by stopped flow kinetic assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID1076532 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Design, synthesis and evaluation of N-substituted saccharin derivatives as selective inhibitors of tumor-associated carbonic anhydrase XII. |
| AID1726079 | Inhibition of Vibrio cholerae beta carbonic anhydrase pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in |
| AID1752204 | Inhibition of recombinant human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors. |
| AID258731 | Inhibitory activity against CA4 isolated from bovine lung microsomes | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib. |
| AID1170185 | Inhibition of human carbonic anhydrase 1 at pH7 and 25 degC by stopped-flow kinetic inhibition assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID424444 | Inhibition of Cryptococcus neoformans recombinant Carbonic anhydrase 2 pre-incubated for 15 mins by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. |
| AID1237480 | Inhibition of Saccharomyces cerevisiae carbonic anhydrase by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID1275625 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms. |
| AID1408649 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity. |
| AID48288 | Inhibition of bovine carbonic anhydrase IV (CA4) from bovine lung microsomes | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1133325 | Octanol-water partition coefficient, log P of the compound | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides. |
| AID1170173 | Inhibition of chimeric carbonic anhydrase 9 (unknown origin) expressing with full length CA2 (1 to 260) at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1358711 | Inhibition of recombinant human carbonic anhydrase 1 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID1243116 | Inhibition of human carbonic anhydrase 9 at 10'-9 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID417828 | Inhibition of human recombinant full length CA4 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1419397 | Inhibition of carbonic anhydrase 2 (unknown origin) preincubated for 15 mins by stopped flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID1446110 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 100 uM after 48 hrs under normoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1652401 | Inhibition of human CA1 pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID1726060 | Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID438005 | Inhibition of human full length mitochondrial carbonic anhydrase 5B after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1442646 | Inhibition of recombinant human carbonic anhydrase 7 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID1731042 | Inhibition of CAH2 in human T47D cells at 1 uM by membrane inlet for mass spectrometry | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID327758 | Inhibition of human full length carbonic anhydrase 1 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1308829 | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID1519754 | Inhibition of recombinant human carbonic anhydrase-1 at 10 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1565730 | Inhibition of human carbonic anhydrase 9 assessed as inhibitory constant incubated for 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID314762 | Inhibition of human carbonic anhydrase 2 in presence of 0.01 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1726082 | Inhibition of human CA1 pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in |
| AID299232 | Activity of Helicobacter pylori beta CA at pH 8.3 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID644085 | Inhibition of human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID551580 | Inhibition of Mycobacterium tuberculosis recombinant beta-carbonic anhydrase Rv3273 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Inhibition of β-carbonic anhydrases with ureido-substituted benzenesulfonamides. |
| AID464122 | Selectivity ratio of Ki for human CA2 to Ki for human CA9 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies. |
| AID342484 | Inhibition of human carbonic anhydrase 12 catalytic domain by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID610535 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID50354 | Inhibitory activity against human recombinant carbonic anhydrase I (CA1) | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
| AID552128 | Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. |
| AID1556935 | Inhibition of human recombinant carbonic anhydrase 9 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID552781 | Inhibition of human carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Inhibition of the β-carbonic anhydrase from Streptococcus pneumoniae by inorganic anions and small molecules: Toward innovative drug design of antiinfectives? |
| AID1434427 | Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | |||
| AID50186 | Inhibition of Carbonic anhydrase enzyme in rabbits | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | Acetazolamide-like carbonic anhydrase inhibitors with topical ocular hypotensive activity. |
| AID1818306 | Inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID646246 | Inhibition of human recombinant carbonic anhydrase 7 C183S/C217S mutant hydrolysis activity using 4-nitrophenyl acetate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID1427075 | Inhibition of human recombinant carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies. |
| AID587126 | Inhibition of human carbonic anhydrase 3 after 15 mins by Lineweaver-Burk plot | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID353229 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties. |
| AID369272 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID25621 | Evaluated for sulfonamide pKa, free acid water solubility | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors. |
| AID26781 | Partition coefficient (logD) (chloroform/buffer) | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring? |
| AID347429 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. |
| AID1251960 | Inhibition of recombinant human carbonic anhydrase 12 catalytic domain expressed in Escherichia coli incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII. |
| AID1769575 | Inhibition of recombinant human CA2 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold. |
| AID1759809 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID50378 | Inhibitory activity against human carbonic anhydrase I (hCA I) | 2003 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17 | Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide. |
| AID1239226 | Inhibition of human recombinant carbonic anhydrase-1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties. |
| AID314768 | Inhibition of human carbonic anhydrase 2 in presence of 0.10 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1291097 | Selectivity ratio of Ki for recombinant Candida albicans beta carbonic anhydrase NCE103 to Ki for recombinant Candida glabrata beta carbonic anhydrase NCE103 expressed in Escherichia coli | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID620791 | Cytotoxicity against CA9 expressing chinese hamster PS120 cells assessed as cell viability at 30 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID263638 | Inhibition of Helicobacter pylori recombinant CA | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori. |
| AID1565740 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration at 10'-9 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID610543 | Inhibition of human recombinant carbonic anhydrase 6 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID222127 | Inhibition of cloned isozyme, human carbonic anhydrase IV | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Carbonic anhydrase inhibitors: synthesis of sulfonamides incorporating dtpa tails and of their zinc complexes with powerful topical antiglaucoma properties. |
| AID1706626 | Selectivity index, ratio of Ki for inhibition of human CA1 to Ki for inhibition of human CA9 | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID238912 | Inhibitory constant against cytosolic human Carbonic anhydrase I using CO2 hydrase assay | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. |
| AID441707 | Inhibition of human recombinant CA3 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID669122 | Antimicrobial activity against Malassezia pachydermatis CBS 6536 after 7 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1511295 | Inhibition of human carbonic anhydrase 12 assessed as reduction in CO2 hydration preincubated for 15 mins to 2 hrs by phenol red dye based stopped flow CO2 hydrase assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID727277 | Inhibition of human recombinant transmembrane CA9 catalytic domain after 6 hrs by stopped-flow CO2 hydration method | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases. |
| AID382954 | Solubility in water in presence of 0.1509 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1692094 | Inhibition of human erythrocyte CA1 using 4-nitrophenyl acetate as substrate by spectrophotometry | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate. |
| AID441208 | Inhibition of human cloned CA9 catalytic domain by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID669321 | Inhibition of human recombinant full length CA2-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, structure-activity relationship studies, and X-ray crystallographic analysis of arylsulfonamides as potent carbonic anhydrase inhibitors. |
| AID1262266 | Inhibition of weddell seal alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus. |
| AID1504975 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID414960 | Inhibition of Methanobacterium thermoautotrophicum carbonic anhydrase by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID1758424 | Selectivity index, ratio of Ki for inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assa | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides. |
| AID1556937 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 1 expressed in Escherichia coli to Ki for human recombinant carbonic anhydrase 9 expressed in Escherichia coli | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID1852043 | Inhibition of recombinant human CA9 pre-incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID367822 | Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates. |
| AID1240212 | Inhibition of Methanosarcina thermophila gamma carbonic anhydrase by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID587125 | Inhibition of human carbonic anhydrase 2 after 15 mins by Lineweaver-Burk plot | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID1140817 | Inhibition of human carbonic anhydrase 1-catalyzed CO2 hydration preincubated for 10 mins by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of human cytosolic isoforms I and II with (reduced) Schiff's bases incorporating sulfonamide, carboxylate and carboxymethyl moieties. |
| AID1170189 | Inhibition of human carbonic anhydrase 12 at pH7 and 25 degC by stopped-flow kinetic inhibition assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1564432 | Inhibition of recombinant human CA12 at at 10'-7 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID757572 | Inhibition of carbonic anhydrase 9 protein expression in human U87MG cells under hypoxic conditions treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1237479 | Inhibition of Candida albicans carbonic anhydrase by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID1339401 | Inhibition of recombinant human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties. |
| AID537654 | Inhibition of human carbonic anhydrase 1 hydratase activity by spectrophotometry | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide. |
| AID293813 | Inhibition of human recombinant CA9 by stopped flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties. |
| AID578224 | Inhibition of human recombinant CA5B mitochondrial isoform by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | (R)-/(S)-10-camphorsulfonyl-substituted aromatic/heterocyclic sulfonamides selectively inhibit mitochondrial over cytosolic carbonic anhydrases. |
| AID743513 | Inhibition of Helicobacter pylori recombinant alpha carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides. |
| AID1190065 | Inhibition of Plasmodium falciparum Eta-carbonic anhydrase pre-incubated for 15 mins before CO2 substrate addition by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum. |
| AID1240216 | Inhibition of Methanosarcina thermophila recombinant gamma carbonic anhydrase by stopped flow CO2 hydrase assay method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID244240 | Binding affinity ratio towards human cloned carbonic anhydrase II to that of human cloned carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1518922 | Inhibition of recombinant human carbonic anhydrase 1 at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID166975 | Tested for level of sulfonamide in red blood cells of albino rabbits at 120 min post-administration of 50 mg/kg sulfonamides | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
| AID1168851 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Structural insights on carbonic anhydrase inhibitory action, isoform selectivity, and potency of sulfonamides and coumarins incorporating arylsulfonylureido groups. |
| AID427124 | Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID1519744 | Inhibition of recombinant human carbonic anhydrase-2 incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1291362 | Inhibition of recombinant Porphyromonas gingivalis beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1142834 | Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11 | Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID408473 | Selectivity for human cloned CA9 over human recombinant CA1 | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1234499 | Inhibition of human carbonic anhydrase 1 by by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design and synthesis of benzothiazole-6-sulfonamides acting as highly potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID730370 | Inhibition of Candida albicans beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Kinetic and anion inhibition studies of a β-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis. |
| AID1154445 | Inhibition of human cloned cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Carbonic anhydrase inhibitors. Synthesis of a novel series of 5-substituted 2,4-dichlorobenzenesulfonamides and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII. |
| AID1631904 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and carbonic anhydrase inhibitory effects of new N-glycosylsulfonamides incorporating the phenol moiety. |
| AID730875 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | An α-carbonic anhydrase from the thermophilic bacterium Sulphurihydrogenibium azorense is the fastest enzyme known for the CO2 hydration reaction. |
| AID1751409 | Inhibition of human CA2 measured by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies. |
| AID474214 | Selectivity ratio of Ki for human recombinant CA2 to Ki for human recombinant CA12 | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID1336558 | Inhibition of Methanosarcina thermophila recombinant carbonic anhydrase gamma assessed as inhibition of CO2 hydration preincubated for 15 mins by Lineweaver-burk plot method | |||
| AID243090 | Ratio of inhibition of carbonic anhydrase IV in human to that of carbonic anhydrase IV in bovine | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. |
| AID697242 | Inhibition of human recombinant CA9 catalytic domain preincubated for 15 mins by stopped-flow CO2 hydration assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. |
| AID1357843 | Inhibition of human transmembrane tumor-associated carbonic anhydrase 9 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | 2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents. |
| AID474211 | Permeability by PAMPA | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID1241137 | Inhibition of human carbonic anhydrase-9 incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Exploring new Probenecid-based carbonic anhydrase inhibitors: Synthesis, biological evaluation and docking studies. |
| AID526864 | Binding affinity to human recombinant carbonic anhydrase 7 by isothermal titration calorimetry assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID1755846 | Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID1808977 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID48304 | Inhibitory activity against human carbonic anhydrase IX. | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates. |
| AID669120 | Antimicrobial activity against Malassezia furfur CBS 9569 after 7 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1766623 | Inhibition of recombinant human CA2 pre-incubated for 15 mins measured by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Discovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations. |
| AID1240217 | Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID484214 | Inhibition of human carbonic anhydrase 2 | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors. |
| AID749807 | Inhibition of human carbonic anhydrase-9 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID552782 | Inhibition of human carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Inhibition of the β-carbonic anhydrase from Streptococcus pneumoniae by inorganic anions and small molecules: Toward innovative drug design of antiinfectives? |
| AID382949 | Solubility in water in presence of 0.0151 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1581512 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1453630 | Inhibition of recombinant human carbonic anhydrase-9 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Synthesis of novel acyl selenoureido benzensulfonamides as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID1758967 | Inhibition of Carbonic anhydrase (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Dibenzazepine-linked isoxazoles: New and potent class of α-glucosidase inhibitors. |
| AID1808976 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID1434428 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | |||
| AID1723501 | Inhibition of carbonic anhydrase in Enterococcus faecium NR-31971 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of ambient air by CLSI protocol based broth microdilution assay | |||
| AID314821 | Inhibition of human carbonic anhydrase 9 in presence of 0.05 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1272994 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID761311 | Inhibition of human mitochondrial carbonic anhydrase 5a after 6 hrs by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | 7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors. |
| AID48088 | Inhibitory activity against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX. |
| AID780926 | Binding affinity to human recombinant carbonic anhydrase 12 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Benzenesulfonamides with pyrimidine moiety as inhibitors of human carbonic anhydrases I, II, VI, VII, XII, and XIII. |
| AID462274 | Inhibition of human CA5A by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1564424 | Inhibition of recombinant human CA2 at 10'-7 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1273001 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 9 to Ki for recombinant human carbonic anhydrase 7 | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1751411 | Inhibition of human CA12 measured by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies. |
| AID48292 | Inhibition constant evaluated for the inhibition of bovine CA IV (Carbonic anhydrase IV) | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1593068 | Inhibition of human CA 12 catalytic domain | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines. |
| AID314824 | Inhibition of human carbonic anhydrase 9 in presence of 0.10 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1607540 | Inhibition of human recombinant carbonic anhydrase 9 preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID1755145 | Inhibition of full length human CA9 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII. |
| AID1357958 | Cytotoxicity against human HT-29 cells after 96 hrs under hypoxic condition by MTT assay | |||
| AID1189116 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase Assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Carbonic Anhydrase Inhibition with Benzenesulfonamides and Tetrafluorobenzenesulfonamides Obtained via Click Chemistry. |
| AID468530 | Inhibition of human CA1 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors; fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II. |
| AID620789 | Selectivity ratio of IC50 for human recombinant CA2 to IC50 for human recombinant CA12 | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID238575 | Inhibitory activity against human carbonic anhydrase IV (hCAIV) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. |
| AID1469002 | Binding affinity to human N-terminal full length His-tagged CA13 (1 to 262 residues) expressed in Escherichia coli BL21(DE3) assessed as dissociation rate constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID328974 | Inhibition of human full length carbonic anhydrase 1 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID1245670 | Inhibition of carbonic anhydrase-13 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID780929 | Binding affinity to human recombinant carbonic anhydrase 2 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Benzenesulfonamides with pyrimidine moiety as inhibitors of human carbonic anhydrases I, II, VI, VII, XII, and XIII. |
| AID1543082 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped flow CO2 hydrase assay | |||
| AID1564418 | Inhibition of recombinant human CA1 at 10'-8 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1152901 | Inhibition of human recombinant carbonic anhydrase 9 pretreated for 15 mins by stopped flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12 | Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors. |
| AID314784 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.05 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID496919 | Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1301275 | Inhibition of human carbonic anhydrase 12 using saturated CO2 as substrate incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1652406 | Inhibition of human CA9 pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID1275910 | Inhibition of Vibrio cholerae beta-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae. |
| AID1519749 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase-2 to Ki for recombinant human carbonic anhydrase-9 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID371558 | Inhibition of full length human recombinant mitochondrial carbonic anhydrase 5B preincubated for 15 mins by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID424442 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. |
| AID1301279 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 12 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID603453 | Selectivity ratio of Ki for human full length cytosolic isoform of carbonic anhydrase 1 to Ki for human recombinant catalytic domain of carbonic anhydrase 12 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1459105 | Inhibition of human erythrocyte carbonic anhydrase-2 | |||
| AID461325 | Inhibition of human erythrocytes CA2 by Lineweaver-Burke analysis | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. |
| AID1254034 | Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID238209 | Inhibitory constant against human Carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols. |
| AID314783 | Inhibition of human carbonic anhydrase 2 in presence of 0.05 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1656168 | Inhibition of human CA12 preincubated for 15 mins by stopped-flow CO2 hydration kinetic assay based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action. |
| AID1504049 | Inhibition of recombinant human carbonic anhydrase 7 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Lucky Switcheroo: Dramatic Potency and Selectivity Improvement of Imidazoline Inhibitors of Human Carbonic Anhydrase VII. |
| AID1520076 | Binding affinity to recombinant human carbonic anhydrase 12 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1158140 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 12 | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties. |
| AID1309026 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | N-Nitrosulfonamides: A new chemotype for carbonic anhydrase inhibition. |
| AID1306530 | Inhibition of Vibrio cholerae carbonic anhydrase beta preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID616477 | Inhibition of Mycobacterium tuberculosis carbonic anhydrase 1 preincubated for 15 mins at pH 8.3 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID610542 | Inhibition of human recombinant carbonic anhydrase 5b preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1723499 | Antibacterial activity against Enterococcus faecalis HM-335 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1442658 | Anticonvulsant activity in Swiss albino mouse assessed as inhibition of myoclonic jerks against subcutaneous pentylenetetrazole-induced seizures at 30 to 100 mg/kg, ip administered 0.5 hrs to 3 hrs prior to PTZ induction | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID1460771 | Inhibition of human CA7 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1703321 | Inhibition of human CA1 incubated for 15 mins by stopped- flow CO2 hydrase assay method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Discovery of first-in-class multi-target adenosine A |
| AID1565766 | Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | From random to rational: A discovery approach to selective subnanomolar inhibitors of human carbonic anhydrase IV based on the Castagnoli-Cushman multicomponent reaction. |
| AID749802 | Inhibition of Mycobacterium tuberculosis RV3588 beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID1419423 | Cytotoxicity against human HT-29 cells assessed as cell viability at 30 uM after 48 hrs under hypoxic conditions by MTT assay (Rvb = 100%) | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID1537867 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) to Ki for recombinant human carbonic anhydrase 12 expressed in Escherichia coli | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID484162 | Inhibition of human carbonic anhydrase 9 catalytic domain preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1688234 | Selectivity index, ratio of Ki for inhibition of recombinant human carbonic anhydrase 2 to inhibition of recombinant human carbonic anhydrase 9 | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID1352816 | Inhibition of human CA2 after 15 mins by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Structural investigations on coumarins leading to chromeno[4,3-c]pyrazol-4-ones and pyrano[4,3-c]pyrazol-4-ones: New scaffolds for the design of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1666825 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID484156 | Inhibition of human carbonic anhydrase 3 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID441714 | Inhibition of human recombinant CA12 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1204106 | Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Sulfonamide inhibition study of the β-class carbonic anhydrase from the caries producing pathogen Streptococcus mutans. |
| AID342470 | Inhibition of AQP4 in wild type mouse brain gilial cells assessed as osmotic water permeability at 10 to 100 uM after 15 mins by calcein quenching assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID295290 | Inhibition of human recombinant CA2 after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID646251 | Inhibition of S-glutathionylated form of human recombinant carbonic anhydrase 7 phosphatase activity using 4-nitrophenyl phosphate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID757574 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1442866 | Inhibition of recombinant human Carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action. |
| AID678517 | Inhibition of human CA9 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors. |
| AID588197 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 2 to Ki for Cryptococcus neoformans recombinant Can2 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1062687 | Inhibition of human CA1 cytosolic isoform after 15 mins by stopped-flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associat |
| AID1655392 | Inhibition of recombinant human carbonic anhydrase 6 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID386501 | Inhibition of human cloned CA9 catalytic domain by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID1266235 | Inhibition of human carbonic anhydrase-12 preincubated for 15 mins by stopped flow CO2 dehydration assay | 2016 | Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1 | Inhibition of carbonic anhydrase isoforms I, II, IV, VII and XII with carboxylates and sulfonamides incorporating phthalimide/phthalic anhydride scaffolds. |
| AID328984 | Inhibition of mouse full length carbonic anhydrase 13 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID367609 | Inhibition of human recombinant full length CA2 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367609 | Inhibition of human recombinant full length CA2 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID50366 | Inhibition constant determined against human cloned carbonic anhydrase I | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
| AID744415 | Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Carbonic anhydrase inhibitors: inhibition of the β-class enzyme from the pathogenic yeast Candida glabrata with sulfonamides, sulfamates and sulfamides. |
| AID1565742 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration at 10'-7 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID238953 | Inhibitory constant against cytosolic human Carbonic anhydrase III using CO2 hydrase assay | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. |
| AID1464264 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase-2 to Ki for human recombinant carbonic anhydrase-12 | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID1902655 | Inhibition of recombinant human CA 12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID1849543 | Binding affinity to human recombinant CA2 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1818406 | Inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors. |
| AID1071787 | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Substituted benzene sulfonamides incorporating 1,3,5-triazinyl moieties potently inhibit human carbonic anhydrases II, IX and XII. |
| AID1408648 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity. |
| AID1902658 | Selectivity ratio of Ki for for inhibition of recombinant human CA 1 to Ki for inhibition of recombinant human CA 12 | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID314786 | Inhibition of human carbonic anhydrase 2 in presence of 0.10 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID759700 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins to 6 hrs by CO2 hydration stopped-flow assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | A class of sulfonamides with strong inhibitory action against the α-carbonic anhydrase from Trypanosoma cruzi. |
| AID739940 | Inhibition of tumor-associated transmembrane human carbonic anhydrase-9 after 15 mins by Stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Structural effect of phenyl ring compared to thiadiazole based adamantyl-sulfonamides on carbonic anhydrase inhibition. |
| AID1692367 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 12 | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID1061891 | Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Inhibition of carbonic anhydrases from the extremophilic bacteria Sulfurihydrogenibium yellostonense (SspCA) and S. azorense (SazCA) with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophe |
| AID239219 | Inhibitory constant value for Carbonic anhydrase II in human determined in esterase assay | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform. |
| AID1188140 | Inhibition of Brucella suis Carbonic anhydrase (213 amino acids) compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID414961 | Inhibition of Mycobacterium tuberculosis H37Rv recombinant beta-carbonic anhydrase 1 expressed in Escherichia coli BL21 by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID1691501 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID1491570 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 12 | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | |
| AID244540 | Inhibition constant against human recombinant carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumo |
| AID1373168 | Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5A expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID647373 | Inhibition of Astrosclera willeyana recombinant GST-tagged astrosclerin 3 expressed in Escherichia coli BL21-DE3-RIPL cells preincubated for 15 mins measured for 10 to 100 secs by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Anion inhibition studies of an α-carbonic anhydrase from the living fossil Astrosclera willeyana. |
| AID1306524 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1709146 | Inhibition of recombinant human carbonic anhydrase 1 by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | 3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation. |
| AID48119 | Inhibition of bovine membrane bound isozyme carbonic anhydrase IV isolated from microsomes at 20 degree C | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
| AID1723513 | Inhibition of carbonic anhydrase in Enterococcus faecalis HM-334 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of 5% CO2 by CLSI protocol based broth microdilution assay | |||
| AID1706628 | Selectivity index, ratio of Ki for inhibition of human CA2 to Ki for inhibition of human CA9 | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID311027 | Inhibition of human carbonic anhydrase 5A | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID734183 | Inhibition of recombinant human carbonic anhydrase 9 after 15 mins by stopped flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship. |
| AID1771799 | Anti-hypersensitive activity in CD-1 albino mouse model of oxaliplatin-induced neuropathic pain assessed as longer duration of action at 100 mg/kg, po administered 14 days post oxaliplatin induction measured after 30 mins by cold plate test | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action. |
| AID1733129 | Inhibition of recombinant human carbonic anhydrase 1 pre-incubated for 10 mins by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 39 | Synthesis and biological evaluation of novel 4,7-disubstituted coumarins as selective tumor-associated carbonic anhydrase IX and XII inhibitors. |
| AID299550 | Inhibition of Helicobacter pylori alpha CA | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID1460773 | Inhibition of human CA12 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID314790 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.25 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID314773 | Inhibition of human carbonic anhydrase 9 in presence of 0.25 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID620796 | Cytotoxicity against CA9-deficient chinese hamster PS120 cells assessed as cell viability at 300 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID167480 | Evaluated for effect on intraocular pressure(IOP) in rabbit after 1 hour | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors. |
| AID238220 | Inhibitory constant against human Carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX. |
| AID328977 | Inhibition of human full length carbonic anhydrase 4 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID1243112 | Inhibition of human carbonic anhydrase 2 at 10'-9 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID339666 | Inhibition of human recombinant carbonic anhydrase 5B by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1076530 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Design, synthesis and evaluation of N-substituted saccharin derivatives as selective inhibitors of tumor-associated carbonic anhydrase XII. |
| AID1423028 | Inhibition of human CA1 by Lineweaver-Burk plot analysis | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides. |
| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID47938 | Inhibitory activity against human recombinant carbonic anhydrase II | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID1242661 | Inhibition of full length human carbonic anhydrase-1 by stopped-flow CO2 hydration assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. |
| AID775834 | Inhibition of human recombinant MMP-2 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2.AcOH as substrate at 10 uM preincubated for 30 mins prior to substrate addition measured for 30 mins by fluorescence assay relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID311030 | Inhibition of human carbonic anhydrase 7 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1291092 | Inhibition of recombinant human carbonic anhydrase 2 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID1784928 | Inhibition of human CA1 measured after 15 mins by stopped flow carbon dioxide anhydrase assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Natural inspired piperine-based sulfonamides and carboxylic acids as carbonic anhydrase inhibitors: Design, synthesis and biological evaluation. |
| AID749806 | Inhibition of human carbonic anhydrase-5A preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID1873564 | Inhibition of human carbonic anhydrase 2 by stopped flow CO2 assay | 2022 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 70 | Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors. |
| AID48295 | Inhibition constant evaluated for the inhibition of human CA IX (Carbonic anhydrase IX) | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1720897 | Inhibition of recombinant human carbonic anhydrase 1 assessed as inhibition constant preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | New coumarin/sulfocoumarin linked phenylacrylamides as selective transmembrane carbonic anhydrase inhibitors: Synthesis and in-vitro biological evaluation. |
| AID1655628 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII. |
| AID1070019 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Anion inhibition studies of two new β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID539004 | Inhibition of Aspergillus fumigatus ChiA1 expressed in Pichia pastoris at 1 mM after 70 mins | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Acetazolamide-based fungal chitinase inhibitors. |
| AID616466 | Inhibition of Mycobacterium tuberculosis carbonic anhydrase 2 preincubated for 15 mins at pH 8.3 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1350479 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
| AID1331202 | Inhibition of human recombinant carbonic anhydrase 7 expressed in Escherichia coli assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1 | Microwave assisted synthesis of novel tetrazole/sulfonamide derivatives based on octahydroacridine, xanthene and chromene skeletons as inhibitors of the carbonic anhydrases isoforms I, II, IV and VII. |
| AID474206 | Selectivity ratio of Ki for human recombinant CA1 to Ki for human recombinant CA9 | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID1631901 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and carbonic anhydrase inhibitory effects of new N-glycosylsulfonamides incorporating the phenol moiety. |
| AID58924 | Relative salidiuretic efficacy was scored in dog; weak | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID1439688 | Inhibition of recombinant human membrane-associated carbonic anhydrase 4 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. |
| AID1647459 | Inhibition of human carbonic anhydrase 2 using 4-NPA as substrate measured for 3 mins by spectrophotometry | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID287700 | Inhibition of human recombinant carbonic anhydrase 9 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates. |
| AID749804 | Inhibition of Candida glabrata beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID1251959 | Inhibition of recombinant human carbonic anhydrase 9 catalytic domain expressed in Escherichia coli incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII. |
| AID1360268 | Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents. |
| AID300870 | Selectivity ratio of Ki for human cloned CA1 to Ki for human cloned catalytic domain CA9 | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety. |
| AID1453629 | Inhibition of recombinant human carbonic anhydrase-7 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Synthesis of novel acyl selenoureido benzensulfonamides as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID1631902 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and carbonic anhydrase inhibitory effects of new N-glycosylsulfonamides incorporating the phenol moiety. |
| AID644379 | Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana. |
| AID588194 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 2 to Ki for Mycobacterium tuberculosis recombinant Rv3273 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1849546 | Binding affinity to human recombinant CA9 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1604486 | Inhibition of human CA9 pre-incubated for 6 hrs by stopped- flow CO2 hydrase assay method based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID239284 | Inhibitory activity against catalytic domain of human carbonic anhydrase XII | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma. |
| AID1331199 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1 | Microwave assisted synthesis of novel tetrazole/sulfonamide derivatives based on octahydroacridine, xanthene and chromene skeletons as inhibitors of the carbonic anhydrases isoforms I, II, IV and VII. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1060763 | Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors. |
| AID462275 | Inhibition of human CA5B by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1517561 | Inhibition of human carbonic anhydrase 2 at 10'-7 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID588185 | Inhibition of Cryptococcus neoformans recombinant Can2 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1849551 | Binding affinity to human recombinant CA12 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID732023 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Carbonic anhydrase inhibitors: benzenesulfonamides incorporating cyanoacrylamide moieties are low nanomolar/subnanomolar inhibitors of the tumor-associated isoforms IX and XII. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID1446118 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 30 uM after 72 hrs under hypoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1129144 | Inhibition of human recombinant cytosolic human carbonic anhydrase-1 incubated for 15 mins prior to testing by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7 | Synthesis and carbonic anhydrase I, II, IX and XII inhibition studies of 4-N,N-disubstituted sulfanilamides incorporating 4,4,4-trifluoro-3-oxo-but-1-enyl, phenacylthiourea and imidazol-2(3H)-one/thione moieties. |
| AID1706620 | Inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID1152903 | Inhibition of human recombinant carbonic anhydrase 14 pretreated for 15 mins by stopped flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12 | Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors. |
| AID1517551 | Selectivity Index, ratio of Ki for human carbonic anhydrase 12 to Ki for human carbonic anhydrase 2 | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1849559 | Binding affinity to human CA2 assessed as inhibition constant by Lineweaver-Burk plot analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1879878 | Inhibition of human recombinant carbonic anhydrase 1 assessed as inhibition constant incubated for 10 mins by phenol red dye based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID1439692 | Selectivity ratio of Ki for human membrane-associated carbonic anhydrase 4 to Ki for recombinant human tumor-associated carbonic anhydrase 9 | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. |
| AID1548135 | Inhibition of Malassezia globosa beta carbonic anhydrase incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID1633344 | Inhibition of recombinant human carbonic anhydrase 4 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID320316 | Inhibition of human recombinant full length carbonic hydrase 14 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID1053400 | Selectivity ratio of Ki for full length human cytosolic carbonic anhydrase-2 to Ki for recombinant human catalytic domain carbonic anhydrase-12 | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates. |
| AID1238073 | Inhibition of human erythrocytes CA2 using 4-nitrophenylacetate as substrate by esterase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Synthesis and carbonic anhydrase inhibitory properties of novel uracil derivatives. |
| AID775833 | Inhibition of human recombinant MMP-12 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2.AcOH as substrate at 10 uM preincubated for 30 mins prior to substrate addition measured for 30 mins by fluorescence assay relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID1692370 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 9 | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID47905 | Inhibitory effect on human Carbonic anhydrase II | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. |
| AID610536 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID238085 | Inhibition constant against human (cloned) isozyme (hCA I) by the CO2 hydration method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID1067261 | Inhibition of human recombinant transmembrane carbonic anhydrase 12 after 6 hrs by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Synthesis of 6-tetrazolyl-substituted sulfocoumarins acting as highly potent and selective inhibitors of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID314809 | Inhibition of human carbonic anhydrase 9 in presence of 0.25 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID287698 | Inhibition of human recombinant carbonic anhydrase 1 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates. |
| AID166788 | Corneal penetration rate constant (k) for excised denuded cornea of albino rabbit | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide. |
| AID1656167 | Inhibition of human CA4 preincubated for 15 mins by stopped-flow CO2 hydration kinetic assay based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action. |
| AID729568 | Inhibition of Drosophila melanogaster recombinant beat carbonic anhydrase expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Characterization, bioinformatic analysis and dithiocarbamate inhibition studies of two new α-carbonic anhydrases, CAH1 and CAH2, from the fruit fly Drosophila melanogaster. |
| AID1736563 | Inhibition of recombinant human CA12 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1358710 | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID300806 | Inhibition of cloned catalytic domani of human carbonic anhydrase 9 by CO2 hydration stopped-flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I and II, and extracellular isoforms IV, IX, and XII with sulfamides incorporating sugar moieties. |
| AID1379905 | Inhibition of recombinant human carbonic anhydrase 9 catalytic domain preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. |
| AID610544 | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID48338 | In vitro inhibition of HCO3- stimulated swelling in cat cerebrocortical tissue slice | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID1821398 | Inhibition of human CA12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes. |
| AID468532 | Inhibition of tumor associated human recombinant CA9 catalytic domain by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors; fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II. |
| AID1061169 | Inhibition of recombinant Methanosarcina thermophila gamma-CA CAM by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis. |
| AID1736565 | Inhibition of recombinant human CA2 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1335032 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 preincubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | 5-Substituted-benzylsulfanyl-thiophene-2-sulfonamides with effective carbonic anhydrase inhibitory activity: Solution and crystallographic investigations. |
| AID27591 | Partition coefficient (logD) (chloroform/buffer) | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID1782945 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 4 to Ki for inhibition of recombinant human carbonic anhydrase 2 | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID1442644 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID1504709 | Inhibition of human carbonic anhydrase-1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study. |
| AID620797 | Cytotoxicity against CA9 expressing chinese hamster PS120 cells assessed as cell viability at 300 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID601818 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed mouse | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV. |
| AID1195032 | Inhibition of human CA-2 using p-nitro-phenylacetate as substrate by Lineweaver-Burk plot analysis | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II. |
| AID1196824 | Inhibition of recombinant human carbonic anhydrase 2 by CO2 hydration assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Carbonic anhydrase inhibitors with dual-tail moieties to match the hydrophobic and hydrophilic halves of the carbonic anhydrase active site. |
| AID237409 | Compound level in Red Blood Cells at 48 h, after Exposure of 10 mL of Blood to Compound solution by electronic spectroscopic method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID462281 | Inhibition of human CA14 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1291356 | Inhibition of recombinant Flaveria bidentis beta-carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID417826 | Inhibition of human recombinant full length CA2 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1240214 | Inhibition of Nostoc commune gamma carbonic anhydrase by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1356463 | Binding affinity to human carbonic anhydrase 9 by stopped flow CO2 hydration method | 2018 | ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7 | Targeting Tumor Associated Carbonic Anhydrases IX and XII: Highly Isozyme Selective Coumarin and Psoralen Inhibitors. |
| AID1571207 | Inhibition of human carbonic anhydrase-9 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies. |
| AID1723511 | Inhibition of carbonic anhydrase in Enterococcus faecium NR-31972 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of 5% CO2 by CLSI protocol based broth microdilution assay | |||
| AID1053403 | Inhibition of recombinant human catalytic domain of carbonic anhydrase-9 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates. |
| AID1360940 | Binding affinity to human carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors. |
| AID1442868 | Inhibition of recombinant human Carbonic anhydrase 5A assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action. |
| AID1373175 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 14 (20 to 280 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1564419 | Inhibition of recombinant human CA1 at 10'-7 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID238852 | Mean inhibitory constant towards human carbonic anhydrase II determined by stopped-flow method | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. |
| AID1231562 | Inhibition of human carbonic anhydrase-12 pre-incubated for 15 mins by stopped-flow CO2 hydration assay based Lineweaver-Burk plot method | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors. |
| AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1360942 | Binding affinity to human carbonic anhydrase 4 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors. |
| AID620645 | Cytotoxicity against chinese hamster PS120 cells expressing CA9 assessed as cell viability at 300 uM and pH 6.4 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1238078 | Inhibition of human carbonic anhydrase-12 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII. |
| AID1604483 | Inhibition of human CA1 pre-incubated for 6 hrs by stopped- flow CO2 hydrase assay method based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID1759810 | Inhibition of Vibrio cholerae alpha carbonic anhydrase preincubated with enzyme for 15 mins by phenol red-based stopped-flow CO2 hydration assay | |||
| AID382966 | Solubility in water in presence of 0.0755 mol/l hydroxypropyl-beta-cyclodextrin and 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1556940 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 2 expressed in Escherichia coli to Ki for human recombinant carbonic anhydrase 12 expressed in Escherichia coli | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID238761 | Binding affinity towards human cloned carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties. |
| AID1268964 | Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA. |
| AID1336560 | Inhibition of Nostoc commune recombinant carbonic anhydrase gamma assessed as inhibition of CO2 hydration preincubated for 15 mins by Lineweaver-burk plot method | |||
| AID1849569 | Binding affinity to human CA2 assessed as inhibition constant by esterase activity assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1243113 | Inhibition of human carbonic anhydrase 2 at 10'-8 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID386500 | Inhibition of human cloned CA1 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID1245668 | Inhibition of carbonic anhydrase-5B (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID238225 | Inhibitory constant against human Carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols. |
| AID316065 | Inhibition of human recombinant full length carbonic hydrase 5B by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1152902 | Inhibition of human recombinant carbonic anhydrase 12 pretreated for 15 mins by stopped flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12 | Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors. |
| AID678516 | Inhibition of human CA2 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors. |
| AID1257052 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Interaction of carbonic anhydrase isozymes I, II, and IX with some pyridine and phenol hydrazinecarbothioamide derivatives. |
| AID1240213 | Inhibition of Porphyromonas gingivalis gamma carbonic anhydrase by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1168854 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Structural insights on carbonic anhydrase inhibitory action, isoform selectivity, and potency of sulfonamides and coumarins incorporating arylsulfonylureido groups. |
| AID1723498 | Antibacterial activity against Enterococcus faecium NR-31971 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1446113 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 100 uM after 48 hrs under hypoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID616481 | Inhibition of human carbonic anhydrase 14 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1655396 | Inhibition of recombinant human carbonic anhydrase 13 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID725956 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4 | Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease. |
| AID1422970 | Inhibition of recombinant human CA9 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1556933 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID1517244 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration incubated for 1 hr by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID1183266 | Inhibition of human cloned CA2 pre-incubated with enzyme for 15 mins by phenol red based CO2 hydration stopped-flow assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis of a new series of N⁴-substituted 4-(2-aminoethyl)benzenesulfonamides and their inhibitory effect on human carbonic anhydrase cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII. |
| AID1394916 | Inhibition of cytosolic human carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID48300 | Inhibitory activity against human cloned carbonic anhydrase isozyme IX, by CO2 hydrase assay method. | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides. |
| AID441207 | Inhibition of human cloned CA2 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID620784 | Inhibition of human recombinant CA1 by CO2 hydration based stopped flow assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1062686 | Inhibition of human CA2 cytosolic isoform after 15 mins by stopped-flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associat |
| AID1604487 | Inhibition of human CA12 pre-incubated for 6 hrs by stopped- flow CO2 hydrase assay method based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID1727539 | Inhibition of recombinant human carbonic anhydrase 4 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion. |
| AID1185072 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Carbonic anhydrase inhibitors: design, synthesis, and biological evaluation of novel sulfonyl semicarbazide derivatives. |
| AID1278408 | Inhibition of Methanosarcina thermophila gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID1425989 | Binding affinity to recombinant human carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. |
| AID1266233 | Inhibition of human carbonic anhydrase-4 preincubated for 15 mins by stopped flow CO2 dehydration assay | 2016 | Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1 | Inhibition of carbonic anhydrase isoforms I, II, IV, VII and XII with carboxylates and sulfonamides incorporating phthalimide/phthalic anhydride scaffolds. |
| AID48093 | Inhibition of human recombinant carbonic anhydrase II (CA2) | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID1474296 | Inhibition of recombinant human transmembrane carbonic anhydrase 9 pretreated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Evaluation of selenide, diselenide and selenoheterocycle derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors. |
| AID1517568 | Inhibition of human carbonic anhydrase 9 at 10'-5 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1518921 | Inhibition of recombinant human carbonic anhydrase 1 at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID50187 | Inhibition concentration by inhibition of carbonic anhydrase from blood in Rat | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8 | Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives. |
| AID1077015 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 9 | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1182980 | Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Synthesis of sulfonamides with effective inhibitory action against Porphyromonas gingivalis γ-carbonic anhydrase. |
| AID1564596 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity. |
| AID493888 | Inhibition of human recombinant carbonic anhydrase 5b after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID166951 | Compound was tested in vitro for corneal permeability of compound across the Denuded epithelial cornea obtained from rabbit | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring? |
| AID730898 | Binding affinity to human recombinant carbonic anhydrase 12 expressed in Escherichia coli Rosetta (DE3) in phosphate buffer at pH 7 by isothermal titration calorimetry assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Characterization of human carbonic anhydrase XII stability and inhibitor binding. |
| AID1560585 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 12 | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID1474380 | Inhibition of recombinant human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate pretreated for 15 mins prior to test by spectrophotometric method | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. |
| AID1849599 | Inhibition of human CA1 using 4-nitrophenylacetate as substrate incubated for 10 mins prior to testing by spectrophotometry based esterase assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1504979 | Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases. |
| AID1312153 | Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID757573 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1655626 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII. |
| AID1623425 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration after 15 mins by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment. |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1518926 | Inhibition of recombinant human carbonic anhydrase 2 assessed as residual activity at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID588184 | Inhibition of Candida albicans recombinant Nce103 beta-carbonic anhydrase after 15 mins by stopped flow CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID238437 | Inhibition constant against human carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes. |
| AID1565736 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration at 10'-9 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1707343 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors. |
| AID616479 | Inhibition of Candida albicans carbonic anhydrase preincubated for 15 mins at pH 8.3 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1704679 | Inhibition of human CA2 preincubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. |
| AID1266245 | Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped flow CO2 dehydration method | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies. |
| AID1504902 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors. |
| AID48122 | Inhibitory activity against bovine carbonic anhydrase IV | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties. |
| AID1518918 | Inhibition of recombinant human carbonic anhydrase 1 assessed as residual activity at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID493894 | Inhibition of human recombinant carbonic anhydrase 14 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1660019 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID1686870 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 1 to Ki for Ki for inhibition of recombinant human carbonic anhydrase 7 | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID1731039 | Inhibition of CAH9 in human UFH-001 cells at 1 uM by membrane inlet for mass spectrometry | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1519760 | Inhibition of recombinant human carbonic anhydrase-9 at 0.01 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1194024 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune. |
| AID314761 | Inhibition of human carbonic anhydrase 9 | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1565735 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration at 10'-5 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID411527 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411527 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID775827 | Binding affinity to human holo-transferrin assessed as pseudo-first-order rate constant measured as removal of ferric ion at 1 mM measured for 1 hr by UV-vis spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID1504048 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Lucky Switcheroo: Dramatic Potency and Selectivity Improvement of Imidazoline Inhibitors of Human Carbonic Anhydrase VII. |
| AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID598015 | Inhibition of human recombinant CA12 catalytic domain by CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and crystallographic analysis of new sulfonamides incorporating NO-donating moieties with potent antiglaucoma action. |
| AID1666822 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID1723510 | Inhibition of carbonic anhydrase in Enterococcus faecium NR-31971 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of 5% CO2 by CLSI protocol based broth microdilution assay | |||
| AID1172692 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Carbonic anhydrase inhibitory activity of sulfonamides and carboxylic acids incorporating cyclic imide scaffolds. |
| AID1125517 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 | Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII. |
| AID462271 | Inhibition of human CA2 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID448552 | Inhibition of human cloned full length carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides. |
| AID612729 | Inhibition of Brucella suis recombinant carbonic anhydrase 1 at pH 8.3 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. |
| AID587127 | Inhibition of human carbonic anhydrase 4 after 15 mins by Lineweaver-Burk plot | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID436746 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
| AID1518916 | Inhibition of recombinant human carbonic anhydrase 1 assessed as residual activity at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID1752205 | Inhibition of recombinant human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors. |
| AID239145 | Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID1597782 | Inhibition of human recombinant N-HA-tagged carbonic anhydrase 2 expressed in HEK293T cells using p-nitrophenyl acetate as substrate measured after 30 mins by colorimetric analysis | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17 | Sulfonate and sulfamate derivatives possessing benzofuran or benzothiophene nucleus as potent carbonic anhydrase II/IX/XII inhibitors. |
| AID47710 | Inhibition of human recombinant carbonic anhydrase I (CA1) | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID1360101 | Inhibition of human carbonic anhydrase 7 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and X-ray crystallography of selenides bearing benzenesulfonamide moiety with neuropathic pain modulating effects. |
| AID1231566 | Inhibition of esterase activity of carbonic anhydrase 1 in human erythrocytes using PNF as substrate by spectrophotometer analysis | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Discovery of potent carbonic anhydrase and acetylcholine esterase inhibitors: novel sulfamoylcarbamates and sulfamides derived from acetophenones. |
| AID1818310 | Selectivity index, ratio of Ki for inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assa | |||
| AID1607539 | Inhibition of human recombinant carbonic anhydrase 7 preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID1518934 | Inhibition of recombinant human carbonic anhydrase 9 assessed as residual activity at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1474295 | Inhibition of recombinant human cytosolic carbonic anhydrase 7 pretreated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Evaluation of selenide, diselenide and selenoheterocycle derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors. |
| AID1433064 | Inhibition of human CA1 using para-nitrophenylacetate as substrate measured over 3 mins by UV-vis spectrophotometric method | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and carbonic anhydrase isoenzymes I, II, IX, and XII inhibitory effects of dimethoxybromophenol derivatives incorporating cyclopropane moieties. |
| AID1849576 | Inhibition of human recombinant CA2 incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1818305 | Inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID365981 | Inhibition of human cloned CA4 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID726599 | Corneal permeability in rabbit corneal tissues mounted on vertical Using chambers | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4 | A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma. |
| AID1442657 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 30 mg/kg, ip administered 0.5 hrs to 3 hrs prior to PTZ induction | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID1731027 | Inhibition of human CAH9 catalytic domain expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1754556 | Inhibition of recombinant human CA 1 preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity. |
| AID1821395 | Inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes. |
| AID314797 | Inhibition of human carbonic anhydrase 9 in presence of 10 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1358714 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 9 | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID1537865 | Inhibition of recombinant human carbonic anhydrase 12 expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID732710 | Binding affinity to human recombinant CA12 at 37 degC and pH 7.0 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | 4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII. |
| AID1504905 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors. |
| AID349606 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. |
| AID1849544 | Binding affinity to human recombinant CA4 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID263639 | Selectivity for Helicobacter pylori recombinant CA over human recombinant CA2 | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori. |
| AID1723517 | Aqueous solubility of compound in water | |||
| AID1072629 | Inhibition of human transmembrane carbonic anhydrase 12 by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID416125 | Inhibition of human erythrocyte CA1 esterase activity using 4-nitrophenyl acetate substrate | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols. |
| AID697243 | Inhibition of full length human CA2 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. |
| AID350905 | Inhibition of human carbonic anhydrase 2 by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Effects of new 5-amino-1,3,4-thiadiazole-2-sulfonamide derivatives on human carbonic anhydrase isozymes. |
| AID1373165 | Binding affinity to recombinant human full length N-terminal His-tagged carbonic anhydrase 2 (1 to 260 residues) expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID295291 | Inhibition of human recombinant CA4 after 15 mins by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
| AID1071784 | Inhibition of human transmembrane carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Substituted benzene sulfonamides incorporating 1,3,5-triazinyl moieties potently inhibit human carbonic anhydrases II, IX and XII. |
| AID244228 | Ratio of inhibitory potency against carbonic anhydrase II to that of inhibitory potency against carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX. |
| AID1723490 | Antibacterial activity against Enterococcus faecium HM965 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID414958 | Inhibition of human mitochondrial carbonic anhydrase 5A by stopped flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. |
| AID1254035 | Inhibition of Plasmodium falciparum eta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID1255572 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli preincubated for 6 hrs by stopped flow CO2 hydrase assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Isatin-pyrazole benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1520075 | Binding affinity to recombinant human carbonic anhydrase 9 expressed in mammalian cell expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID725955 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4 | Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease. |
| AID1560584 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 12 | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID301578 | Inhibition of human recombinant CA 3 assessed as CO2 hydration by stopped flow kinetic assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID1278742 | Inhibition of recombinant Vibrio cholerae beta-carbonic anhydrase expressed in competent Escherichia coli BL21(DE3) cells preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5 | Anion inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae. |
| AID258732 | Inhibitory activity against cloned human CA9 | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib. |
| AID1902656 | Selectivity ratio of Ki for for inhibition of recombinant human CA 1 to Ki for inhibition of recombinant human CA 9 | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID388108 | Cytotoxicity against human BC cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Carbonic anhydrase inhibitors: inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides-in vitro and in vivo studies. |
| AID1809103 | Inhibition of recombinant human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis. |
| AID301521 | Inhibition of human cloned carbonic anhydrase1 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2-thione derivatives with carbonic anhydrase inhibitory activity. |
| AID1688233 | Inhibition of recombinant human carbonic anhydrase 12 measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID272522 | Inhibition of human cloned CA4 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1604484 | Inhibition of human CA2 pre-incubated for 6 hrs by stopped- flow CO2 hydrase assay method based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID1194025 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune. |
| AID757575 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1511291 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins to 2 hrs by phenol red dye based stopped flow CO2 hydrase assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID1161954 | Inhibition of Helicobacter pylori carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID726603 | Inhibition of human recombinant carbonic anhydrase 2 by dansylamide (DNSA) competition assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4 | A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma. |
| AID1754559 | Inhibition of recombinant human CA7 preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity. |
| AID1504977 | Inhibition of human carbonic anhydrase 4 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases. |
| AID764496 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Inhibition of tumor-associated human carbonic anhydrase isozymes IX and XII by a new class of substituted-phenylacetamido aromatic sulfonamides. |
| AID1752203 | Inhibition of recombinant human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors. |
| AID242850 | Kcat value against human carbonic anhydrase III | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID734182 | Selectivity ratio of IC50 for recombinant human carbonic anhydrase 1 to IC50 for recombinant human carbonic anhydrase 9 | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship. |
| AID369274 | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID1517565 | Inhibition of human carbonic anhydrase 9 at 10'-8 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID441206 | Inhibition of human cloned CA1 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID1310851 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | PEGylated Bis-Sulfonamide Carbonic Anhydrase Inhibitors Can Efficiently Control the Growth of Several Carbonic Anhydrase IX-Expressing Carcinomas. |
| AID1291363 | Inhibition of recombinant Vibrio cholerae gamma-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID474208 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID1336989 | Inhibition of recombinant human membrane bound carbonic anhydrase 12 by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID1125515 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 | Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII. |
| AID1347714 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydration assay | |||
| AID1170187 | Inhibition of human carbonic anhydrase 9 at pH7 and 25 degC by stopped-flow kinetic inhibition assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID93579 | Level in red blood cells after incubation of human erythrocytes for 30 min, was determined by EI method | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1243104 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID650298 | Inhibition of human full length cloned transmembrane carbonic anhydrase 14 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases. |
| AID775832 | Inhibition of human carbonic anhydrase 2 assessed as p-nitrophenyl acetate conversion to p-nitrophenolate anion at 10 uM preincubated for 10 mins prior to substrate addition measured for 20 mins by spectrophotometric analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID1306532 | Inhibition of Vibrio cholerae recombinant carbonic anhydrase gamma expressed in Escherichia coli DE3 cells preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID299224 | Activity of human CA1 at pH 7.5 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID681388 | TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes | 2000 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1 | Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1. |
| AID1491567 | Inhibition of recombinant human carbonic anhydrase 2 assessed as reduction in CO2 hydration pretreated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | |
| AID1478802 | Inhibition of human carbonic anhydrase 7 incubated for 10 mins by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Synthesis and biological evaluation of novel aromatic and heterocyclic bis-sulfonamide Schiff bases as carbonic anhydrase I, II, VII and IX inhibitors. |
| AID739939 | Inhibition of tumor-associated transmembrane human carbonic anhydrase-12 after 15 mins by Stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Structural effect of phenyl ring compared to thiadiazole based adamantyl-sulfonamides on carbonic anhydrase inhibition. |
| AID238259 | Ratio against Carbonic anhydrase II to Carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds. |
| AID456400 | Inhibition of human recombinant carbonic anhydrase 5B by stopped flow CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Carbonic anhydrase inhibitors. Identification of selective inhibitors of the human mitochondrial isozymes VA and VB over the cytosolic isozymes I and II from a natural product-based phenolic library. |
| AID1692374 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID25801 | The compound was evaluated for in Vitro corneal permeability when no epithelium | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route. |
| AID1548131 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID1427471 | Inhibition of recombinant human carbonic anhydrase-7 assessed as reduction in enzyme-catalyzed hydration activity using CO2 as substrate preincubated for 15 mins followed substrate addition measured after 10 to 100 sec by phenol red dye based stopped flow | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3- and 4-(hetero)arylisoxazol-5-amine scaffolds. |
| AID271172 | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
| AID1849568 | Binding affinity to human CA1 assessed as inhibition constant by esterase activity assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1336992 | Selectivity ratio of Ki for human erythrocyte cytosolic carbonic anhydrase 1 to Ki for human membrane bound carbonic anhydrase 12 | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID1262263 | Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus. |
| AID1352817 | Inhibition of human CA9 after 15 mins by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Structural investigations on coumarins leading to chromeno[4,3-c]pyrazol-4-ones and pyrano[4,3-c]pyrazol-4-ones: New scaffolds for the design of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1518940 | Inhibition of recombinant human carbonic anhydrase 12 at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1275912 | Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae. |
| AID1757211 | Inhibition of human CA2 by stopped- flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID365984 | Inhibition of human cloned CA6 by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID577533 | Antibacterial activity against Brucella suis at 100 uM after 11 days | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID243113 | Ratio of Kcat/Km against huamn carbonic anhydrase III | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID610540 | Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1857417 | Inhibition of human recombinant CA9 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID1243117 | Inhibition of human carbonic anhydrase 9 at 10'-8 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID314814 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 10 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID387434 | Inhibition of Candida albicans Nce103 at 20 degC by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions. |
| AID577526 | Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID1706627 | Selectivity index, ratio of Ki for inhibition of human CA1 to Ki for inhibition of human CA12 | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID711005 | Inhibition of human erythrocyte carbonic anhydrase-2 assessed as hydrolysis of 4-nitrophenylacetate | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors. |
| AID382961 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.1660 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1067226 | Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 9 | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. |
| AID1879884 | Selectivity ratio of Ki for inhibition of human recombinant carbonic anhydrase 1 to Ki for inhibition of human recombinant carbonic anhydrase 12 | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID1879881 | Inhibition of human recombinant carbonic anhydrase 12 assessed as inhibition constant incubated for 10 mins by phenol red dye based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID753461 | Selectivity ratio of IC50 for full length carbonic anhydrase-2 in human erythrocytes to IC50 for GST-tagged recombinant carbonic anhydrase-9 catalytic domain (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening. |
| AID1519748 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase-1 to Ki for recombinant human carbonic anhydrase-12 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID428458 | Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1581510 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1231567 | Inhibition of esterase activity of carbonic anhydrase 2 in human erythrocytes using PNF as substrate by spectrophotometer analysis | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Discovery of potent carbonic anhydrase and acetylcholine esterase inhibitors: novel sulfamoylcarbamates and sulfamides derived from acetophenones. |
| AID1170158 | Inhibition of human CA-2 by stopped flow CO2 hydrase assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | A class of 4-sulfamoylphenyl-ω-aminoalkyl ethers with effective carbonic anhydrase inhibitory action and antiglaucoma effects. |
| AID552127 | Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. |
| AID759696 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for Trypanosoma cruzi carbonic anhydrase | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | A class of sulfonamides with strong inhibitory action against the α-carbonic anhydrase from Trypanosoma cruzi. |
| AID1360265 | Inhibition of human carbonic anhydrase 2 expressed in Escherichia coli BL21 D3 strain using p-nitrophenyl acetate as substrate by UV/visible spectrophotometry | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents. |
| AID1659547 | Selectivity index, ratio of IC50 for human carbonic anhydrase 2 using p-nitrophenyl acetate as substrate to IC50 for human carbonic anhydrase 9 using p-nitrophenyl acetate as substrate | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX. |
| AID48098 | The equilibrium dissociation constant of the inhibitor-enzyme complex of human carbonic anhydrase | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma. |
| AID1306529 | Inhibition of Helicobacter pylori beta carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID238830 | Inhibitory activity against human carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma. |
| AID1387633 | Inhibition of recombinant human carbonic anhydrase 9 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines. |
| AID342485 | Inhibition of human carbonic anhydrase 14 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1818308 | Inhibition of human CA12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1460767 | Inhibition of human CA4 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1857412 | Inhibition of human recombinant CA1 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID166762 | Variation of intraocular pressure in seventh day at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID1242664 | Inhibition of human recombinant carbonic anhydrase-12 catalytic domain by stopped-flow CO2 hydration assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. |
| AID1511292 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins to 2 hrs by phenol red dye based stopped flow CO2 hydrase assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID238224 | Inhibitory constant against human Carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX. |
| AID437834 | Inhibition of human full length cytosolic carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1322630 | Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped flow carbon dioxide hydrase assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure Lowering Investigations. |
| AID1633346 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1185075 | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Carbonic anhydrase inhibitors: design, synthesis, and biological evaluation of novel sulfonyl semicarbazide derivatives. |
| AID1193750 | Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID1726059 | Inhibition of Vibrio cholerae alpha carbonic anhydrase incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1581511 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID271174 | Inhibition of human recombinant carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
| AID441715 | Inhibition of human recombinant CA13 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1723495 | Antibacterial activity against Enterococcus faecium NR-31914 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID1129146 | Inhibition of human recombinant transmembrane tumor associated carbonic anhydrase-9 incubated for 15 mins prior to testing by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7 | Synthesis and carbonic anhydrase I, II, IX and XII inhibition studies of 4-N,N-disubstituted sulfanilamides incorporating 4,4,4-trifluoro-3-oxo-but-1-enyl, phenacylthiourea and imidazol-2(3H)-one/thione moieties. |
| AID415833 | Selectivity ratio of Ki for human CA2 to Ki for human recombinant CA9 | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors. |
| AID1739496 | Inhibition of human CA1 by stopped-flow carbon dioxide hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases. |
| AID1548137 | Inhibition of Leishmania donovani beta carbonic anhydrase incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID1234500 | Inhibition of human carbonic anhydrase 2 by by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design and synthesis of benzothiazole-6-sulfonamides acting as highly potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1336986 | Inhibition of recombinant human erythrocyte cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID1519765 | Inhibition of recombinant human carbonic anhydrase-12 at 0.1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1471680 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX). |
| AID1125516 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 | Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII. |
| AID339673 | Inhibition of human recombinant carbonic anhydrase 6 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1275629 | Inhibition of human carbonic anhydrase 2 for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Kinetic and X-ray crystallographic investigations on carbonic anhydrase isoforms I, II, IX and XII of a thioureido analog of SLC-0111. |
| AID1322631 | Inhibition of human carbonic anhydrase 9 pre-incubated for 15 mins by stopped flow carbon dioxide hydrase assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure Lowering Investigations. |
| AID50373 | Inhibitory activity against human recombinant carbonic anhydrase I | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID1234859 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | 5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII. |
| AID317581 | Inhibition of human CA9 catalytic domain by CO2 hydration method | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. |
| AID484164 | Inhibition of full length mouse carbonic anhydrase 13 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID242849 | Kcat value against human carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID299234 | Ratio of kcat to Km of human CA2 | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID369276 | Inhibition of human carbonic anhydrase 4 | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID1518925 | Inhibition of recombinant human carbonic anhydrase 2 assessed as residual activity at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID753465 | Inhibition of full length carbonic anhydrase-1 in human erythrocytes | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening. |
| AID711662 | Selectivity ratio of Ki for human CA2 to Ki for human CA9 | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel series 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1053405 | Inhibition of full length human cytosolic carbonic anhydrase-1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates. |
| AID1266232 | Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped flow CO2 dehydration assay | 2016 | Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1 | Inhibition of carbonic anhydrase isoforms I, II, IV, VII and XII with carboxylates and sulfonamides incorporating phthalimide/phthalic anhydride scaffolds. |
| AID1175499 | Inhibition of human recombinant carbonic anhydrase 6 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1308823 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID1183559 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Cyclic tertiary sulfamates: selective inhibition of the tumor-associated carbonic anhydrases IX and XII by N- and O-substituted acesulfame derivatives. |
| AID1470979 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | Synthesis of new 3-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-benzenesulfonamides with strong inhibition properties against the tumor associated carbonic anhydrases IX and XII. |
| AID238221 | Inhibitory constant against human Carbonic anhydrase II | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols. |
| AID256965 | Inhibitory activity against human recombinant mitochondrial isozyme CA VB | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors. |
| AID732714 | Inhibition of human erythrocytes esterase activity of carbonic anhydrase-2 using 4-nitrophenylacetate as substrate after 3 mins by Lineweaver-Burk plot analysis | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Novel sulfamides as potential carbonic anhydrase isoenzymes inhibitors. |
| AID417827 | Inhibition of human recombinant full length CA3 expressed in Escherichia coli BL21 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID299542 | Inhibition of human CA5A | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID1306800 | Inhibition of human recombinant CA2 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Microwave assisted synthesis of novel acridine-acetazolamide conjugates and investigation of their inhibition effects on human carbonic anhydrase isoforms hCA I, II, IV and VII. |
| AID441712 | Inhibition of human recombinant CA7 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1275560 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 9 | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1419398 | Inhibition of carbonic anhydrase 9 (unknown origin) preincubated for 15 mins by stopped flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID1449739 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Inhibition of Malassezia globosa carbonic anhydrase with phenols. |
| AID1756969 | Inhibition of human carbonic anhydrase 2 using p-nitrophenyl acetate as substrate by UV-VIS spectrophotometric analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
| AID315096 | Inhibition of human carbonic anhydrase 1 assessed as 4-nitrophenyl acetate hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID1517550 | Selectivity Index, ratio of Ki for human carbonic anhydrase 9 to Ki for human carbonic anhydrase 2 | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1519764 | Inhibition of recombinant human carbonic anhydrase-12 at 0.01 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID388304 | Antimalarial activity against Plasmodium berghei infected mice (Mus musculus) at 2.5 to 25 mg/kg | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Carbonic anhydrase inhibitors: inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides-in vitro and in vivo studies. |
| AID1183830 | Inhibition of recombinant human carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Selective inhibition of human carbonic anhydrases by novel amide derivatives of probenecid: synthesis, biological evaluation and molecular modelling studies. |
| AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1243115 | Inhibition of human carbonic anhydrase 2 at 10'-6 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID339674 | Inhibition of human recombinant carbonic anhydrase 7 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID475906 | Antibacterial activity against Brucella suis at 100 uM after 8 to 11 days | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides. |
| AID314796 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 10 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID747808 | Inhibition of recombinant human CA2 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID730372 | Inhibition of Flaveria bidentis beta-carbonic anhydrase-1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Kinetic and anion inhibition studies of a β-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis. |
| AID436750 | Selectivity ratio of Ki for human recombinant cytosolic carbonic anhydrase 2 to Ki for human recombinant full length mitochondrial carbonic anhydrase 5A | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
| AID1166264 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel sulfonamides bearing pyrrole and pyrrolopyrimidine moieties as carbonic anhydrase inhibitors: Synthesis, cytotoxic activity and molecular modeling. |
| AID552129 | Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. |
| AID1072626 | Selectivity ratio of Ki for human cytosolic carbonic anhydrase 1 to Ki for human transmembrane carbonic anhydrase 12 | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID1206507 | Inhibition of human recombinant carbonic anhdydrase-1 expressed in Escherichia coli pre-incubated for 6 hrs by stopped-flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | 6-Substituted sulfocoumarins are selective carbonic anhdydrase IX and XII inhibitors with significant cytotoxicity against colorectal cancer cells. |
| AID1470978 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | Synthesis of new 3-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-benzenesulfonamides with strong inhibition properties against the tumor associated carbonic anhydrases IX and XII. |
| AID1172256 | Selectivity index, ratio of Ki for human full length CA2 to Ki for human recombinant CA9 catalytic domain | 2014 | Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22 | Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. |
| AID598730 | Inhibition of Brucella suis carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay at pH 8.3 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID1453374 | Selectivity ratio of IC50 for carbonic anhydrase-1 in human erythrocyte membranes to IC50 for carbonic anhydrase-2 in human erythrocyte membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives. |
| AID1517562 | Inhibition of human carbonic anhydrase 2 at 10'-6 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1459104 | Inhibition of human erythrocyte carbonic anhydrase-1 | |||
| AID1565734 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration at 10'-6 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1460775 | Inhibition of human CA14 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1918140 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 10 mins and measured by phenol red based stopped-flow CO2 hydration assay | |||
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID733597 | Inhibition of human recombinant carbonic anhydrase-2-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | o-Benzenedisulfonimido-sulfonamides are potent inhibitors of the tumor-associated carbonic anhydrase isoforms CA IX and CA XII. |
| AID1301272 | Inhibition of human carbonic anhydrase 1 using saturated CO2 as substrate incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1170172 | Inhibition of human carbonic anhydrase 9 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID166903 | Variation of intraocular pressure in sixth day at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID730889 | Intrinsic thermodynamic binding affinity to carbonic anhydrase 13 (unknown origin) by isothermal titration calorimetry assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Characterization of human carbonic anhydrase XII stability and inhibitor binding. |
| AID316066 | Inhibition of human recombinant full length carbonic hydrase 6 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1262267 | Inhibition of Chionodraco hamatus alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus. |
| AID1564415 | Inhibition of recombinant human CA2 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID314802 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.05 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID48287 | Inhibitory activity against carbonic anhydrase IV from bovine lung microsomes | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX. |
| AID1733131 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 10 mins by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 39 | Synthesis and biological evaluation of novel 4,7-disubstituted coumarins as selective tumor-associated carbonic anhydrase IX and XII inhibitors. |
| AID316064 | Inhibition of human recombinant full length carbonic hydrase 5A by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID25576 | Dissociation constant in water | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides. |
| AID1454029 | Inhibition of recombinant human membrane bound carbonic anhydrase 11 expressed in Escherichia coli pretreated for 15 mins prior to testing by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases. |
| AID1310849 | Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | PEGylated Bis-Sulfonamide Carbonic Anhydrase Inhibitors Can Efficiently Control the Growth of Several Carbonic Anhydrase IX-Expressing Carcinomas. |
| AID446439 | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors. |
| AID1058341 | Inhibition of carbonic anhydrase 2 in human erythrocytes by CO2 hydration-based fluorimetric assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112). |
| AID1534905 | Inhibition of human carbonic anhydrase-12 catalytic domain assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID328979 | Inhibition of human full length carbonic anhydrase 5B | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID588196 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 2 to Ki for Candida albicans recombinant Nce103 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID492419 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Coumarinyl-substituted sulfonamides strongly inhibit several human carbonic anhydrase isoforms: solution and crystallographic investigations. |
| AID1310850 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | PEGylated Bis-Sulfonamide Carbonic Anhydrase Inhibitors Can Efficiently Control the Growth of Several Carbonic Anhydrase IX-Expressing Carcinomas. |
| AID1182977 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Synthesis of sulfonamides with effective inhibitory action against Porphyromonas gingivalis γ-carbonic anhydrase. |
| AID1763381 | Inhibition of human CA9 by stopped-flow assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Developments of small molecules as inhibitors for carbonic anhydrase isoforms. |
| AID1334828 | Inhibition of human recombinant carbonic anhydrase-2 preincubated for 6 hrs by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity. |
| AID1782946 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 9 to Ki for inhibition of recombinant human carbonic anhydrase 2 | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID1852047 | Selectivity index, ratio of Ki for inhibition of recombinant human CA1 to Ki for inhibition of recombinant human CA9 | |||
| AID264311 | Inhibition of human CA2 | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
| AID25354 | Compound was evaluated for pKa | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. |
| AID697240 | Inhibition of human CA1 using 4-nitrophenylacetate as substrate preincubated for 10 mins by spectrophotometric esterase assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. |
| AID238536 | Inhibitory activity against human carbonic anhydrase I (hCAI) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. |
| AID47931 | Inhibition constant (Ki) against human cloned carbonic anhydrase II (CAH) | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
| AID1888318 | Inhibition of recombinant human carbonic anhydrase 7 assessed as inhibition constant preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain. |
| AID436748 | Inhibition of human recombinant full length mitochondrial carbonic anhydrase 5A by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
| AID47898 | Inhibition of human cytosolic isozyme Carbonic anhydrase II at 20 degree C | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
| AID1172253 | Inhibition of human full length CA2 by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22 | Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. |
| AID339669 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1647458 | Inhibition of human carbonic anhydrase 1 using 4-NPA as substrate measured for 3 mins by spectrophotometry | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID1312162 | Inhibition of Flaveria bidentis beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID1520074 | Binding affinity to recombinant human carbonic anhydrase 7 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1703323 | Inhibition of human CA9 incubated for 15 mins by stopped- flow CO2 hydrase assay method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Discovery of first-in-class multi-target adenosine A |
| AID1731032 | Inhibition of human CAH9 catalytic domain expressed in Escherichia coli BL21 (DE3) assessed as reduction in esterase activity using p-nitrophenyl acetate substrate by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID315088 | Inhibition of human carbonic anhydrase 1 by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID441212 | Apparent effective permeability by PAMPA method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID732713 | Binding affinity to human recombinant CA1 at 37 degC and pH 7.0 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | 4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII. |
| AID1173859 | Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | 4-Functionalized 1,3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of carbonic anhydrase isoforms hCA I, II, IX and XII. |
| AID1852042 | Inhibition of recombinant human CA4 pre-incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1456318 | Inhibition of Vibrio cholerae beta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Synthesis and human/bacterial carbonic anhydrase inhibition with a series of sulfonamides incorporating phthalimido moieties. |
| AID1237483 | Growth inhibition of Pseudomonas aeruginosa PAO1 assessed as reduction in growth rate and yield at 100 and 200 uM after 4 hrs | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID271712 | Inhibition of human cloned CA9 catalytic domain by CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". |
| AID1175503 | Inhibition of human recombinant carbonic anhydrase 13 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1419421 | Cytotoxicity against human HT-29 cells assessed as cell viability at 100 uM after 48 hrs under normoxic conditions by MTT assay (Rvb = 100%) | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID48280 | Inhibitory activity against bovine carbonic anhydrase isozyme IV isolated from bovine lung microsomes, by esterase assay method. | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides. |
| AID437754 | Ratio of Kcat to Km human recombinant CA1 by stopped-flow hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID367614 | Inhibition of human recombinant full length CA6 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367614 | Inhibition of human recombinant full length CA6 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1245669 | Inhibition of carbonic anhydrase-7 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1266234 | Inhibition of human carbonic anhydrase-7 preincubated for 15 mins by stopped flow CO2 dehydration assay | 2016 | Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1 | Inhibition of carbonic anhydrase isoforms I, II, IV, VII and XII with carboxylates and sulfonamides incorporating phthalimide/phthalic anhydride scaffolds. |
| AID1607535 | Inhibition of human recombinant carbonic anhydrase 2 preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID382964 | Solubility in water in presence of 0.0302 mol/l hydroxypropyl-beta-cyclodextrin and 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1061038 | Inhibition of human mitochondrial CA5A preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID428372 | Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1292253 | Inhibition of human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate by Lineweaver-Burk plot analysis | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. |
| AID131557 | Protective dose against maximal electroshock in mice after peroral administration | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides. |
| AID28907 | Partition coefficient (logD) (chloroform/buffer) | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID512001 | Inhibition of human cloned CA1 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID512001 | Inhibition of human cloned CA1 after 15 mins by stopped-flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1185164 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for Vibrio cholerae cytosolic carbonic anhydrase | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae. |
| AID1061066 | Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii. |
| AID1373188 | Acid ionization constant, pKa of sulfonamide group of the compound by NMR chemical shift based method | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID301571 | Activity of human recombinant CA 2 assessed as CO2 hydration | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID238316 | Ki value against human carbonic anhydrase XII (hCA XII) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? |
| AID293193 | Inhibition of human recombinant CA12 by CO2 hydration assay | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides. |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1303400 | Selectivity ratio, ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID427123 | Inhibition of Cryptococcus neoformans recombinant Can2 by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID415830 | Inhibition of human CA2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors. |
| AID1460776 | Inhibition of mouse CA15 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID462273 | Inhibition of human CA4 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1061039 | Inhibition of human CA3 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1453410 | Inhibition of Francisella tularensis beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | |||
| AID1060767 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors. |
| AID620642 | Cytotoxicity against chinese hamster PS120 cells expressing CA9 assessed as cell viability at 30 uM and pH 6.4 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID650296 | Inhibition of human carbonic anhydrase 9 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases. |
| AID1272997 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID623072 | Inhibition of recombinant carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis of glycoconjugate carbonic anhydrase inhibitors by ruthenium-catalysed azide-alkyne 1,3-dipolar cycloaddition. |
| AID1182979 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Synthesis of sulfonamides with effective inhibitory action against Porphyromonas gingivalis γ-carbonic anhydrase. |
| AID441210 | Selectivity for human cloned CA9 over human cloned CA1 | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases. |
| AID1859986 | Inhibition of human carbonic anhydrase 12 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide derivatives utilizing tail/dual-tail approaches as novel carbonic anhydrase inhibitors. |
| AID1571209 | Inhibition of recombinant human carbonic anhydrase-2 expressed in Escherichia coli incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies. |
| AID165491 | Reduction in maximum Intra ocular pressure in the rabbit model of ocular hypertension, when treated with a minimum effective oral dose of 10 mg/Kg; NE is No Effect | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity. |
| AID761313 | Inhibition of human cytosolic carbonic anhydrase 1 after 6 hrs by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | 7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors. |
| AID1852050 | Selectivity index, ratio of Ki for inhibition of recombinant human CA2 to Ki for inhibition of recombinant human CA12 | |||
| AID347430 | Inhibition of human recombinant CA9 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. |
| AID743514 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides. |
| AID254246 | Inhibitory activity against catalytic domain of human cloned Carbonic anhydrase IX by the CO2 hydration method | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides. |
| AID371703 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 by by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273. |
| AID714400 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Anion inhibition studies of the fastest carbonic anhydrase (CA) known, the extremo-CA from the bacterium Sulfurihydrogenibium azorense. |
| AID1278564 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow carbon dioxide hydrase assay | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII. |
| AID238409 | Inhibition constant against human carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes. |
| AID1170157 | Inhibition of human CA-1 by stopped flow CO2 hydrase assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | A class of 4-sulfamoylphenyl-ω-aminoalkyl ethers with effective carbonic anhydrase inhibitory action and antiglaucoma effects. |
| AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID603448 | Inhibition of human full length cytosolic isoform of carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID238769 | Inhibitory activity against Carbonic anhydrase IX | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1434430 | Inhibition of Vibrio cholerae Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | |||
| AID1461935 | Inhibition of Burkholderia pseudomallei beta-CA incubated for 15 mins by stopped-flow CO2 hydration assay | |||
| AID239422 | Inhibitory potency against catalytic domain of human Carbonic anhydrase IX expressed in Escherichia coli strain BL21 | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX. |
| AID1691506 | Selectivity ratio of Ki for inhibition of recombinant human CA2 to Ki for inhibition of recombinant human CA9 | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID1717280 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Sulfonamide/sulfamate switch with a series of piperazinylureido derivatives: Synthesis, kinetic and in silico evaluation as carbonic anhydrase isoforms I, II, IV, and IX inhibitors. |
| AID1238811 | Selectivity ratio of Ki for human recombinant CA2 to Ki for human recombinant CA12 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID1238453 | Selectivity ratio of Ki for human carbonic anhydrase-2 to Ki for human carbonic anhydrase-9 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1303395 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 min to 72 hrs by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID21971 | Tested for solubility in pH 7.4 buffer, at 25 Degree C | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID1849600 | Inhibition of human CA2 using 4-nitrophenylacetate as substrate incubated for 10 mins prior to testing by spectrophotometry based esterase assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1275913 | Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae. |
| AID1168852 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Structural insights on carbonic anhydrase inhibitory action, isoform selectivity, and potency of sulfonamides and coumarins incorporating arylsulfonylureido groups. |
| AID1238805 | Inhibition of human recombinant CA2 expressed in Escherichia coli by stopped flow CO2 hydration assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates. |
| AID1170184 | Inhibition of human carbonic anhydrase 13 at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID761312 | Inhibition of human cytosolic carbonic anhydrase 2 after 6 hrs by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | 7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors. |
| AID616467 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID1312155 | Inhibition of Candida glabrata beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID1238448 | Inhibition of human carbonic anhydrase-2 incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1193931 | Inhibition of oxaliplatin-induced neuropathic pain in CD-1 mouse model assessed as latency to pain-related behavior at 100 mg/kg, po after 15 mins by cold plate test | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID474209 | Inhibition of human recombinant CA9 by stopped flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID514210 | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity. |
| AID1902659 | Selectivity ratio of Ki for for inhibition of recombinant human CA 2 to Ki for inhibition of recombinant human CA 12 | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID1518851 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID427126 | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase method | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID314791 | Inhibition of human carbonic anhydrase 9 in presence of 0.25 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID441713 | Inhibition of human recombinant CA9 by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1755849 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID620655 | Inhibition of human CA9 expressed in chinese hamster PS120 cells assessed as reduction in rate of extracellular acidification in response to CO2-load at 60 uM after 30 mins | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1170180 | Inhibition of human carbonic anhydrase 7 at pH7 and 37 degC by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID775829 | Inhibition of mushroom tyrosinase assessed as L-DOPA conversion to melanin at 10 uM preincubated for 10 mins prior to substrate addition measured after 10 mins by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID1723530 | Inhibition of human carbonic anhydrase 13 expressed in Escherichia coliBL21(DE3) pLysS incubated for 10 mins by phenol red dye based assay | |||
| AID238772 | Binding affinity towards human cloned carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. |
| AID714402 | Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 alpha-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Anion inhibition studies of the fastest carbonic anhydrase (CA) known, the extremo-CA from the bacterium Sulfurihydrogenibium azorense. |
| AID48736 | Mortality of animals recorded as the number of animals dead out of the total animals (16) taken for the study at dose 1 mg/kg given q.i.d. | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID1518950 | Inhibition of recombinant human carbonic anhydrase 9 at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1180163 | Inhibition of CA-9 (unknown origin) after 15 mins by CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors. |
| AID1245672 | Inhibition of carbonic anhydrase-6 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1809974 | Selectivity ratio of IC50 for inhibition of recombinant human CA1 to IC50 for inhibition of recombinant human CA2 using 4-nitrophenylacetate as substrate by esterase assay | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID1689403 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay to Ki for recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID484215 | Inhibition of human carbonic anhydrase 9 | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors. |
| AID195089 | Inhibitor level was measured in red blood cells at 30 min after exposure of 10 mL of blood to solutions by HPLC method | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID620651 | Reduction in CA9 mRNA level in ca9/ca12 double silenced human LS 174T cells under hypoxia at 60 uM after 48 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1237871 | Selectivity ratio of Ki for human alpha-carbonic anhydrase 1 to Ki for Leishmania donovani chagasi beta-carbonic anhydrase | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID299233 | Ratio of kcat to Km of human CA1 | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID411396 | Inhibition of Saccharomyces cerevisiae carbonic anhydrase by oxygen-18 isotope exchange assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with anions. |
| AID1058395 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID1570385 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by phenol red staining-based stopped flow CO2 hydrase assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure. |
| AID48124 | Inhibitory activity against carbonic anhydrase isolated from bovine lung microsome (bCA IV) | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. |
| AID1692246 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII. |
| AID320310 | Inhibition of human recombinant full length carbonic hydrase 5B by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID589730 | Inhibition of Candida albicans Nce103 beta-carbonic anhydrase by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. |
| AID780325 | Inhibition of human carbonic anhydrase2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID484163 | Inhibition of human carbonic anhydrase 12 catalytic domain preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID299539 | Inhibition of human CA2 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID486935 | Inhibition of human cloned carbonic anhydrase 12 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID486935 | Inhibition of human cloned carbonic anhydrase 12 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1736569 | Selectivity index, ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 9 | |||
| AID382977 | Solubility in water in presence of 0.34 M triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID732026 | Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Carbonic anhydrase inhibitors: benzenesulfonamides incorporating cyanoacrylamide moieties are low nanomolar/subnanomolar inhibitors of the tumor-associated isoforms IX and XII. |
| AID382970 | Solubility in water in presence of 0.334 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID371706 | Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273. |
| AID1849586 | Inhibition of human CA1 using 4-nitrophenylacetate as substrate by spectrophotometrical analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID349607 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. |
| AID1504904 | Inhibition of recombinant human carbonic anhydrase 7 incubated for 15 mins by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors. |
| AID526861 | Binding affinity to human recombinant carbonic anhydrase 2 by thermal shift assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID382952 | Solubility in water in presence of 0.0755 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID761309 | Inhibition of human transmembrane carbonic anhydrase 12 after 6 hrs by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | 7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors. |
| AID1269931 | Inhibition of Colwellia psychrerythraea gamma carbonic anhydrase expressed in Escherichia coli incubated for 15 mins prior to testing by stopped flow CO2 hydration method | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Cloning, characterization and anion inhibition studies of a γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID1442645 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID1170168 | Inhibition of human carbonic anhydrase 5A at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1555970 | Inhibition of human carbonic anhydrase 13 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID600783 | Activity at human carbonic anhydrase 2 assessed as hydrolysis of p- nitrophenyl acetate at 0.3 umol/L at pH 7.6 | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Synthesis and evaluation of new carbonic anhydrase inhibitors. |
| AID1564425 | Inhibition of recombinant human CA2 at 10'-6 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID305489 | Inhibition of human recombinant CA9 catalytic domain by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions. |
| AID1593066 | Inhibition of full length human CA 2 | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines. |
| AID758952 | Inhibition of human recombinant CA2 by CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14 | A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules. |
| AID537658 | Inhibition of human carbonic anhydrase 1 esterase activity by spectrophotometry | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID1519759 | Inhibition of recombinant human carbonic anhydrase-9 at 1 nM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1306531 | Inhibition of Methanosarcina thermophila gamma carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1555964 | Inhibition of human carbonic anhydrase 5A incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID775828 | Inhibition of TPCK-treated trypsin (unknown origin) at 10 uM preincubated for 10 mins prior to substrate addition measured for 30 mins by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID1462734 | Inhibition of human CA1 pre-incubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Synthesis and carbonic anhydrase inhibition of polycyclic imides incorporating N-benzenesulfonamide moieties. |
| AID1581515 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID314780 | Inhibition of human carbonic anhydrase 2 in presence of 0.01 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID669115 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1518923 | Inhibition of recombinant human carbonic anhydrase 1 at 10 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1769574 | Inhibition of recombinant human CA1 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold. |
| AID238309 | Inhibitory activity against human Carbonic anhydrase I | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Carbonic anhydrase inhibitors: the first on-resin screening of a 4-sulfamoylphenylthiourea library. |
| AID347432 | Selectivity ratio of Ki for human CA2 to Ki for human CA9 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. |
| AID254244 | Inhibitory activity against human Carbonic anhydrase IX (hCA IX) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. |
| AID387190 | Inhibition of Cryptococcus neoformans Can2 at 20 degC by CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions. |
| AID300754 | Inhibition of human recombinant CA1 by CO2 hydration stopped flow assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID1238077 | Inhibition of human carbonic anhydrase-9 | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII. |
| AID1379159 | Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino) benzenesulfonamides: Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular modelling studies. |
| AID301523 | Inhibition of catalytic domain of human cloned carbonic anhydrase9 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2-thione derivatives with carbonic anhydrase inhibitory activity. |
| AID697241 | Inhibition of human recombinant CA12 catalytic domain preincubated for 15 mins by stopped-flow CO2 hydration assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. |
| AID620646 | Reduction of intracellular pH in chinese hamster PS120 cells expressing CA9 at 60 uM and pH 6.4 after 30 mins by weak acid [7-14C]-benzoic acid distribution technique | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1464261 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase-1 to Ki for human recombinant carbonic anhydrase-9 | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID1175494 | Inhibition of human recombinant carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1140120 | Inhibition of human carbonic anhydrase 2-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity. |
| AID1565767 | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | From random to rational: A discovery approach to selective subnanomolar inhibitors of human carbonic anhydrase IV based on the Castagnoli-Cushman multicomponent reaction. |
| AID1520086 | Binding affinity to recombinant human carbonic anhydrase 7 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID493885 | Inhibition of human recombinant carbonic anhydrase 3 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1731028 | Inhibition of human CAH12 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1242663 | Inhibition of human recombinant carbonic anhydrase-9 catalytic domain by stopped-flow CO2 hydration assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. |
| AID437755 | Ratio of Kcat to Km human recombinant CA2 by stopped-flow hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID1888319 | Inhibition of recombinant human carbonic anhydrase 9 assessed as inhibition constant preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain. |
| AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1273002 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 12 to Ki for recombinant human carbonic anhydrase 7 | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID610545 | Inhibition of human recombinant carbonic anhydrase 13 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1758423 | Inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides. |
| AID1373176 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 1 (3 to 261 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1603060 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors. |
| AID610546 | Inhibition of Candida albicans Carbonic anhydrase preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1256863 | Inhibition of human carbonic anhydrase-14 assessed as CO2 hydration activity by stopped-flow method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID1254029 | Inhibition of Vibrio cholerae alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID1435063 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 10 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5 | Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID48090 | Inhibitory activity against human carbonic anhydrase II (hCA II) by using esterase assay method | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design. |
| AID275812 | Inhibition of human mitochondrail isozyme CA VA | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID315097 | Inhibition of human carbonic anhydrase 2 assessed as 4-nitrophenyl acetate hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID1655937 | Inhibition of recombinant human carbonic anhydrase 12 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer. |
| AID1239229 | Inhibition of human recombinant carbonic anhydrase-12 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties. |
| AID714401 | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Anion inhibition studies of the fastest carbonic anhydrase (CA) known, the extremo-CA from the bacterium Sulfurihydrogenibium azorense. |
| AID1308825 | Inhibition of human recombinant carbonic anhydrase 5A expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID50345 | Inhibitory activity against human carbonic anhydrase I was determined | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID1275558 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID749808 | Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID1628037 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17 | Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum. |
| AID327763 | Inhibition of human full length carbonic anhydrase 5B by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID243118 | Ratio of Kcat/Km against mouse carbonic anhydrase XIII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID749805 | Inhibition of human carbonic anhydrase-12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID239220 | Inhibitory constant value for Carbonic anhydrase II in human determined in pH-shift assay | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform. |
| AID1335043 | Inhibition of human erythrocyte carbonic anhydrase 2 preincubated for 15 mins prior to testing by bromothymol blue-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Dithiocarbamates effectively inhibit the β-carbonic anhydrase from the dandruff-producing fungus Malassezia globosa. |
| AID1170175 | Inhibition of chimeric carbonic anhydrase 12 (unknown origin) expressing with full length CA2 (1 to 260) at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID669119 | Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1555961 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID732715 | Inhibition of human erythrocytes esterase activity of carbonic anhydrase-1 using 4-nitrophenylacetate as substrate after 3 mins by Lineweaver-Burk plot analysis | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Novel sulfamides as potential carbonic anhydrase isoenzymes inhibitors. |
| AID1072628 | Selectivity ratio of Ki for human cytosolic carbonic anhydrase 1 to Ki for human transmembrane carbonic anhydrase 9 | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID239703 | Inhibitory constant against human carbonic anhydrase XIV in CO2 hydrase assay | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. |
| AID314829 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 1.00 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID537656 | Inhibition of human carbonic anhydrase 1 by Lineweaver-Burke plot analysis | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide. |
| AID588186 | Inhibition of human recombinant alpha-carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1782942 | Inhibition of recombinant human carbonic anhydrase 4 by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID238928 | Inhibitory constant against cytosolic human Carbonic anhydrase II using CO2 hydrase assay | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. |
| AID299546 | Inhibition of human CA9 catalytic domain | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15 | Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies. |
| AID1230148 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies. |
| AID464118 | Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies. |
| AID1753388 | Inhibition of recombinant human CA9 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities. |
| AID437752 | Activity at human recombinant CA2 by stopped-flow hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID1195371 | Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides. |
| AID588193 | Selectivity ratio of Ki for human recombinant alpha-carbonic anhydrase 1 to Ki for Cryptococcus neoformans recombinant Can2 beta-carbonic anhydrase | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1173860 | Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | 4-Functionalized 1,3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of carbonic anhydrase isoforms hCA I, II, IX and XII. |
| AID603070 | Inhibition of human recombinant cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Conformational variability of different sulfonamide inhibitors with thienyl-acetamido moieties attributes to differential binding in the active site of cytosolic human carbonic anhydrase isoforms. |
| AID1373178 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1849564 | Binding affinity to human CA9 assessed as inhibition constant by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID464216 | Inhibition of human carbonic anhydrase 2 assessed as conversion of 4-nitrophenyl acetate to 4-nitrophnolate after 5 mins | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Synthesis and investigation of inhibition effect of fluorinated sulfonamide derivatives on carbonic anhydrase. |
| AID1808985 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID1152900 | Inhibition of human recombinant carbonic anhydrase 2 pretreated for 15 mins by stopped flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12 | Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors. |
| AID1172254 | Inhibition of human recombinant CA9 catalytic domain by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22 | Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. |
| AID764497 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Inhibition of tumor-associated human carbonic anhydrase isozymes IX and XII by a new class of substituted-phenylacetamido aromatic sulfonamides. |
| AID1649850 | Inhibition of human CA1 preincubated for 15 mins by stopped-flow carbon dioxide hydration assay | |||
| AID1849563 | Binding affinity to human CA2 assessed as inhibition constant by stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID47743 | Activity against human carbonic anhydrase II | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides. |
| AID620690 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 12 catalytic domain | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID1570353 | Inhibition of recombinant human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Carbonic anhydrase inhibitors based on sorafenib scaffold: Design, synthesis, crystallographic investigation and effects on primary breast cancer cells. |
| AID382965 | Solubility in water in presence of 0.0604 mol/l hydroxypropyl-beta-cyclodextrin and 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1469006 | Binding affinity to human N-terminal full length His-tagged CA13 (1 to 262 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic thermodynamic equilibrium constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1518852 | Inhibition of recombinant human carbonic anhydrase 9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID456398 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Carbonic anhydrase inhibitors. Identification of selective inhibitors of the human mitochondrial isozymes VA and VB over the cytosolic isozymes I and II from a natural product-based phenolic library. |
| AID492420 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Coumarinyl-substituted sulfonamides strongly inhibit several human carbonic anhydrase isoforms: solution and crystallographic investigations. |
| AID272524 | Inhibition of human cloned CA5B by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID614107 | Inhibition of human cloned carbonic anhydrase 9 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Carbonic anhydrase inhibitors. Synthesis, molecular structures, and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with novel 3-pyridinesulfonamide derivatives. |
| AID307889 | Inhibition of human CA5B by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID339679 | Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1309028 | Inhibition of Malassezia globosa beta carbonic anhydrase preincubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | N-Nitrosulfonamides: A new chemotype for carbonic anhydrase inhibition. |
| AID1301273 | Inhibition of human carbonic anhydrase 2 using saturated CO2 as substrate incubated for 10 mins prior to testing by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII. |
| AID1655151 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 1 preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for recombinant human carbonic anhydrase 2 preincubated with enzyme for 10 mins b | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1689400 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID764565 | Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | 5-Substituted-(1,2,3-triazol-4-yl)thiophene-2-sulfonamides strongly inhibit human carbonic anhydrases I, II, IX and XII: solution and X-ray crystallographic studies. |
| AID1336565 | Inhibition of human recombinant carbonic anhydrase-4 using CO2 as substrate preincubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors. |
| AID497127 | Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors. |
| AID496922 | Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID614106 | Inhibition of human cloned carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Carbonic anhydrase inhibitors. Synthesis, molecular structures, and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with novel 3-pyridinesulfonamide derivatives. |
| AID93581 | Level in red blood cells after incubation of human erythrocytes for 30 min, was determined by HPLC method | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX. |
| AID1278996 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6 | Development of 3-(4-aminosulphonyl)-phenyl-2-mercapto-3H-quinazolin-4-ones as inhibitors of carbonic anhydrase isoforms involved in tumorigenesis and glaucoma. |
| AID1753386 | Inhibition of recombinant human CA1 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities. |
| AID328982 | Inhibition of human catalytic domain carbonic anhydrase 9 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID1849567 | Binding affinity to human CA2 assessed as inhibition constant using 4-nitrophenylacetate as substrate by spectrophotometrical analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1275555 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1461804 | Inhibition of human CA9 | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | 1,3-Oxazole-based selective picomolar inhibitors of cytosolic human carbonic anhydrase II alleviate ocular hypertension in rabbits: Potency is supported by X-ray crystallography of two leads. |
| AID1879880 | Inhibition of human recombinant carbonic anhydrase 9 assessed as inhibition constant incubated for 10 mins by phenol red dye based stopped-flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID646244 | Inhibition of human recombinant carbonic anhydrase 3 hydrolysis activity using 4-nitrophenyl acetate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID1442647 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. |
| AID408471 | Inhibition of human cloned CA9 catalytic domain by stopped flow CO2 hydration assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII. |
| AID1239227 | Inhibition of human recombinant carbonic anhydrase-2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties. |
| AID1763378 | Inhibition of human CA1 by stopped-flow assay | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | Developments of small molecules as inhibitors for carbonic anhydrase isoforms. |
| AID1902653 | Inhibition of recombinant human CA 2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID1585350 | Inhibition of recombinant human carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID733598 | Inhibition of human recombinant carbonic anhydrase-1-mediated CO2 hydration preincubated for 10 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | o-Benzenedisulfonimido-sulfonamides are potent inhibitors of the tumor-associated carbonic anhydrase isoforms CA IX and CA XII. |
| AID428371 | Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1707342 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors. |
| AID1818557 | Inhibition of human CA4 incubated for 15 mins prior to testing by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | 2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity. |
| AID1304444 | Inhibition of human recombinant CA9 preincubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Synthesis of 4-(thiazol-2-ylamino)-benzenesulfonamides with carbonic anhydrase I, II and IX inhibitory activity and cytotoxic effects against breast cancer cell lines. |
| AID1062685 | Inhibition of human CA9 after 15 mins by stopped-flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associat |
| AID261582 | Selectivity ratio for human carbonic anhydrase 2 over Helicobacter pylori carbonic anhydrase | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. |
| AID1243109 | Inhibition of human carbonic anhydrase 1 at 10'-8 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID461089 | Inhibition of hydratase-activity of human erythrocytes CA2 by CO2-hydration method | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. |
| AID428369 | Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1519752 | Inhibition of recombinant human carbonic anhydrase-1 at 0.1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID238574 | Inhibitory activity against human carbonic anhydrase II (hCAII) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. |
| AID1072627 | Selectivity ratio of Ki for human cytosolic carbonic anhydrase 2 to Ki for human transmembrane carbonic anhydrase 9 | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID1183560 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Cyclic tertiary sulfamates: selective inhibition of the tumor-associated carbonic anhydrases IX and XII by N- and O-substituted acesulfame derivatives. |
| AID1560586 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 9 to Ki for recombinant human carbonic anhydrase 12 | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID1731038 | Inhibition of CAH2 in human UFH-001 cells at 1 uM by membrane inlet for mass spectrometry | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID238227 | Inhibitory constant against human Carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds. |
| AID1422966 | Inhibition of recombinant human CA5a preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID272525 | Inhibition of human cloned CA7 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1196823 | Inhibition of recombinant human carbonic anhydrase 1 by CO2 hydration assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Carbonic anhydrase inhibitors with dual-tail moieties to match the hydrophobic and hydrophilic halves of the carbonic anhydrase active site. |
| AID1275564 | Inhibition of human carbonic anhydrase-2 using p-nitrophenyl acetate as substrate by esterase assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID238326 | Ki value against mouse carbonic anhydrase VII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID660367 | Inhibition of human CA9 pre-incubated for 15 mins by stopped-flow CO2 hydration method | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo. |
| AID1166968 | Inhibition of human CA-2 after 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Inhibition of carbonic anhydrase isoforms I, II, IX and XII with novel Schiff bases: identification of selective inhibitors for the tumor-associated isoforms over the cytosolic ones. |
| AID47899 | In vitro inhibitory activity against human carbonic anhydrase II (hCAII) | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | Carbonic anhydrase inhibitors: synthesis and topical intraocular pressure lowering effects of fluorine-containing inhibitors devoid of enhanced reactivity. |
| AID539003 | Inhibition of human chitinase | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Acetazolamide-based fungal chitinase inhibitors. |
| AID1185161 | Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae. |
| AID1314076 | Inhibition of human CA2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis 4-[2-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-ethyl]-benzenesulfonamides with subnanomolar carbonic anhydrase II and XII inhibitory properties. |
| AID1266246 | Inhibition of human carbonic anhydrase-9 preincubated for 15 mins by stopped flow CO2 dehydration method | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies. |
| AID411529 | Inhibition of human recombinant CA3 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411529 | Inhibition of human recombinant CA3 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID623071 | Inhibition of recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis of glycoconjugate carbonic anhydrase inhibitors by ruthenium-catalysed azide-alkyne 1,3-dipolar cycloaddition. |
| AID26085 | pKa of the compound was determined | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides. |
| AID759699 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins to 6 hrs by CO2 hydration stopped-flow assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | A class of sulfonamides with strong inhibitory action against the α-carbonic anhydrase from Trypanosoma cruzi. |
| AID493892 | Inhibition of human recombinant carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1234501 | Inhibition of human carbonic anhydrase 9 by by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Design and synthesis of benzothiazole-6-sulfonamides acting as highly potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII. |
| AID1491571 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | |
| AID388306 | Inhibition of Plasmodium falciparum recombinant carbonic anhydrase | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Carbonic anhydrase inhibitors: inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides-in vitro and in vivo studies. |
| AID1652407 | Inhibition of human CA12 pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID47908 | Dissociation constant against human Carbonic anhydrase II (HCA II) | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Identification of two hydrophobic patches in the active-site cavity of human carbonic anhydrase II by solution-phase and solid-state studies and their use in the development of tight-binding inhibitors. |
| AID775845 | Inhibition of human carbonic anhydrase 2 assessed as p-nitrophenyl acetate conversion to p-nitrophenolate anion preincubated for 10 mins prior to substrate addition measured for 20 mins by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Investigating the selectivity of metalloenzyme inhibitors. |
| AID299241 | Ratio of kcat to Km of Helicobacter pylori beta CA | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1446114 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 300 uM after 48 hrs under hypoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1466465 | Inhibition of recombinant human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII. |
| AID238438 | Inhibition constant against human carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes. |
| AID441710 | Inhibition of human recombinant CA5B by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID23539 | Solubility (in uM) in pH 7.40 at 25 degree C | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID1188137 | Inhibition of Porphyromonas gingivalis Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes. |
| AID438011 | Inhibition of human full length membrane-bound carbonic anhydrase 14 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1519756 | Inhibition of recombinant human carbonic anhydrase-2 at 0.01 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1314075 | Inhibition of human CA1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis 4-[2-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-ethyl]-benzenesulfonamides with subnanomolar carbonic anhydrase II and XII inhibitory properties. |
| AID526862 | Binding affinity to human recombinant carbonic anhydrase 2 by isothermal titration calorimetry assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID1357959 | Cytotoxicity against human HT-29 cells after 96 hrs under normoxic condition by MTT assay | |||
| AID1873666 | Inhibition of recombinant human carbonic anhydrase 9 assessed as inhibition constant incubated for 1 hr prior to testing by phenol red based stopped-flow CO2 hydration assay | 2022 | Bioorganic & medicinal chemistry, 08-01, Volume: 67 | Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation. |
| AID552784 | Inhibition of Cryptococcus neoformans carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Inhibition of the β-carbonic anhydrase from Streptococcus pneumoniae by inorganic anions and small molecules: Toward innovative drug design of antiinfectives? |
| AID1350478 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
| AID417825 | Inhibition of human recombinant full length CA1 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1161955 | Inhibition of Legionella pneumophila carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID1520077 | Binding affinity to recombinant human carbonic anhydrase 13 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID48294 | Inhibitory activity against human carbonic anhydrase IX was determined | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID1142837 | Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-2 assessed as CO2 hydrase activity by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11 | Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID1166967 | Inhibition of human CA-1 after 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Inhibition of carbonic anhydrase isoforms I, II, IX and XII with novel Schiff bases: identification of selective inhibitors for the tumor-associated isoforms over the cytosolic ones. |
| AID1336988 | Inhibition of recombinant human membrane bound carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID1633347 | Inhibition of Trypanosoma cruzi carbonic anhydrase preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1517560 | Inhibition of human carbonic anhydrase 2 at 10'-8 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1660014 | Inhibition of human carbonic anhydrase 2 assessed as inhibitory constant incubated for 6 hrs by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID311028 | Inhibition of human carbonic anhydrase 5B | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1330454 | Inhibition of human full length carbonic anhydrase 2 | |||
| AID1519757 | Inhibition of recombinant human carbonic anhydrase-2 at 0.1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID1597784 | Inhibition of human recombinant N-His-tagged carbonic anhydrase 11 expressed in HEK293T cells using p-nitrophenyl acetate as substrate measured after 30 mins by colorimetric analysis | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17 | Sulfonate and sulfamate derivatives possessing benzofuran or benzothiophene nucleus as potent carbonic anhydrase II/IX/XII inhibitors. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID242853 | Kcat value against mouse carbonic anhydrase XIII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1739499 | Inhibition of human CA12 by stopped-flow carbon dioxide hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases. |
| AID456399 | Inhibition of human recombinant carbonic anhydrase 5A by stopped flow CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Carbonic anhydrase inhibitors. Identification of selective inhibitors of the human mitochondrial isozymes VA and VB over the cytosolic isozymes I and II from a natural product-based phenolic library. |
| AID587131 | Inhibition of human carbonic anhydrase 2 after 15 mins by CO2 hydrase assay at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID1190063 | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum. |
| AID1255571 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli preincubated for 6 hrs by stopped flow CO2 hydrase assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Isatin-pyrazole benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID441709 | Inhibition of human recombinant CA5A by stopped flow CO2 hydrase assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. |
| AID1518853 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID620643 | Cytotoxicity against chinese hamster PS120 cells expressing CA9 assessed as cell viability at 60 uM and pH 6.4 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1193930 | Inhibition of oxaliplatin-induced neuropathic pain in po dosed CD-1 mouse model assessed as latency to pain-related behavior after 15 to 45 mins by cold plate test | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID1275631 | Inhibition of human carbonic anhydrase 12 for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Kinetic and X-ray crystallographic investigations on carbonic anhydrase isoforms I, II, IX and XII of a thioureido analog of SLC-0111. |
| AID600784 | Antihypoxic activity in fasted Kunming mouse assessed as survival time of mouse under hypoxic condition at 80 mg/kg administered for 5 days (Rvb = 2199 +/-217 secs) | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Synthesis and evaluation of new carbonic anhydrase inhibitors. |
| AID436564 | Inhibition of human recombinant CA2 by stopped-flow CO2 assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. |
| AID603454 | Selectivity ratio of Ki for human full length cytosolic isoform of carbonic anhydrase 2 to Ki for human recombinant catalytic domain of carbonic anhydrase 9 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1706621 | Inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID316063 | Inhibition of human recombinant full length carbonic hydrase 4 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID461322 | Inhibition of esterase-activity of CA1 from human erythrocytes by spectrophotometry | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. |
| AID731403 | Inhibition of human carbonic anhydrase 9 preincubated for 10 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | New selective carbonic anhydrase IX inhibitors: synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides. |
| AID1347711 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydration assay | |||
| AID644036 | Inhibition of human carbonic anhydrase 4 esterase activity using 4-nitrophenylacetate as substrate | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives. |
| AID428459 | Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1373167 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 4 expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1312160 | Inhibition of Mycobacterium tuberculosis beta-carbonic anhydrase Rv3588 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID413965 | Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates. |
| AID1306838 | Inhibition of human carbonic anhydrase 9 catalytic domain preincubated for 6 hrs at 4 degC measured for 10 to 100 secs by stopped-flow carbon dioxide hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1,6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors. |
| AID48282 | Inhibitory activity against bovine carbonic anhydrase IV from lung microsomes | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1234861 | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | 5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII. |
| AID438004 | Inhibition of human full length mitochondrial carbonic anhydrase 5A after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID1162890 | Inhibition of Vibrio cholerae alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | Quinazoline-sulfonamides with potent inhibitory activity against the α-carbonic anhydrase from Vibrio cholerae. |
| AID1170186 | Inhibition of human carbonic anhydrase 2 at pH7 and 25 degC by stopped-flow kinetic inhibition assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID1158138 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties. |
| AID1291091 | Inhibition of recombinant human carbonic anhydrase 1 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID1427078 | Inhibition of human recombinant carbonic anhydrase 7 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies. |
| AID314804 | Inhibition of human carbonic anhydrase 2 in presence of 0.10 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID314816 | Inhibition of human carbonic anhydrase 2 in presence of 0.01 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1306802 | Inhibition of human recombinant membrane bound CA7 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Microwave assisted synthesis of novel acridine-acetazolamide conjugates and investigation of their inhibition effects on human carbonic anhydrase isoforms hCA I, II, IV and VII. |
| AID1194925 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of a new series of dithiocarbamates with effective human carbonic anhydrase inhibitory activity and antiglaucoma action. |
| AID1204093 | Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-2 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-9 | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1571210 | Selectivity ratio of IC50 for human erythrocyte carbonic anhydrase-1 to IC50 for human carbonic anhydrase-9 | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies. |
| AID314763 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.01 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1188769 | Inhibition of bovine erythrocyte carbonic anhydrase 2 using 4-nitrophenyl acetate substrate by photometric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Sulfamates of methyl triterpenoates are effective and competitive inhibitors of carbonic anhydrase II. |
| AID382956 | Solubility in NaOH-NaHCO3 buffer at pH 9.57 in presence of 0.0226 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1062684 | Inhibition of human CA12 after 15 mins by stopped-flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associat |
| AID1133326 | Induction of diuretic activity in po dosed rat assessed as increase in urine output after 4 hrs | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides. |
| AID166746 | Variation of intraocular pressure in day one at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID1517241 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration incubated for 1 hr by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID299236 | Ratio of kcat to Km of human CA5A | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID275814 | Inhibition of catalytic domain of human CA XII | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID1460765 | Inhibition of human CA2 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID1726080 | Inhibition of Vibrio cholerae alpha carbonic anhydrase pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in |
| AID1518936 | Inhibition of recombinant human carbonic anhydrase 12 assessed as residual activity at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID367821 | Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates. |
| AID1336564 | Inhibition of human recombinant carbonic anhydrase-2 using CO2 as substrate preincubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors. |
| AID1456315 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Synthesis and human/bacterial carbonic anhydrase inhibition with a series of sulfonamides incorporating phthalimido moieties. |
| AID1570388 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins by phenol red staining-based stopped flow CO2 hydrase assay | 2019 | Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21 | Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure. |
| AID1556939 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 2 expressed in Escherichia coli to Ki for human recombinant carbonic anhydrase 9 expressed in Escherichia coli | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX. |
| AID462277 | Inhibition of human CA7 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1076531 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Design, synthesis and evaluation of N-substituted saccharin derivatives as selective inhibitors of tumor-associated carbonic anhydrase XII. |
| AID1426785 | Inhibition of recombinant human CA1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis. |
| AID272521 | Inhibition of human cloned CA2 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID590767 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 2 | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Virtual screening-driven identification of human carbonic anhydrase inhibitors incorporating an original, new pharmacophore. |
| AID300758 | Selectivity for human CA9 over human CA1 | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1375668 | Inhibition of recombinant human carbonic anhydrase-4 incubated for 15 mins by stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis. |
| AID411534 | Inhibition of human recombinant CA7 by stopped flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID411534 | Inhibition of human recombinant CA7 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1852040 | Inhibition of recombinant human CA1 pre-incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID299242 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID747809 | Inhibition of recombinant human CA1 cytosolic isoform preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID350899 | Inhibition of CO2-hydratase activity of human carbonic anhydrase 1 by CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Effects of new 5-amino-1,3,4-thiadiazole-2-sulfonamide derivatives on human carbonic anhydrase isozymes. |
| AID1563832 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis. |
| AID1257051 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Interaction of carbonic anhydrase isozymes I, II, and IX with some pyridine and phenol hydrazinecarbothioamide derivatives. |
| AID456397 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Carbonic anhydrase inhibitors. Identification of selective inhibitors of the human mitochondrial isozymes VA and VB over the cytosolic isozymes I and II from a natural product-based phenolic library. |
| AID1468998 | Binding affinity to human full length His-tagged CA2 (1 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic association rate constant after 60 secs at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID461324 | Inhibition of CA1 from human erythrocytes by Lineweaver-Burke analysis | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. |
| AID1607538 | Inhibition of human recombinant carbonic anhydrase 5B preincubated with enzyme for 1 hr prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy. |
| AID239146 | Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID1058184 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | A prodrug approach toward cancer-related carbonic anhydrase inhibition. |
| AID1548134 | Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID669487 | Inhibition of human recombinant full length CA14-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, structure-activity relationship studies, and X-ray crystallographic analysis of arylsulfonamides as potent carbonic anhydrase inhibitors. |
| AID417835 | Inhibition of mouse recombinant full length CA13 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1456316 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Synthesis and human/bacterial carbonic anhydrase inhibition with a series of sulfonamides incorporating phthalimido moieties. |
| AID1468992 | Binding affinity to human CA9 catalytic domain expressed in mammalian expression system assessed as intrinsic association rate constant after 60 secs at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID620689 | Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 9 catalytic domain | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II. |
| AID1655152 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 9 preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for recombinant human carbonic anhydrase 2 preincubated with enzyme for 10 mins b | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors. |
| AID238760 | Binding affinity towards human cloned carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. |
| AID1918142 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 10 mins and measured by phenol red based stopped-flow CO2 hydration assay | |||
| AID772921 | Inhibition of human carbonic anhydrase-9 by stopped flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20 | Effect of incorporating a thiophene tail in the scaffold of acetazolamide on the inhibition of human carbonic anhydrase isoforms I, II, IX and XII. |
| AID254245 | Inhibitory activity against human Carbonic anhydrase XII (hCA XII) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. |
| AID1520080 | Binding affinity to recombinant human carbonic anhydrase 2 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1172255 | Inhibition of human recombinant CA12 catalytic domain by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22 | Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. |
| AID1406817 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel hydrazido benzenesulfonamides-isatin conjugates: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID1245664 | Inhibition of carbonic anhydrase-1 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1519753 | Inhibition of recombinant human carbonic anhydrase-1 at 1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID493884 | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1175495 | Inhibition of human recombinant carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1739497 | Inhibition of human CA2 by stopped-flow carbon dioxide hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases. |
| AID464123 | Selectivity ratio of Ki for human CA2 to Ki for human CA14 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies. |
| AID1254030 | Inhibition of Leishmania donovani chagasi beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID1628036 | Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17 | Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum. |
| AID1070018 | Inhibition of Cryptococcus neoformans beta-carbonic anhydrase Can2 | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Anion inhibition studies of two new β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID257063 | Inhibition of recombinant human cytosolic isozyme CA II | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID1623426 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration after 15 mins by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment. |
| AID342469 | Inhibition of AQP4 expressed in rat FRT cells assessed as transepithelial osmotic water permeability at 100 uM by dye dilution method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID367616 | Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367616 | Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID50178 | Concentration producing 50% inhibition of carbonic anhydrase taken from mouse erythrocytes | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides. |
| AID1275563 | Inhibition of human carbonic anhydrase-1 using p-nitrophenyl acetate as substrate by esterase assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID47709 | Inhibition of human recombinant carbonic anhydrase I | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
| AID1241136 | Inhibition of human carbonic anhydrase-2 incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Exploring new Probenecid-based carbonic anhydrase inhibitors: Synthesis, biological evaluation and docking studies. |
| AID462279 | Inhibition of human CA12 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID1243120 | Inhibition of human carbonic anhydrase 12 at 10'-9 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1918139 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 10 mins and measured by phenol red based stopped-flow CO2 hydration assay | |||
| AID413966 | Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydrase assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates. |
| AID537657 | Inhibition of human carbonic anhydrase 2 by Lineweaver-Burke plot analysis | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide. |
| AID1303398 | Selectivity ratio, ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 9 | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII. |
| AID669114 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1649852 | Inhibition of human CA7 preincubated for 15 mins by stopped-flow carbon dioxide hydration assay | |||
| AID415831 | Inhibition of human recombinant CA9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors. |
| AID50193 | Inhibition concentration by inhibition of carbonic anhydrase from myelin in Rat | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8 | Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives. |
| AID320309 | Inhibition of human recombinant full length carbonic hydrase 5A by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID327762 | Inhibition of human full length carbonic anhydrase 5A by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1175504 | Inhibition of human recombinant carbonic anhydrase 14 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. |
| AID1605089 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action. |
| AID758951 | Inhibition of Cryptococcus neoformans recombinant Can2 by CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14 | A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules. |
| AID1170190 | Inhibition of human carbonic anhydrase 13 at pH7 and 25 degC by stopped-flow kinetic inhibition assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID314789 | Inhibition of human carbonic anhydrase 2 in presence of 0.25 mM beta-mercaptoethanol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID52076 | Relative salidiuretic efficacy was scored in chimpanzee; weak | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID1520081 | Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1373184 | Binding affinity to recombinant human carbonic anhydrase 9 (1 to 260 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID350901 | Inhibition of esterase activity of human carbonic anhydrase 1 by CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Effects of new 5-amino-1,3,4-thiadiazole-2-sulfonamide derivatives on human carbonic anhydrase isozymes. |
| AID263636 | Inhibition of human recombinant CA1 | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori. |
| AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1849578 | Inhibition of human recombinant CA12 incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1278411 | Inhibition of Nostoc commune gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID238340 | Ki value against mouse carbonic anhydrase XIII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID1603063 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors. |
| AID1631903 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and carbonic anhydrase inhibitory effects of new N-glycosylsulfonamides incorporating the phenol moiety. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID365982 | Inhibition of human cloned CA5A by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID369275 | Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID1430527 | Inhibition of Burkholderia pseudomallei recombinant carbonic anhydrase gamma incubated for 15 mins prior to testing by stopped flow CO2 hydration method | |||
| AID1461802 | Inhibition of human CA1 | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | 1,3-Oxazole-based selective picomolar inhibitors of cytosolic human carbonic anhydrase II alleviate ocular hypertension in rabbits: Potency is supported by X-ray crystallography of two leads. |
| AID264310 | Inhibition of human CA1 | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
| AID1723497 | Antibacterial activity against Enterococcus faecium NR-32052 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay | |||
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1058181 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | A prodrug approach toward cancer-related carbonic anhydrase inhibition. |
| AID1809105 | Inhibition of recombinant human carbonic anhydrase 9 using 4-nitrophenylacetate as substrate | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis. |
| AID1446106 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1626026 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma. |
| AID1360105 | Pain relieving effect in mouse oxaliplatin-induced neuropathic pain model at 30 to 100 mg/kg, po measured at 15 mins by cold plate test | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and X-ray crystallography of selenides bearing benzenesulfonamide moiety with neuropathic pain modulating effects. |
| AID1666826 | Selectivity index, ratio of Ki for human carbonic anhydrase 1 to Ki for human carbonic anhydrase 2 | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID462280 | Inhibition of mouse CA13 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID620657 | Reduction in CA12 protein level in ca9/ca12 double silenced human LS 174T cells under hypoxia at 60 uM after 48 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1491566 | Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration pretreated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | |
| AID1518935 | Inhibition of recombinant human carbonic anhydrase 12 assessed as residual activity at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1659544 | Inhibition of human carbonic anhydrase 2 using p-nitrophenyl acetate as substrate by UV-VIS spectrophotometric analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX. |
| AID475901 | Inhibition of human recombinant carbonic anhydrase1 after 15 mins by stopped flow carbon dioxide hydrase assay method | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides. |
| AID307886 | Inhibition of human CA1 by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID1061033 | Inhibition of human CA12 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1564429 | Inhibition of recombinant human CA9 at 10'-6 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1655387 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1061032 | Inhibition of human CA13 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1655391 | Inhibition of recombinant human carbonic anhydrase 5B preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1731029 | Inhibition of human CAH13 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1517549 | Inhibition of human carbonic anhydrase 9 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1256859 | Inhibition of human carbonic anhydrase-1 assessed as CO2 hydration activity by stopped-flow method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID1461936 | Inhibition of Vibrio cholerae beta-CA incubated for 15 mins by stopped-flow CO2 hydration assay | |||
| AID1578354 | Inhibition of recombinant human CA2 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors. |
| AID1688238 | Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases. |
| AID1849539 | Binding affinity to human CA1 assessed as inhibition constant using p-Nitrophenylacetate as substrate by SDS-PAGE analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID300869 | Inhibition of human cloned catalytic domain CA9 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety. |
| AID464119 | Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies. |
| AID299248 | Inhibition of human carbonic anhydrase 14 by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID761444 | Inhibition of human recombinant CA2 using 4-nitrophenylacetate as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Sulfonamides containing coumarin moieties selectively and potently inhibit carbonic anhydrases II and IX: design, synthesis, inhibitory activity and 3D-QSAR analysis. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1726083 | Inhibition of human CA2 pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in |
| AID1758425 | Selectivity index, ratio of Ki for inhibition of human CA2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assa | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides. |
| AID299247 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID484161 | Inhibition of full length human carbonic anhydrase 7 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1405951 | Inhibition of human recombinant carbonic anhydrase 7 assessed as CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye-based stopped-flow assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal. |
| AID1262265 | Inhibition of human CA3 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus. |
| AID1809971 | Inhibition of recombinant human CA1 using 4-nitrophenylacetate as substrate by esterase assay | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID300761 | Selectivity for human CA12 over human CA2 | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID780928 | Binding affinity to human recombinant carbonic anhydrase 6 expressed in Escherichia coli Rosetta2 (DE3) by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Benzenesulfonamides with pyrimidine moiety as inhibitors of human carbonic anhydrases I, II, VI, VII, XII, and XIII. |
| AID1768056 | Inhibition of human carbonic anhydrase 1 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
| AID1161950 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID315099 | Inhibition of human carbonic anhydrase 1 assessed as 4-nitrophenyl phosphate hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates. |
| AID1596538 | Selectivity index, ratio of Ki of human carbonic anhydrase 1 to Ki of human carbonic anhydrase 9 | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID350904 | Inhibition of human carbonic anhydrase 1 by Lineweaver-Burke plot | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Effects of new 5-amino-1,3,4-thiadiazole-2-sulfonamide derivatives on human carbonic anhydrase isozymes. |
| AID1852045 | Selectivity index, ratio of Ki for inhibition of recombinant human CA1 to Ki for inhibition of recombinant human CA4 | |||
| AID475903 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for Brucella suis recombinant (6X)His tagged-beta carbonic anhydrase | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides. |
| AID1511296 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 4 | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID526863 | Binding affinity to human recombinant carbonic anhydrase 7 by thermal shift assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID1808983 | Inhibition of human carbonic anhydrase 7 by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID1166266 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel sulfonamides bearing pyrrole and pyrrolopyrimidine moieties as carbonic anhydrase inhibitors: Synthesis, cytotoxic activity and molecular modeling. |
| AID1633348 | Inhibition of Leishmania donovani chagasi carbonic anhydrase preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID492422 | Inhibition of human recombinant carbonic anhydrase 12 catalytic domain preincubated for 15 mins by CO2 hydration method | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Coumarinyl-substituted sulfonamides strongly inhibit several human carbonic anhydrase isoforms: solution and crystallographic investigations. |
| AID1058082 | Inhibition of human recombinant carbonic anhydrase 2-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Salen and tetrahydrosalen derivatives act as effective inhibitors of the tumor-associated carbonic anhydrase XII--a new scaffold for designing isoform-selective inhibitors. |
| AID1067263 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 after 6 hrs by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Synthesis of 6-tetrazolyl-substituted sulfocoumarins acting as highly potent and selective inhibitors of the tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1245674 | Inhibition of carbonic anhydrase-12 (unknown origin) | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18 | Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases. |
| AID1243122 | Inhibition of human carbonic anhydrase 12 at 10'-7 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1565745 | Inhibition of human carbonic anhydrase 12 assessed as reduction in CO2 hydration at 10'-8 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1818404 | Inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors. |
| AID314801 | Inhibition of human carbonic anhydrase 2 in presence of 0.05 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID342468 | Inhibition of AQP4 expressed in rat FRT cells assessed as osmotic water permeability at 100 uM after 60 mins by stopped-flow light scattering method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID739941 | Inhibition of human carbonic anhydrase-3 cytosolic isoform after 15 mins by Stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Structural effect of phenyl ring compared to thiadiazole based adamantyl-sulfonamides on carbonic anhydrase inhibition. |
| AID1166969 | Inhibition of human CA-9 after 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Inhibition of carbonic anhydrase isoforms I, II, IX and XII with novel Schiff bases: identification of selective inhibitors for the tumor-associated isoforms over the cytosolic ones. |
| AID1194926 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of a new series of dithiocarbamates with effective human carbonic anhydrase inhibitory activity and antiglaucoma action. |
| AID484157 | Inhibition of full length human carbonic anhydrase 4 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID496917 | Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1351428 | Inhibition of human carbonic anhydrase 9 using 4-NPA as substrate after 3 mins by spectrophotometric analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, synthesis and biological evaluation of novel pyridine-thiazolidinone derivatives as anticancer agents: Targeting human carbonic anhydrase IX. |
| AID730374 | Inhibition of human cytosolic carbonic anhydrase-1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Kinetic and anion inhibition studies of a β-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis. |
| AID1336990 | Selectivity ratio of Ki for human erythrocyte cytosolic carbonic anhydrase 1 to Ki for human membrane bound carbonic anhydrase 9 | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Benzenesulfonamide bearing imidazothiadiazole and thiazolotriazole scaffolds as potent tumor associated human carbonic anhydrase IX and XII inhibitors. |
| AID1422962 | Inhibition of recombinant human CA1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID610537 | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID1520078 | Binding affinity to recombinant human carbonic anhydrase 14 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID413964 | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates. |
| AID1408650 | Inhibition of recombinant human carbonic anhydrase 5a incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity. |
| AID275808 | Inhibition of human recombinant cytosolic isozyme CA II by stopped-flow CO2 hydrase method | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. |
| AID578221 | Inhibition of human recombinant CA1 cytosolic isoform by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | (R)-/(S)-10-camphorsulfonyl-substituted aromatic/heterocyclic sulfonamides selectively inhibit mitochondrial over cytosolic carbonic anhydrases. |
| AID1235243 | Inhibition of Porphyromonas gingivalis CA after 15 mins by stopped-flow/Co2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Cloning, characterization and anion inhibition studies of a new γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1425987 | Binding affinity to recombinant human carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. |
| AID271037 | Inhibition of human cloned CA1 by CO2 hydration assay | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors. |
| AID1185162 | Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae. |
| AID1195030 | Inhibition of human CA-2 using p-nitro-phenylacetate as substrate after 3 mins by UV-Vis spectrophotometry | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II. |
| AID1272993 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1061035 | Inhibition of human CA7 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID321162 | Selectivity for human CA12 over human CA1 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1534901 | Inhibition of recombinant full length human carbonic anhydrase-1 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID314800 | Inhibition of human carbonic anhydrase 9 in presence of 0.01 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID367610 | Inhibition of human recombinant full length CA3 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367610 | Inhibition of human recombinant full length CA3 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID732027 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Carbonic anhydrase inhibitors: benzenesulfonamides incorporating cyanoacrylamide moieties are low nanomolar/subnanomolar inhibitors of the tumor-associated isoforms IX and XII. |
| AID1310847 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | PEGylated Bis-Sulfonamide Carbonic Anhydrase Inhibitors Can Efficiently Control the Growth of Several Carbonic Anhydrase IX-Expressing Carcinomas. |
| AID1350480 | Inhibition of recombinant human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
| AID238788 | Inhibitory activity against human carbonic anhydrase IX expressed in Escherichia coli BL21 | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties. |
| AID1154448 | Inhibition of human cloned transmembrane tumor-associated catalytic domain of carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Carbonic anhydrase inhibitors. Synthesis of a novel series of 5-substituted 2,4-dichlorobenzenesulfonamides and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII. |
| AID669118 | Inhibition of Candida glabrata CgNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1375670 | Inhibition of recombinant human carbonic anhydrase-12 incubated for 15 mins by stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis. |
| AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1454028 | Inhibition of recombinant human membrane bound carbonic anhydrase 9 expressed in Escherichia coli pretreated for 15 mins prior to testing by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases. |
| AID1358712 | Inhibition of recombinant human carbonic anhydrase 4 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. |
| AID1555969 | Inhibition of human carbonic anhydrase 9 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID293811 | Inhibition of human recombinant CA1 by stopped flow CO2 hydrase assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties. |
| AID1464262 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase-2 to Ki for human recombinant carbonic anhydrase-9 | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID256963 | Inhibitory activity against human recombinant cytosolic CA2 | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors. |
| AID1660017 | Inhibition of human carbonic anhydrase 12 assessed as inhibitory constant incubated for 6 hrs by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID1518850 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1275562 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 12 | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. |
| AID1435060 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 10 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5 | Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID314775 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 1.00 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1519762 | Inhibition of recombinant human carbonic anhydrase-9 at 1 uM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID669123 | Antimicrobial activity against Malassezia globosa CBS 7966 after 7 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1355469 | Inhibition of recombinant human cytosolic CA1 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | 4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors. |
| AID316062 | Inhibition of human recombinant full length carbonic hydrase 3 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID1474294 | Inhibition of recombinant human membrane bound carbonic anhydrase 4 pretreated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Evaluation of selenide, diselenide and selenoheterocycle derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors. |
| AID1564386 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitors. |
| AID1434431 | Inhibition of Porphyromonas gingivalis Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | |||
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1278409 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID261581 | Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. |
| AID1406815 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel hydrazido benzenesulfonamides-isatin conjugates: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID1172252 | Inhibition of human full length CA1 by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22 | Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. |
| AID730518 | Inhibition of Helicobacter pylori alpha-carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | An α-carbonic anhydrase from the thermophilic bacterium Sulphurihydrogenibium azorense is the fastest enzyme known for the CO2 hydration reaction. |
| AID1234860 | Inhibition of human recombinant carbonic anhydrase 9 expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | 5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII. |
| AID1433067 | Inhibition of human CA12 by stopped-flow CO2 hydration method | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and carbonic anhydrase isoenzymes I, II, IX, and XII inhibitory effects of dimethoxybromophenol derivatives incorporating cyclopropane moieties. |
| AID1704680 | Inhibition of human CA9 preincubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. |
| AID1564414 | Inhibition of recombinant human CA1 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID734184 | Inhibition of recombinant human carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship. |
| AID1736564 | Inhibition of recombinant human CA9 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1243111 | Inhibition of human carbonic anhydrase 1 at 10'-6 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1739498 | Inhibition of human CA9 by stopped-flow carbon dioxide hydration assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases. |
| AID1355475 | Inhibition of recombinant human CA9 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | 4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors. |
| AID301572 | Activity of human recombinant CA 3 assessed as CO2 hydration | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. |
| AID1666827 | Selectivity index, ratio of Ki for human carbonic anhydrase 9 to Ki for human carbonic anhydrase 2 | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies. |
| AID578222 | Inhibition of human recombinant CA2 cytosolic isoform by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | (R)-/(S)-10-camphorsulfonyl-substituted aromatic/heterocyclic sulfonamides selectively inhibit mitochondrial over cytosolic carbonic anhydrases. |
| AID1268962 | Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA. |
| AID307892 | Inhibition of human CA12 catalytic domain by stopped flow CO2 hydrase method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Carbonic anhydrase activators: the first activation study of the human secretory isoform VI with amino acids and amines. |
| AID1446104 | Inhibition of recombinant human carbonic anhydrase 12 preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1339403 | Inhibition of recombinant human carbonic anhydrase 7 assessed as reduction in CO2 hydration preincubated for 15 mins by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties. |
| AID1692369 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 12 | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID669320 | Inhibition of human recombinant full length CA1-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, structure-activity relationship studies, and X-ray crystallographic analysis of arylsulfonamides as potent carbonic anhydrase inhibitors. |
| AID1067229 | Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. |
| AID1442869 | Inhibition of recombinant human Carbonic anhydrase 5B assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action. |
| AID272528 | Inhibition of murine CA13 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID166907 | Variation of intraocular pressure in third day at a dose of 30 mg/kg by oral administration in hypertensive rabbits | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID21085 | Evaluated for lipid solubility measured as partition coefficient at a pH 7.4 (CHCl3/buffer) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors. |
| AID593734 | Inhibition of human recombinant CAH7 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides. |
| AID1723506 | Inhibition of carbonic anhydrase in Enterococcus faecium NR-31972 assessed as antibacterial activity incubated for 18 to 20 hrs in presence of ambient air by CLSI protocol based broth microdilution assay | |||
| AID1723531 | Antibacterial activity against Enterococcus faecium ATCC 700221 by CLSI protocol based assay | |||
| AID386505 | Selectivity for human CA12 over human CA1 | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID1464259 | Inhibition of human recombinant carbonic anhydrase-9 preincubated for 10 mins by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID1656166 | Inhibition of human CA2 preincubated for 15 mins by stopped-flow CO2 hydration kinetic assay based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action. |
| AID514213 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 9 to Ki for human recombinant carbonic anhydrase 2 | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity. |
| AID598728 | Inhibition of recombinant human carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay at pH 8.3 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Inhibition studies with anions and small molecules of two novel β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium. |
| AID1133323 | Dissociation constant, pKa of the compound | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides. |
| AID1434429 | Inhibition of Burkholderia pseudomallei Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | |||
| AID1756971 | Selectivity index, ratio of IC50 for human carbonic anhydrase 2 to IC50 for human carbonic anhydrase 9 | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
| AID1360941 | Binding affinity to human carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors. |
| AID1604482 | Inhibition of human CA7 pre-incubated for 6 hrs by stopped- flow CO2 hydrase assay method based Cheng-Prusoff equation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis. |
| AID1243114 | Inhibition of human carbonic anhydrase 2 at 10'-7 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1753406 | Inhibition of recombinant human CA9 pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Insertion of metal carbenes into the anilinic N-H bond of unprotected aminobenzenesulfonamides delivers low nanomolar inhibitors of human carbonic anhydrase IX and XII isoforms. |
| AID328981 | Inhibition of human full length carbonic anhydrase 7 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID237405 | Compound level in Red Blood Cells at 30 min, after exposure of 10 mL of Blood to compound solution by HPLC method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID1422973 | Inhibition of recombinant human CA14 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID1058081 | Inhibition of human recombinant carbonic anhydrase 9-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Salen and tetrahydrosalen derivatives act as effective inhibitors of the tumor-associated carbonic anhydrase XII--a new scaffold for designing isoform-selective inhibitors. |
| AID1194928 | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of a new series of dithiocarbamates with effective human carbonic anhydrase inhibitory activity and antiglaucoma action. |
| AID371559 | Selectivity for full length human recombinant mitochondrial carbonic anhydrase 5A over human recombinant cytosolic carbonic anhydrase 2 | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. |
| AID1357960 | Cytotoxicity against human MDA-MB-231 cells after 96 hrs under hypoxic condition by MTT assay | |||
| AID339675 | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1322629 | Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped flow carbon dioxide hydrase assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure Lowering Investigations. |
| AID590765 | Inhibition of human carbonic anhydrase 1 after 6 hrs by Lineweaver-Burk plot analysis | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Virtual screening-driven identification of human carbonic anhydrase inhibitors incorporating an original, new pharmacophore. |
| AID1686871 | Selectivity index. ratio of Ki for inhibition of recombinant human carbonic anhydrase 9 to Ki for Ki for inhibition of recombinant human carbonic anhydrase 2 | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID382979 | Permeability across rabbit cornea | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID697239 | Inhibition of human CA2 using 4-nitrophenylacetate as substrate preincubated for 10 mins by spectrophotometric esterase assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. |
| AID314828 | Inhibition of human carbonic anhydrase 2 in presence of 1.00 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1273034 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII. |
| AID1520073 | Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as observed dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1564593 | Inhibition of recombinant human carbonic anhydrase 2 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity. |
| AID238314 | Ki value against human carbonic anhydrase III | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. |
| AID314823 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.10 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID409600 | Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes at 20 uM | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Inhibition of aquaporin 4 by antiepileptic drugs. |
| AID729569 | Inhibition of Drosophila melanogaster recombinant carbonic anhydrase-2 expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | Characterization, bioinformatic analysis and dithiocarbamate inhibition studies of two new α-carbonic anhydrases, CAH1 and CAH2, from the fruit fly Drosophila melanogaster. |
| AID1534906 | Inhibition of human carbonic anhydrase-14 catalytic domain assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID382971 | Solubility in water in presence of 0.1001 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1460774 | Inhibition of human CA13 by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Bortezomib inhibits mammalian carbonic anhydrases. |
| AID448554 | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides. |
| AID1251972 | Inhibition of human carbonic anhydrase 1 incubated for 6 hrs by stopped flow carbon-di-oxide hydrase assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Click-tailed coumarins with potent and selective inhibitory action against the tumor-associated carbonic anhydrases IX and XII. |
| AID1784931 | Inhibition of human CA12 measured after 15 mins by stopped flow carbon dioxide anhydrase assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Natural inspired piperine-based sulfonamides and carboxylic acids as carbonic anhydrase inhibitors: Design, synthesis and biological evaluation. |
| AID644034 | Inhibition of human carbonic anhydrase 6 esterase activity using 4-nitrophenylacetate as substrate | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives. |
| AID1759814 | Inhibition of Burkholderia pseudomallei gamma carbonic anhydrase preincubated with enzyme for 15 mins by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1425988 | Binding affinity to recombinant human carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. |
| AID730369 | Inhibition of Saccharomyces cerevisiae beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Kinetic and anion inhibition studies of a β-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis. |
| AID1581514 | Inhibition of recombinant human carbonic anhydrase 9 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1410855 | Inhibition of human CA1 assessed as enzyme inhibitor complex formation preincubated for 15 mins and measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Discovery of 4-Hydroxy-3-(3-(phenylureido)benzenesulfonamides as SLC-0111 Analogues for the Treatment of Hypoxic Tumors Overexpressing Carbonic Anhydrase IX. |
| AID272520 | Inhibition of human cloned CA1 by stopped-flow CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. |
| AID1076533 | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Design, synthesis and evaluation of N-substituted saccharin derivatives as selective inhibitors of tumor-associated carbonic anhydrase XII. |
| AID382967 | Solubility in water in presence of 0.1132 mol/l hydroxypropyl-beta-cyclodextrin and 0.335 mol/l triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1563830 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15 | Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis. |
| AID1449740 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Inhibition of Malassezia globosa carbonic anhydrase with phenols. |
| AID342481 | Inhibition of human carbonic anhydrase 6 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID1278561 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow carbon dioxide hydrase assay | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII. |
| AID1655149 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors. |
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID493890 | Inhibition of human recombinant carbonic anhydrase 7 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1852049 | Selectivity index, ratio of Ki for inhibition of recombinant human CA1 to Ki for inhibition of recombinant human CA12 | |||
| AID1753391 | Selectivity index, ratio of Ki for inhibition of human CA2 to Ki for inhibition of human CA9 | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities. |
| AID1717282 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Sulfonamide/sulfamate switch with a series of piperazinylureido derivatives: Synthesis, kinetic and in silico evaluation as carbonic anhydrase isoforms I, II, IV, and IX inhibitors. |
| AID1726061 | Inhibition of Vibrio cholerae gamma carbonic anhydrase incubated for 30 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | |||
| AID1335034 | Inhibition of human recombinant transmembrane tumor associated carbonic anhydrase 9 preincubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | 5-Substituted-benzylsulfanyl-thiophene-2-sulfonamides with effective carbonic anhydrase inhibitory activity: Solution and crystallographic investigations. |
| AID1272995 | Inhibition of recombinant human carbonic anhydrase 7 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. |
| AID1736572 | Selectivity index, ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 12 | |||
| AID331291 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols. |
| AID587001 | Inhibition of tumor-associated human carbonic anhydrase 9 preincubated for 15 min by CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis. |
| AID427129 | Inhibition of human carbonic anhydrase 5B by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID1308827 | Inhibition of human recombinant carbonic anhydrase 7 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID1469004 | Binding affinity to human N-terminal full length His-tagged CA13 (1 to 262 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic association rate constant after 60 secs at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1330455 | Selectivity ratio of Ki of human full length carbonic anhydrase 2 to Ki for human full length carbonic anhydrase 1 | |||
| AID367612 | Inhibition of human recombinant full length CA5A by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367612 | Inhibition of human recombinant full length CA5A by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID382942 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.0226 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID367611 | Inhibition of human recombinant full length CA4 by stopped-flow CO2 hydration method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID367611 | Inhibition of human recombinant full length CA4 by stopped-flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID1072630 | Inhibition of human transmembrane carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Benzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XII. |
| AID461323 | Inhibition of esterase-activity of human erythrocytes CA2 by spectrophotometry | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. |
| AID305485 | Inhibition of human recombinant CA1 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions. |
| AID1425991 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. |
| AID1433065 | Inhibition of human CA2 using para-nitrophenylacetate as substrate measured over 3 mins by UV-vis spectrophotometric method | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and carbonic anhydrase isoenzymes I, II, IX, and XII inhibitory effects of dimethoxybromophenol derivatives incorporating cyclopropane moieties. |
| AID1605091 | Inhibition of recombinant human carbonic anhydrase 7 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action. |
| AID1172694 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Carbonic anhydrase inhibitory activity of sulfonamides and carboxylic acids incorporating cyclic imide scaffolds. |
| AID1067228 | Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. |
| AID1357842 | Inhibition of human membrane-anchored carbonic anhydrase 4 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | 2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents. |
| AID589727 | Inhibition of human cytosolic carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. |
| AID428460 | Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1462736 | Inhibition of human CA9 pre-incubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Synthesis and carbonic anhydrase inhibition of polycyclic imides incorporating N-benzenesulfonamide moieties. |
| AID1061067 | Inhibition of Porphyromonas gingivalis recombinant gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii. |
| AID1518942 | Inhibition of recombinant human carbonic anhydrase 9 assessed as residual activity at 1 nM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1731022 | Inhibition of human CAH4 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1405952 | Inhibition of human recombinant carbonic anhydrase 9 assessed as CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red dye-based stopped-flow assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal. |
| AID1471692 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX). |
| AID314765 | Inhibition of human carbonic anhydrase 2 in presence of 0.05 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1888320 | Inhibition of recombinant human carbonic anhydrase 12 assessed as inhibition constant preincubated for 15 mins by measured for 10 to 100 secs by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain. |
| AID1520089 | Binding affinity to recombinant human carbonic anhydrase 13 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID1439691 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for recombinant human tumor-associated carbonic anhydrase 9 | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. |
| AID1462735 | Inhibition of human CA2 pre-incubated for 10 mins by stopped-flow CO2 hydrase assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Synthesis and carbonic anhydrase inhibition of polycyclic imides incorporating N-benzenesulfonamide moieties. |
| AID367656 | Inhibition of Stylophora pistillata carbonic anhydrase measured by CO2 hydration reaction assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Carbonic anhydrase inhibitors: inhibition studies of a coral secretory isoform with inorganic anions. |
| AID1456317 | Inhibition of Vibrio cholerae alpha carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Synthesis and human/bacterial carbonic anhydrase inhibition with a series of sulfonamides incorporating phthalimido moieties. |
| AID1291359 | Inhibition of recombinant Sulfurihydrogenibium yellostonense alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1596540 | Selectivity index, ratio of Ki of human carbonic anhydrase 1 to Ki of human carbonic anhydrase 12 | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID232688 | Selectivity ratio of KI, human carbonic anhydrase II (hCA II), to that of KI, mouse carbonic anhydrase V (mCA V) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides. |
| AID1769577 | Inhibition of recombinant human CA9 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold. |
| AID1649855 | Inhibition of human CA14 preincubated for 15 mins by stopped-flow carbon dioxide hydration assay | |||
| AID23571 | The solubility at pH 7.40 and 25 degree Centigrade was evaluated. | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route. |
| AID339670 | Inhibition of human recombinant carbonic anhydrase 3 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1809976 | Solubility of compound in water | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID678515 | Inhibition of human CA1 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors. |
| AID1166267 | Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 12 | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel sulfonamides bearing pyrrole and pyrrolopyrimidine moieties as carbonic anhydrase inhibitors: Synthesis, cytotoxic activity and molecular modeling. |
| AID386502 | Inhibition of human cloned CA12 catalytic domain by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozymes I and II and tumor-associated isozymes IX and XII with S-substituted 4-chloro-2-mercapto-5-methyl-benzenesulfonamides. |
| AID678521 | Inhibition of Candida albicans beta carbonic anhydrase NCE103 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors. |
| AID1237882 | Inhibition of Cryptococcus neoformans var. grubii beta-carbonic anhydrase incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties. |
| AID1255574 | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli preincubated for 6 hrs by stopped flow CO2 hydrase assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Isatin-pyrazole benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID780324 | Inhibition of human carbonic anhydrase6 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID23922 | Lipophilicity of the compound | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. |
| AID1720899 | Inhibition of recombinant human carbonic anhydrase 9 assessed as inhibition constant preincubated with enzyme for 10 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | New coumarin/sulfocoumarin linked phenylacrylamides as selective transmembrane carbonic anhydrase inhibitors: Synthesis and in-vitro biological evaluation. |
| AID620793 | Cytotoxicity against CA9 expressing chinese hamster PS120 cells assessed as cell viability at 60 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1548136 | Inhibition of Cryptococcus neoformans beta carbonic anhydrase incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. |
| AID417832 | Inhibition of human recombinant full length CA7 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1519746 | Inhibition of recombinant human carbonic anhydrase-12 incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID526865 | Binding affinity to human recombinant carbonic anhydrase 13 by thermal shift assay | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII. |
| AID1230150 | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID427130 | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID474212 | Selectivity ratio of Ki for human recombinant CA1 to Ki for human recombinant CA12 | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID339678 | Inhibition of mouse recombinant carbonic anhydrase 13 by stopped flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? |
| AID1185074 | Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Carbonic anhydrase inhibitors: design, synthesis, and biological evaluation of novel sulfonyl semicarbazide derivatives. |
| AID50379 | Inhibitory activity against human carbonic anhydrase I (hCA I) by using esterase assay method | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design. |
| AID1251975 | Inhibition of human carbonic anhydrase 12 incubated for 6 hrs by stopped flow carbon-di-oxide hydrase assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Click-tailed coumarins with potent and selective inhibitory action against the tumor-associated carbonic anhydrases IX and XII. |
| AID464120 | Inhibition of human recombinant CA9 by stopped-flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies. |
| AID587129 | Inhibition of Leptonychotes weddellii alpha-carbonic anhydrase after 15 mins by Lineweaver-Burk plot | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii. |
| AID1678134 | Inhibition of recombinant human CA2 expressed in Escherichia coli BL21 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Structural Basis of Nanomolar Inhibition of Tumor-Associated Carbonic Anhydrase IX: X-Ray Crystallographic and Inhibition Study of Lipophilic Inhibitors with Acetazolamide Backbone. |
| AID314764 | Inhibition of human carbonic anhydrase 9 in presence of 0.01 mM dithiothreitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1596539 | Selectivity index, ratio of Ki of human carbonic anhydrase 2 to Ki of human carbonic anhydrase 9 | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | 5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors. |
| AID1183832 | Inhibition of recombinant human carbonic anhydrase 9 after 15 mins by stopped flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Selective inhibition of human carbonic anhydrases by novel amide derivatives of probenecid: synthesis, biological evaluation and molecular modelling studies. |
| AID1534909 | Anticonvulsant activity in mouse assessed as reduction in PTZ-induced seizures | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. |
| AID1058180 | Inhibition of human carbonic anhydrase 14 by stopped-flow CO2 hydration assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | A prodrug approach toward cancer-related carbonic anhydrase inhibition. |
| AID1517243 | Inhibition of human carbonic anhydrase 4 assessed as reduction in CO2 hydration incubated for 1 hr by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID311026 | Inhibition of human carbonic anhydrase 4 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1170171 | Inhibition of human carbonic anhydrase 7 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID48112 | Inhibitory activity of compound against bovine carbonic anhydrase IV | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. |
| AID1193748 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID47749 | Inhibitory activity against human carbonic anhydrase II was determined | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID780321 | Inhibition of human carbonic anhydrase12 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID21964 | Solubility (in phosphate buffer) | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | Acetazolamide-like carbonic anhydrase inhibitors with topical ocular hypotensive activity. |
| AID1565741 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration at 10'-8 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID1537869 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 expressed in Escherichia coli BL21 (DE3) to Ki for recombinant human carbonic anhydrase 12 expressed in Escherichia coli | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID599954 | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors. |
| AID1571208 | Inhibition of human erythrocyte carbonic anhydrase-1 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies. |
| AID1291093 | Inhibition of recombinant Candida albicans beta carbonic anhydrase NCE103 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID1649854 | Inhibition of human CA12 preincubated for 15 mins by stopped-flow carbon dioxide hydration assay | |||
| AID1647462 | Anti-hypoxia in mouse assessed as increase in mouse survival at 400 mg/kg, po administered for 3 days and observed upto day 3 after dosing of 1.5 hrs | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors. |
| AID462270 | Inhibition of human CA1 by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. |
| AID610538 | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by CO2 hydration method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. |
| AID320306 | Inhibition of human recombinant full length carbonic hydrase 2 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID1348311 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases. |
| AID222126 | Inhibition of cloned isozyme, human carbonic anhydrase II | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Carbonic anhydrase inhibitors: synthesis of sulfonamides incorporating dtpa tails and of their zinc complexes with powerful topical antiglaucoma properties. |
| AID352787 | Inhibition of human recombinant CA1 by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Carbonic anhydrase inhibitors. Synthesis of 2,4,6-trimethylpyridinium derivatives of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides acting as potent inhibitors of the tumor-associated isoform IX and XII. |
| AID50377 | Inhibitory activity against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX. |
| AID650294 | Inhibition of human cloned carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases. |
| AID616478 | Inhibition of Mycobacterium tuberculosis carbonic anhydrase 3 preincubated for 15 mins at pH 8.3 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID660237 | Inhibition of human CA1 pre-incubated for 15 mins by stopped-flow CO2 hydration method | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo. |
| AID577527 | Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID436747 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. |
| AID1162892 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | Quinazoline-sulfonamides with potent inhibitory activity against the α-carbonic anhydrase from Vibrio cholerae. |
| AID428457 | Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1419396 | Inhibition of recombinant human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles. |
| AID1704681 | Inhibition of human CA12 preincubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1852046 | Selectivity index, ratio of Ki for inhibition of recombinant human CA2 to Ki for inhibition of recombinant human CA4 | |||
| AID427127 | Inhibition of human carbonic anhydrase 3 by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
| AID1498920 | Inhibition of recombinant human carbonic anhydrase 9 assessed as reduction in CO2 hydration preincubated for 10 mins by stopped flow assay | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery. |
| AID1655394 | Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors. |
| AID1242666 | Selectivity index, ratio of Ki for full length human carbonic anhydrase-2 to Ki for human recombinant carbonic anhydrase-12 catalytic domain | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. |
| AID26315 | Dissociation constant (pKa) (determined in 30% EtOH) | 1982 | Journal of medicinal chemistry, May, Volume: 25, Issue:5 | Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids. |
| AID1759815 | Inhibition of recombinant human carbonic anhydrase 1 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | |||
| AID1406816 | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel hydrazido benzenesulfonamides-isatin conjugates: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. |
| AID493895 | Inhibition of mouse recombinant carbonic anhydrase 15 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1254033 | Inhibition of Candida glabrata beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Poly(amidoamine) dendrimers show carbonic anhydrase inhibitory activity against α-, β-, γ- and η-class enzymes. |
| AID486936 | Inhibition of human full length carbonic anhydrase 14 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. |
| AID486936 | Inhibition of human full length carbonic anhydrase 14 catalytic domain preincubated for 15 mins by stopped flow CO2 hydration assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. |
| AID1058396 | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID1518948 | Inhibition of recombinant human carbonic anhydrase 9 at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID415675 | Inhibition of Caenorhabditis elegans carbonic anhydrase 4b by CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Carbonic anhydrase inhibitors. The nematode alpha-carbonic anhydrase of Caenorhabditis elegans CAH-4b is highly inhibited by 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides. |
| AID646240 | Inhibition of human recombinant carbonic anhydrase 3 using carbon-dioxide as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID1731031 | Inhibition of human full length CAH2 expressed in Escherichia coli BL21 (DE3) assessed as reduction in esterase activity using p-nitrophenyl acetate substrate by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1464233 | Inhibition of human CA2 catalytic activity pre-incubated for 15 mins followed by 4-NPA substrate addition and measured every 12 to 15 secs for 5 mins by spectrophotometry | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | A prodrug design for improved oral absorption and reduced hepatic interaction. |
| AID428370 | Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1312159 | Inhibition of Mycobacterium tuberculosis beta-carbonic anhydrase Rv1284 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID764718 | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety. |
| AID1849574 | Binding affinity to human CA2 assessed as inhibition constant using 4-nitrophenylacetate as substrate by spectrophotometry based esterase assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1466464 | Inhibition of recombinant human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII. |
| AID1195369 | Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides. |
| AID1555967 | Inhibition of human carbonic anhydrase 7 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID1692368 | Selectivity index, ratio of Ki for recombinant human carbonic anhydrase 2 to Ki for recombinant human carbonic anhydrase 9 | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity. |
| AID611568 | Inhibition of bovine carbonic anhydrase assessed as formation of p-nitrophenol from p-nitrophenyl acetate substrate after 30 mins by spectrophotometric method | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Discovery of new chromone containing sulfonamides as potent inhibitors of bovine cytosolic carbonic anhydrase. |
| AID1464257 | Inhibition of human recombinant carbonic anhydrase-1 preincubated for 10 mins by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of sulfonamides incorporating phenylacrylamido functionalities as carbonic anhydrase isoforms I, II, IX and XII inhibitors. |
| AID1731020 | Inhibition of human CAH2 expressed in Escherichia coli BL21 (DE3) by stopped flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer. |
| AID1189115 | Inhibition of recombinant human carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase Assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Carbonic Anhydrase Inhibition with Benzenesulfonamides and Tetrafluorobenzenesulfonamides Obtained via Click Chemistry. |
| AID1564428 | Inhibition of recombinant human CA9 at 10'-7 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1426786 | Inhibition of recombinant human CA2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Design and Synthesis of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Treatment of Rheumatoid Arthritis. |
| AID438007 | Inhibition of human full length cytosolic carbonic anhydrase 7 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID320311 | Inhibition of human recombinant full length carbonic hydrase 6 by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies. |
| AID1287518 | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13. |
| AID1808982 | Inhibition of human carbonic anhydrase 5B by stopped-flow CO2 hydration assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors. |
| AID1394917 | Inhibition of membrane bound human carbonic anhydrase 4 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors. |
| AID1185073 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Carbonic anhydrase inhibitors: design, synthesis, and biological evaluation of novel sulfonyl semicarbazide derivatives. |
| AID759698 | Inhibition of Trypanosoma cruzi carbonic anhydrase preincubated for 15 mins to 6 hrs by CO2 hydration stopped-flow assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | A class of sulfonamides with strong inhibitory action against the α-carbonic anhydrase from Trypanosoma cruzi. |
| AID1140121 | Inhibition of human carbonic anhydrase 9-mediated CO2 hydration preincubated for 15 mins by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity. |
| AID1660021 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins by stopped-flow CO2 hydration assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. |
| AID468533 | Inhibition of tumor associated human recombinant CA12 catalytic domain by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Carbonic anhydrase inhibitors; fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II. |
| AID474210 | Inhibition of human recombinant CA12 by stopped flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID1251973 | Inhibition of human carbonic anhydrase 2 incubated for 6 hrs by stopped flow carbon-di-oxide hydrase assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Click-tailed coumarins with potent and selective inhibitory action against the tumor-associated carbonic anhydrases IX and XII. |
| AID369271 | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. |
| AID238957 | Inhibitory activity against human carbonic anhydrase I at 0.09 uM | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID1256866 | Selectivity ratio, ratio of Ki for human carbonic anahydrase-9 to Ki for carbonic anhydrase-14 | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors. |
| AID195088 | Inhibitor level in red blood cells after 2 hours of administration. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. |
| AID1387632 | Inhibition of recombinant human carbonic anhydrase 2 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines. |
| AID1518920 | Inhibition of recombinant human carbonic anhydrase 1 at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID314815 | Inhibition of human carbonic anhydrase 9 in presence of 10 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1172257 | Selectivity index, ratio of Ki for human full length CA2 to Ki for human recombinant CA12 catalytic domain | 2014 | Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22 | Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. |
| AID1585351 | Inhibition of recombinant human carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID1266247 | Inhibition of human carbonic anhydrase-12 preincubated for 15 mins by stopped flow CO2 dehydration method | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies. |
| AID1161956 | Inhibition of Legionella pneumophila carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID1707344 | Inhibition of recombinant human carbonic anhydrase 4 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors. |
| AID166653 | Tested in vitro for transcorneal accession rates (corneal permeability) against cornea with no epithelium | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects. |
| AID254240 | Inhibitory activity against human cloned Carbonic anhydrase I by the CO2 hydration method | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides. |
| AID493883 | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID382944 | Solubility in citric acid-Na2HPO4 buffer at pH 4.12 in presence of 0.0604 mol/l hydroxypropyl-beta-cyclodextrin | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1193927 | Inhibition of human recombinant CA-7 after 15 mins by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. |
| AID437757 | Inhibition of human recombinant CA1 by stopped-flow hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. |
| AID620654 | Reduction in CA12 mRNA level in ca9/ca12 double silenced human LS 174T cells under hypoxia at 60 uM after 48 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID314805 | Inhibition of human carbonic anhydrase 9 catalytic domain in presence of 0.10 mM tris-(carboxyethyl)-phosphine | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1235246 | Inhibition of human CA1 after 15 mins by stopped-flow/Co2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Cloning, characterization and anion inhibition studies of a new γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis. |
| AID1623424 | Inhibition of human carbonic anhydrase 1 assessed as reduction in CO2 hydration after 15 mins by phenol red staining-based stopped flow assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment. |
| AID1195370 | Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides. |
| AID1255573 | Inhibition of human recombinant carbonic anhydrase 9 expressed in Escherichia coli preincubated for 6 hrs by stopped flow CO2 hydrase assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Isatin-pyrazole benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase isoforms IX and XII. |
| AID1709148 | Inhibition of recombinant human carbonic anhydrase 9 by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | 3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation. |
| AID424445 | Inhibition of Candida albicans recombinant Carbonic anhydrase pre-incubated for 15 mins by CO2 hydration stopped-flow assay | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. |
| AID752644 | Inhibition of Sachcharomyces cerevisiae beta carbonic anhydrase after 15 mins by stopped-flow CO2 hydrase assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Carbonic anhydrase inhibitors. Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase. |
| AID1849577 | Inhibition of human recombinant CA9 incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID1335033 | Inhibition of human recombinant cytosolic carbonic anhydrase 2 preincubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | 5-Substituted-benzylsulfanyl-thiophene-2-sulfonamides with effective carbonic anhydrase inhibitory activity: Solution and crystallographic investigations. |
| AID753463 | Inhibition of GST-tagged recombinant carbonic anhydrase-9 catalytic domain (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening. |
| AID1857416 | Inhibition of human recombinant CA5B assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID1291094 | Inhibition of recombinant Candida glabrata beta carbonic anhydrase NCE103 expressed in Escherichia coli preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID48121 | Inhibitory activity against bovine carbonic anhydrase IV (CA4), obtained from bovine lung microsomes | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
| AID1564426 | Inhibition of recombinant human CA9 at 10'-9 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1771793 | Inhibition of recombinant human CA1 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action. |
| AID1308826 | Inhibition of human recombinant carbonic anhydrase 6 expressed in Escherichia coli BL21 (DE3) by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | An Unusual Natural Product Primary Sulfonamide: Synthesis, Carbonic Anhydrase Inhibition, and Protein X-ray Structures of Psammaplin C. |
| AID616468 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins at pH 7.5 by stopped flow CO2 hydration method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases. |
| AID47901 | Inhibitory activity against Human carbonic anhydrase II | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties. |
| AID1142838 | Inhibition of Helicobacter pylori carbonic anhydrase by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11 | Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila. |
| AID732711 | Binding affinity to human recombinant CA7 at 37 degC and pH 7.0 by thermal shift assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | 4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII. |
| AID1809106 | Selectivity ratio of IC50 for recombinant human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate to IC50 for recombinant human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate | 2021 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 51 | Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis. |
| AID475175 | inhibition of Candida albicans recombinant Nce103 after 15 mins by stopped-flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | Carbonic anhydrase inhibitors. The beta-carbonic anhydrases from the fungal pathogens Cryptococcus neoformans and Candida albicans are strongly inhibited by substituted-phenyl-1H-indole-5-sulfonamides. |
| AID48301 | Inhibitory activity against human carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered. |
| AID428368 | Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID437833 | Inhibition of human full length cytosolic carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay | 2009 | Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19 | Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. |
| AID48126 | Inhibitory effect on bovine Carbonic anhydrase IV | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. |
| AID496913 | Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1593067 | Inhibition of human CA 9 catalytic domain | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines. |
| AID300871 | Selectivity ratio of Ki for human cloned CA1 to Ki for human cloned catalytic domain CA9 | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety. |
| AID620792 | Cytotoxicity against CA9-deficient chinese hamster PS120 cells assessed as cell viability at 60 uM and pH 7.5 after 24 hrs by giemsa staining | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. |
| AID1355473 | Inhibition of recombinant human CA4 preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | 4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors. |
| AID47748 | Inhibitory activity of compound against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. |
| AID1237481 | Inhibition of Flaveria bidentis carbonic anhydrase-1 by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID766611 | Inhibition of recombinant human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18 | Synthesis of novel acridine and bis acridine sulfonamides with effective inhibitory activity against the cytosolic carbonic anhydrase isoforms II and VII. |
| AID47930 | Inhibition against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase. |
| AID1818309 | Selectivity index, ratio of Ki for inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay to Ki for inhibition of human CA9 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assa | |||
| AID321157 | Inhibition of human recombinant CA2 by CO2 hydration stopped flow assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID1511294 | Inhibition of human carbonic anhydrase 9 assessed as reduction in CO2 hydration preincubated for 15 mins to 2 hrs by phenol red dye based stopped flow CO2 hydrase assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID166955 | In vitro transcorneal accession rate in rabbit corneal intact epithelium | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action. |
| AID1202643 | Inhibition of human cytosolic form of carbonic anhydrase-1 assessed as CO2 hydration activity incubated for 15 mins prior to testing by stopped flow method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis, carbonic anhydrase inhibition and cytotoxic activity of novel chromone-based sulfonamide derivatives. |
| AID1373182 | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 6 expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID228500 | Ocular sensitization assay as susceptibility to nucleophilic attack by cysteine | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1849587 | Inhibition of human CA2 using 4-nitrophenylacetate as substrate by spectrophotometrical analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID48114 | Inhibitory activity against bovine carbonic anhydrase IV was determined | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. |
| AID1727538 | Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion. |
| AID1373185 | Binding affinity to recombinant human carbonic anhydrase 12 (1 to 260 residues) expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID1560581 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors. |
| AID409949 | Inhibition of human liver MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1254156 | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22 | New natural product carbonic anhydrase inhibitors incorporating phenol moieties. |
| AID1824503 | Inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Synthesis, biological evaluation, and in silico studies of potential activators of apoptosis and carbonic anhydrase inhibitors on isatin-5-sulfonamide scaffold. |
| AID1182981 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Synthesis of sulfonamides with effective inhibitory action against Porphyromonas gingivalis γ-carbonic anhydrase. |
| AID1520085 | Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms. |
| AID316061 | Inhibition of human recombinant full length carbonic hydrase 2 by stopped-flow assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). |
| AID588187 | Inhibition of human recombinant alpha-carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Natural product-based phenols as novel probes for mycobacterial and fungal carbonic anhydrases. |
| AID1077012 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 12 | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII. |
| AID730373 | Inhibition of human cytosolic carbonic anhydrase-2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Kinetic and anion inhibition studies of a β-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis. |
| AID48091 | Inhibitory activity against human carbonic anhydrase II. | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates. |
| AID50191 | Inhibition concentration by inhibition of carbonic anhydrase from kidney in Rat | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8 | Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives. |
| AID757571 | Inhibition of carbonic anhydrase 9 protein expression in human U373 cells under hypoxic conditions treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID47732 | 50% inhibition of human carbonic anhydrase II assayed by CO2 hydration catalyzed by human erythrocytes | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity. |
| AID1061034 | Inhibition of human CA9 preincubated for 15 mins by stopped-flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: solution and X-ray crystallographic studies. |
| AID1161952 | Inhibition of Porphyromonas gingivalis beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Anion inhibition study of the β-class carbonic anhydrase (PgiCAb) from the oral pathogen Porphyromonas gingivalis. |
| AID757568 | Inhibition of carbonic anhydrase 9 protein expression in human U87MG cells under normoxic conditions by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1306839 | Inhibition of human carbonic anhydrase 12 preincubated for 6 hrs at 4 degC measured for 10 to 100 secs by stopped-flow carbon dioxide hydration assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Kinetic and X-ray crystallographic investigations of substituted 2-thio-6-oxo-1,6-dihydropyrimidine-benzenesulfonamides acting as carbonic anhydrase inhibitors. |
| AID780320 | Inhibition of human carbonic anhydrase13 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID300867 | Inhibition of human cloned CA1 by CO2 hydration method | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety. |
| AID1691502 | Inhibition of recombinant human carbonic anhydrase 2 incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID238276 | Ki value against human carbonic anhydrase I (hCA I) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? |
| AID1379913 | Inhibition of recombinant human carbonic anhydrase 4 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | 2017 | ACS medicinal chemistry letters, Sep-14, Volume: 8, Issue:9 | Discovery of New Selenoureido Analogues of 4-(4-Fluorophenylureido)benzenesulfonamide as Carbonic Anhydrase Inhibitors. |
| AID1442871 | Inhibition of recombinant human Carbonic anhydrase 12 assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action. |
| AID603067 | Inhibition of human recombinant cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12 | Conformational variability of different sulfonamide inhibitors with thienyl-acetamido moieties attributes to differential binding in the active site of cytosolic human carbonic anhydrase isoforms. |
| AID1723518 | Apparent permeability across apical to basolateral side in human Caco2 cells | |||
| AID1312161 | Inhibition of Drosophila melanogaster beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Bortezomib inhibits bacterial and fungal β-carbonic anhydrases. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1511298 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 12 | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors. |
| AID1360099 | Inhibition of human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and X-ray crystallography of selenides bearing benzenesulfonamide moiety with neuropathic pain modulating effects. |
| AID1771796 | Inhibition of recombinant human CA7 pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action. |
| AID314825 | Inhibition of human carbonic anhydrase 2 in presence of 0.25 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1158141 | Selectivity ratio of Ki for human recombinant carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 12 | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties. |
| AID1879883 | Selectivity ratio of Ki for inhibition of human recombinant carbonic anhydrase 2 to Ki for inhibition of human recombinant carbonic anhydrase 9 | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases. |
| AID650295 | Inhibition of human cloned carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases. |
| AID725595 | Inhibition of human CA1 by stopped-flow assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors. |
| AID328976 | Inhibition of human full length carbonic anhydrase 3 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID47729 | 50% inhibitory concentration against human carbonic anhydrase II (HCA II) after pre-incubation for 4 min at 37 degree C | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma. |
| AID271710 | Inhibition of human cloned CA1 by CO2 hydration method | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". |
| AID271040 | Inhibition of human cloned CA12 catalytic domain by CO2 hydration assay | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors. |
| AID1058393 | Inhibition of Methanobacterium thermoautotrophicum beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens. |
| AID1758421 | Inhibition of human CA1 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides. |
| AID1243121 | Inhibition of human carbonic anhydrase 12 at 10'-8 M preincubated for 15 mins by stopped flow CO2 hydration method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID238773 | Binding affinity towards human cloned carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties. |
| AID365987 | Inhibition of human cloned CA12 catalytic domain by stopped-flow CO2 hydration method | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15 | Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. |
| AID237406 | Compound level in Red Blood Cells at 60 min, after exposure of 10 mL of Blood to compound solution by HPLC method | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors. |
| AID264312 | Inhibition of human CA9 | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. |
| AID342479 | Inhibition of human carbonic anhydrase 5A by stopped-flow CO2 hydration assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. |
| AID749809 | Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine. |
| AID1578353 | Inhibition of recombinant human CA1 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors. |
| AID1356464 | Binding affinity to human carbonic anhydrase 12 by stopped flow CO2 hydration method | 2018 | ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7 | Targeting Tumor Associated Carbonic Anhydrases IX and XII: Highly Isozyme Selective Coumarin and Psoralen Inhibitors. |
| AID342467 | Inhibition of AQP4 expressed in rat FRT cells assessed as osmotic water permeability at 100 uM after 15 mins by stopped-flow light scattering method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides. |
| AID417829 | Inhibition of human recombinant full length CA5A by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID551578 | Inhibition of Candida albicans recombinant beta-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Inhibition of β-carbonic anhydrases with ureido-substituted benzenesulfonamides. |
| AID1686866 | Inhibition of recombinant human carbonic anhydrase 2 by stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID474207 | Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. |
| AID730519 | Inhibition of Sulfurihydrogenibium azorense carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay | 2013 | Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6 | An α-carbonic anhydrase from the thermophilic bacterium Sulphurihydrogenibium azorense is the fastest enzyme known for the CO2 hydration reaction. |
| AID1809980 | Cytotoxicity against HCEC cells assessed as cell viability at 2 % by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 53 | Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors. |
| AID601815 | Inhibition of human carbonic anhydrase 7 preincubated with compound for 15 mins by carbon dioxide hydration assay | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV. |
| AID382978 | Solubility in water in presence of 0.2 M hydroxypropyl-beta-cyclodextrin and 0.34 M triethanolamine | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex. |
| AID1194028 | Inhibition of recombinant Nostoc commune gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune. |
| AID417836 | Inhibition of human recombinant full length CA14 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1519763 | Inhibition of recombinant human carbonic anhydrase-12 at 1 nM after 15 mins by stopped flow CO2 hydrase assay (Rvb = 0%) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. |
| AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID646247 | Inhibition of S-glutathionylated form of human recombinant carbonic anhydrase 7 hydrolysis activity using 4-nitrophenyl acetate as substrate preincubated for 10 mins prior to substrate addition by stopped flow cytometry | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID1230147 | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies. |
| AID1360943 | Binding affinity to human carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors. |
| AID1755144 | Inhibition of recombinant human CA7 incubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Design, synthesis and biochemical evaluation of novel carbonic anhydrase inhibitors triggered by structural knowledge on hCA VII. |
| AID1335035 | Inhibition of human recombinant transmembrane tumor associated carbonic anhydrase 12 preincubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | 5-Substituted-benzylsulfanyl-thiophene-2-sulfonamides with effective carbonic anhydrase inhibitory activity: Solution and crystallographic investigations. |
| AID1422969 | Inhibition of recombinant human CA7 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Famotidine, an Antiulcer Agent, Strongly Inhibits |
| AID752642 | Selectivity ratio of Ki for Sachcharomyces cerevisiae beta carbonic anhydrase to Ki for human carbonic anhydrase-1 | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Carbonic anhydrase inhibitors. Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase. |
| AID1555968 | Inhibition of human carbonic anhydrase 12 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects. |
| AID764717 | Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety. |
| AID1170167 | Inhibition of human carbonic anhydrase 4 at pH7 and 37 degC by fluorescent thermal shift assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX. |
| AID244127 | Ratio of Ki for human carbonic anhydrases II and IX | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties. |
| AID299240 | Ratio of kcat to Km of Helicobacter pylori alpha CA | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13 | Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors. |
| AID1468999 | Binding affinity to human full length His-tagged CA2 (1 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic dissociation rate constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID753462 | Selectivity ratio of IC50 for full length carbonic anhydrase-1 in human erythrocytes to IC50 for GST-tagged recombinant carbonic anhydrase-9 catalytic domain (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening. |
| AID757588 | Inhibition of carbonic anhydrase 9 protein expression in human U251 cells under hypoxic conditions at 4000 nM treated prior to hypoxic-challenge followed by compound addition 12 hrs after first treatment by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Hypoxia induced CA9 inhibitory targeting by two different sulfonamide derivatives including acetazolamide in human glioblastoma. |
| AID1585354 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 1 to Ki for recombinant human carbonic anhydrase 9 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. |
| AID327760 | Inhibition of human full length carbonic anhydrase 3 by stopped flow CO2 hydrase assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. |
| AID1692097 | Inhibition of human erythrocyte CA2 using 4-nitrophenyl acetate as substrate by Lineweaver-Burk plot analysis | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate. |
| AID770581 | Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 9 | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. |
| AID1237476 | Inhibition of Cryptococcus neoformans carbonic anhydrase-2 by CO2 hydration reaction based colorimetric stopped-flow method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa. |
| AID239102 | Inhibitory constant against catalytic domain of human carbonic anhydrase IX | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. |
| AID243011 | Selectivity ratio against human carbonic anhydrases II and XII | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? |
| AID1518928 | Inhibition of recombinant human carbonic anhydrase 2 at 0.01 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1652402 | Inhibition of human CA2 pre-incubated for 15 mins by stopped flow CO2 hydrase assay | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors. |
| AID1518919 | Inhibition of recombinant human carbonic anhydrase 1 assessed as residual activity at 10 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID233702 | Selectivity ratio, inhibition (Ki) of human carbonic anhydrase IX compared to human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered. |
| AID1446112 | Antiproliferative activity against human HT-29 cells assessed as cell viability at 30 uM after 48 hrs under hypoxic conditions by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. |
| AID1565739 | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration at 10'-6 M incubated for 15 mins by phenol red dye based stopped flow assay relative to control (Rvb = 0 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation. |
| AID238211 | Inhibitory constant against human Carbonic anhydrase I | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds. |
| AID1061892 | Inhibition of Sulfurihydrogenibium azorense alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Inhibition of carbonic anhydrases from the extremophilic bacteria Sulfurihydrogenibium yellostonense (SspCA) and S. azorense (SazCA) with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophe |
| AID484165 | Inhibition of full length human carbonic anhydrase 14 preincubated for 15 mins by CO2 hydration stopped-flow assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. |
| AID1373180 | Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5A expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. |
| AID300760 | Selectivity for human CA12 over human CA1 | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides. |
| AID1474382 | Cytotoxicity against human HT-29 cells assessed as cell viability at 100 uM after 72 hrs under normoxic condition by MTT assay relative to control | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. |
| AID166952 | Compound was tested in vitro for corneal permeability of compound across the intact cornea obtained from rabbit | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring? |
| AID321161 | Selectivity for human CA9 over human CA2 | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. |
| AID1331200 | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli assessed as reduction in CO2 hydration preincubated for 15 mins prior to testing measured for 10 to 100 secs by stopped-flow assay | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1 | Microwave assisted synthesis of novel tetrazole/sulfonamide derivatives based on octahydroacridine, xanthene and chromene skeletons as inhibitors of the carbonic anhydrases isoforms I, II, IV and VII. |
| AID1410857 | Inhibition of human CA9 assessed as enzyme inhibitor complex formation preincubated for 15 mins and measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydrase assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Discovery of 4-Hydroxy-3-(3-(phenylureido)benzenesulfonamides as SLC-0111 Analogues for the Treatment of Hypoxic Tumors Overexpressing Carbonic Anhydrase IX. |
| AID1453413 | Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | |||
| AID1649853 | Inhibition of human CA9 preincubated for 15 mins by stopped-flow carbon dioxide hydration assay | |||
| AID648180 | Inhibition of human wild type carbonic anhydrase 2 Gln92Val mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors. |
| AID257065 | Inhibition of cloned human transmembrane, tumor-associated isozyme CA IX | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID496916 | Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration method | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. |
| AID1334829 | Inhibition of human recombinant carbonic anhydrase-9 preincubated for 6 hrs by stopped-flow CO2 hydration assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID678520 | Inhibition of Cryptococcus neoformans beta carbonic anhydrase Can2 using CO2 as substrate incubated for 6 hrs prior to substrate addition measured for 10 to 100 secs by stopped flow technique | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Inhibition of α-class cytosolic human carbonic anhydrases I, II, IX and XII, and β-class fungal enzymes by carboxylic acids and their derivatives: new isoform-I selective nanomolar inhibitors. |
| AID311024 | Inhibition of human carbonic anhydrase 2 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1468996 | Binding affinity to human full length His-tagged CA2 (1 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as association rate constant after 60 secs at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID1686867 | Inhibition of recombinant human carbonic anhydrase 7 by stopped-flow CO2 hydration assay | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation. |
| AID1312217 | Inhibition of Helicobacter pylori recombinant alpha-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Anion inhibition profiles of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum. |
| AID1691508 | Selectivity ratio of Ki for inhibition of recombinant human CA2 to Ki for inhibition of recombinant human CA12 | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes. |
| AID577528 | Inhibition of human carbonic anhydrase VA by spectrophotometry at pH 7.5 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. |
| AID1152899 | Inhibition of human recombinant carbonic anhydrase 1 pretreated for 15 mins by stopped flow CO2 hydrase assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12 | Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors. |
| AID1243105 | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. |
| AID1310852 | Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins prior to testing by stopped-flow CO2 hydration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | PEGylated Bis-Sulfonamide Carbonic Anhydrase Inhibitors Can Efficiently Control the Growth of Several Carbonic Anhydrase IX-Expressing Carcinomas. |
| AID1518937 | Inhibition of recombinant human carbonic anhydrase 12 assessed as residual activity at 1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID1275624 | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms. |
| AID1278413 | Inhibition of recombinant Colwellia psychrerythraea gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea. |
| AID1468994 | Binding affinity to human CA9 catalytic domain expressed in mammalian expression system assessed as thermodynamic equilibrium constant at pH 7 by SPR assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design. |
| AID590766 | Inhibition of human carbonic anhydrase 2 after 6 hrs by Lineweaver-Burk plot analysis | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Virtual screening-driven identification of human carbonic anhydrase inhibitors incorporating an original, new pharmacophore. |
| AID1709147 | Inhibition of recombinant human carbonic anhydrase 2 by stopped flow CO2 hydrase assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | 3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation. |
| AID1857413 | Inhibition of human recombinant CA2 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. |
| AID1902657 | Selectivity ratio of Ki for for inhibition of recombinant human CA 2 to Ki for inhibition of recombinant human CA 9 | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
| AID50362 | Compound was evaluated for inhibition against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. |
| AID470873 | Inhibition of carbonic anhydrase 2 assessed as inhibition of carbon dioxide hydration | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | A QSAR study on relationship between structure of sulfonamides and their carbonic anhydrase inhibitory activity using the eigenvalue (EVA) method. |
| AID1291096 | Selectivity ratio of Ki for recombinant human carbonic anhydrase 2 expressed in Escherichia coli to Ki for recombinant Candida glabrata beta carbonic anhydrase NCE103 expressed in Escherichia coli | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes. |
| AID229677 | Selectivity ratio towards hCA IX as compared to hCA II | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates. |
| AID1504707 | Inhibition of Cryptococcus neoformans Can2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study. |
| AID314831 | Inhibition of human carbonic anhydrase 2 in presence of 10 mM threitol | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX. |
| AID1306525 | Inhibition of Helicobacter pylori alpha carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydrase assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Anion inhibition profiles of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae. |
| AID1517567 | Inhibition of human carbonic anhydrase 9 at 10'-6 M incubated for 10 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID1517552 | Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs under hypoxic condition by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies. |
| AID428366 | Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID328985 | Inhibition of human full length carbonic anhydrase 14 | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 | Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. |
| AID1706622 | Inhibition of human CA12 preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. |
| AID514211 | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity. |
| AID1564422 | Inhibition of recombinant human CA2 at 10'-9 M preincubated for 15 mins by phenol red dye-based stopped-flow CO2 hydration assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment. |
| AID1757213 | Inhibition of human CA12 by stopped- flow CO2 hydration assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. |
| AID1161930 | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration method | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Discovery of a new family of carbonic anhydrases in the malaria pathogen Plasmodium falciparum--the η-carbonic anhydrases. |
| AID1537864 | Inhibition of recombinant human carbonic anhydrase 9 expressed in Escherichia coli GOLD BL21 (DE3) by stopped-flow CO2 hydration assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma. |
| AID1194026 | Inhibition of recombinant Methanosarcina thermophila gamma-carbonic anhydrase by stopped flow CO2 hydrase assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune. |
| AID1849540 | Binding affinity to human CA2 assessed as inhibition constant using p-Nitrophenylacetate as substrate by SDS-PAGE analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. |
| AID417833 | Inhibition of human recombinant CA9 catalytic domain by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. |
| AID1076060 | Inhibition of human recombinant carbonic anhydrase 9-mediated CO2 hydration after 6 hrs by stopped-flow assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | 6-Triazolyl-substituted sulfocoumarins are potent, selective inhibitors of the tumor-associated carbonic anhydrases IX and XII. |
| AID1518939 | Inhibition of recombinant human carbonic anhydrase 12 at 0.1 uM preincubated for 15 mins by phenol red dye based stopped flow CO2 hydration assay (Rvb = 0%) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. |
| AID446435 | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli by stopped-flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors. |
| AID1731966 | Inhibition of MMP9 (unknown origin) using Mca-Lys-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 5 min followed by substrate addition and measured for 30 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 1996 | Biochemistry, Mar-19, Volume: 35, Issue:11 | Reversal of the hydrogen bond to zinc ligand histidine-119 dramatically diminishes catalysis and enhances metal equilibration kinetics in carbonic anhydrase II. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 1996 | Biochemistry, Mar-19, Volume: 35, Issue:11 | Reversal of the hydrogen bond to zinc ligand histidine-119 dramatically diminishes catalysis and enhances metal equilibration kinetics in carbonic anhydrase II. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 1995 | Biochemistry, Mar-28, Volume: 34, Issue:12 | Structural basis of inhibitor affinity to variants of human carbonic anhydrase II. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 1995 | Biochemistry, Mar-28, Volume: 34, Issue:12 | Structural basis of inhibitor affinity to variants of human carbonic anhydrase II. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2009 | Biochemistry, Feb-17, Volume: 48, Issue:6 | Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer properties. |
| AID1345928 | Human carbonic anhydrase 1 (4.2.1.1 Carbonate dehydratases) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? |
| AID1346210 | Human carbonic anhydrase 12 (4.2.1.1 Carbonate dehydratases) | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1346003 | Human carbonic anhydrase 4 (4.2.1.1 Carbonate dehydratases) | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX. |
| AID1346210 | Human carbonic anhydrase 12 (4.2.1.1 Carbonate dehydratases) | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? |
| AID1346166 | Mouse carbonic anhydrase 13 (4.2.1.1 Carbonate dehydratases) | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1345928 | Human carbonic anhydrase 1 (4.2.1.1 Carbonate dehydratases) | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1345957 | Human carbonic anhydrase 14 (4.2.1.1 Carbonate dehydratases) | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties. |
| AID1346202 | Human carbonic anhydrase 7 (4.2.1.1 Carbonate dehydratases) | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1346003 | Human carbonic anhydrase 4 (4.2.1.1 Carbonate dehydratases) | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1345957 | Human carbonic anhydrase 14 (4.2.1.1 Carbonate dehydratases) | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. |
| AID1345928 | Human carbonic anhydrase 1 (4.2.1.1 Carbonate dehydratases) | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Acetazolamide-based fungal chitinase inhibitors. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2012 | Journal of the American Chemical Society, Sep-12, Volume: 134, Issue:36 | Neutron diffraction of acetazolamide-bound human carbonic anhydrase II reveals atomic details of drug binding. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 1997 | Biochemistry, Dec-16, Volume: 36, Issue:50 | Histidine --> carboxamide ligand substitutions in the zinc binding site of carbonic anhydrase II alter metal coordination geometry but retain catalytic activity. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 1997 | Biochemistry, Dec-16, Volume: 36, Issue:50 | Histidine --> carboxamide ligand substitutions in the zinc binding site of carbonic anhydrase II alter metal coordination geometry but retain catalytic activity. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2009 | Acta crystallographica. Section F, Structural biology and crystallization communications, Oct-01, Volume: 65, Issue:Pt 10 | High-resolution structure of human carbonic anhydrase II complexed with acetazolamide reveals insights into inhibitor drug design. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2007 | Chemistry & biology, May, Volume: 14, Issue:5 | Structure of Saccharomyces cerevisiae chitinase 1 and screening-based discovery of potent inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2009 | Proteins, Jan, Volume: 74, Issue:1 | Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 3510 (48.76) | 18.7374 |
| 1990's | 1030 (14.31) | 18.2507 |
| 2000's | 990 (13.75) | 29.6817 |
| 2010's | 1294 (17.97) | 24.3611 |
| 2020's | 375 (5.21) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (108.64) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 495 (6.51%) | 5.53% |
| Reviews | 379 (4.98%) | 6.00% |
| Case Studies | 868 (11.42%) | 4.05% |
| Observational | 12 (0.16%) | 0.25% |
| Other | 5,850 (76.93%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Randomized Controlled Trial of N-acetylcysteine and Acetazolamide in Treatment of Chronic Mountain Sickness [NCT01187108] | Phase 1/Phase 2 | 85 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
| Acetazolamide for Treating NPH in Shunt-candidates Patients: an Open Label Feasibility Trial [NCT03779594] | Phase 2 | 15 participants (Anticipated) | Interventional | 2018-12-31 | Recruiting | ||
| Cerebrovascular Reserve and White Matter Disease in Patients With Chronic Anemia [NCT03715972] | 165 participants (Actual) | Observational | 2018-07-15 | Completed | |||
| Acetazolamide and Hydrochlorothiazide Followed by Furosemide Versus Hydrochlorothiazide and Furosemide Followed by Furosemide for the Treatment of Adults With Refractory Nephrotic Edema: A Randomized, Double-Blind Trial [NCT02427880] | Phase 4 | 20 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| Effect of Acetazolamide on Sleep Related Breathing Disturbances in Patients With Chronic Obstructive Pulmonary Disease at Altitude, Assessed by Respiratory Polygraphy: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03177850] | Phase 4 | 185 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Effect of Acetazolamide on Right Heart Function at Rest in Lowlanders Older Than 40 Years at Altitude.: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03540914] | Phase 4 | 400 participants (Anticipated) | Interventional | 2018-06-01 | Active, not recruiting | ||
| Randomized Trial of Medical Therapy (MT) vs. MT Plus Optic Nerve Sheath Fenestration vs. MT Plus Ventriculoperitoneal Cerebrospinal Fluid Shunting in Subjects With Idiopathic Intracranial Hypertension and Moderate to Severe Visual Loss [NCT03501966] | Phase 3 | 7 participants (Actual) | Interventional | 2019-02-06 | Terminated(stopped due to Low enrollment) | ||
| A Phase II/III, Randomised, Double-Blind Clinical Trial to Determine the Safety and Efficacy of IHL-42X in Subjects With Obstructive Sleep Apnoea Who Are Intolerant, Non-Compliant, or Naïve to Positive Airway Pressure [NCT06146101] | Phase 2/Phase 3 | 560 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
| Diuretic Strategies in Acute Heart Failure Patients at High Risk for Diuretic Resistance (P-Value-AHF): A Multicentre, Randomized, Parallel-group, Open-label Trial [NCT05986773] | Phase 4 | 75 participants (Anticipated) | Interventional | 2023-10-10 | Recruiting | ||
| A Randomised Four-Period Cross-Over Phase I Study to Assess Bioavailability, Bioequivalence and Tolerability of IHL-42X Compared to the Reference Drugs in Healthy Volunteers [NCT05857384] | Phase 1 | 116 participants (Anticipated) | Interventional | 2023-09-08 | Recruiting | ||
| Short Term Intraocular Pressure Fluctuations After Intravitreal Bevacizumab Injection: the Effect of Pretreatment With Antiglaucoma Agents [NCT02140450] | 70 participants (Actual) | Interventional | 2012-02-29 | Completed | |||
| [NCT02090738] | Phase 2 | 0 participants (Actual) | Interventional | 2014-03-31 | Withdrawn | ||
| D-dimer and the Use of Anticoagulation in IIH [NCT03963336] | Early Phase 1 | 48 participants (Actual) | Interventional | 2017-07-22 | Completed | ||
| Acetazolamide Per os for Decompensation of Heart Failure [NCT05802849] | Phase 4 | 400 participants (Anticipated) | Interventional | 2023-05-01 | Recruiting | ||
| Acetazolamide and Tubuloglomerular Feedback in Persons With Type 1 Diabetes: A Clinical Trial [NCT05473364] | Phase 1/Phase 2 | 12 participants (Anticipated) | Interventional | 2023-03-20 | Recruiting | ||
| Influences of Acetazolamide on Endurance Exercise Performance and Cognitive Function During Acute Exposure to Hypobaric Hypoxia [NCT03525561] | Early Phase 1 | 10 participants (Actual) | Interventional | 2018-10-10 | Completed | ||
| Effect of Acetazolamide on Visuomotor Learning Performance in Patients With Chronic Obstructive Pulmonary Disease at Altitude [NCT03165890] | Phase 4 | 78 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Non-inferiority Prospective Randomized Trial of Acetazolamide Versus Diazepam in Patients With Continuous Spike and Wave in Sleep (CSWS)/Landau Kleffner Syndrome (LKS) [NCT02904265] | Phase 2/Phase 3 | 3 participants (Actual) | Interventional | 2016-09-30 | Terminated(stopped due to Lack of enrollment) | ||
| Physiological Study to Predict Successful Sleep Apnea Treatment With Acetazolamide in Heart Failure Patients [NCT01377987] | 29 participants (Actual) | Interventional | 2011-08-31 | Completed | |||
| Acetazolamide as a Means to Mitigate Falling Ventilatory Drive and Drive-dependent OSA [NCT06091085] | Phase 1/Phase 2 | 36 participants (Anticipated) | Interventional | 2023-11-01 | Not yet recruiting | ||
| [NCT02163330] | Phase 3 | 2 participants (Actual) | Interventional | 2014-06-30 | Terminated(stopped due to difficulty in recruiting participants to the study) | ||
| Acetazolamide for Prevention of Acute Mountain Sickness in Healthy Lowlanders Older Than 40 Years. Randomized Trial. [NCT03561675] | Phase 4 | 349 participants (Actual) | Interventional | 2018-05-15 | Completed | ||
| Sickness Evaluation at Altitude With Acetazolamide at Relative Dosages [NCT03424226] | Phase 1 | 105 participants (Actual) | Interventional | 2018-08-04 | Completed | ||
| A Multi-center, Randomized, Double-blind, Phase IV Clinical Trial on the Diuretic Effects of Acetazolamide in Patients With Decompensated Heart Failure and Volume OveRload [NCT03505788] | Phase 4 | 519 participants (Actual) | Interventional | 2018-11-11 | Completed | ||
| Targeting Carbonic Anhydrase Mediated Coupling as a Novel Vasospasm Prophylaxis in Aneurysmal Sub Arachnoid Hemorrhage [NCT02165644] | Phase 2 | 0 participants (Actual) | Interventional | 2015-09-30 | Withdrawn(stopped due to The PI is leaving the University of Florida.) | ||
| Stop Retinal Ganglion Cell Dysfunction Study [NCT02390284] | Phase 3 | 500 participants (Anticipated) | Interventional | 2015-09-30 | Active, not recruiting | ||
| Phase I Trial of Carbonic Anhydrase Inhibition Associated With Platinum-based Chemotherapy and Etoposide in Concomitance With Radiotherapy in Localized Small Cell Lung Carcinomas [NCT03467360] | Phase 1 | 30 participants (Anticipated) | Interventional | 2019-08-02 | Recruiting | ||
| Prospective Analysis Between Acetazolamide vs Placebo in Patients With Acute Heart Failure [NCT03720288] | Phase 3 | 90 participants (Anticipated) | Interventional | 2018-10-01 | Recruiting | ||
| Acetazolamide Facilitates Ventilator Weaning Multicenter, Prospective, Double Blinded, Randomised Controlled Trial [NCT01131377] | 150 participants (Anticipated) | Interventional | 2010-05-31 | Recruiting | |||
| Acetazolamide (AZ) for Management of Refractory Hypokalemia Metabolic Alkalosis in Bartter Syndrome [NCT03847571] | 20 participants (Anticipated) | Observational | 2019-01-10 | Recruiting | |||
| A Multicenter, Double-blind, Randomized, Placebo-controlled Study of Weight-Reduction and/or Low Sodium Diet Plus Acetazolamide vs Diet Plus Placebo in Subjects With Idiopathic Intracranial Hypertension With Mild Visual Loss [NCT01003639] | Phase 2/Phase 3 | 165 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Effect of Acetazolamide and Methazolamide on Hypoxic Exercise Performance [NCT05575180] | Phase 4 | 15 participants (Anticipated) | Interventional | 2023-08-11 | Recruiting | ||
| A Phase I Study of Safety and Tolerability of Acetazolamide With Temozolomide in Adults With Newly Diagnosed MGMT Promoter-Methylated IDH Wildtype Glioblastoma [NCT03011671] | Phase 1 | 60 participants (Anticipated) | Interventional | 2018-10-03 | Recruiting | ||
| A Single Center, Double-blind, Placebo-controlled Phase I Single-dose Cross-over Study in Healthy Subjects to Investigate the Inhibitory Effect of CG100649, Celecoxib, Naproxen, and Acetazolamide on the Activity of Cyclooxygenases (COX-1, COX-2) and Carbo [NCT00780325] | Phase 1 | 26 participants (Actual) | Interventional | 2008-10-31 | Terminated(stopped due to A total of three parts were planned for this study. The sponsor funded only Part 1, so that neither Part 2 nor Part 3 of this study has been conducted.) | ||
| Augmenting Cerebral Blood Flow to Treat Established Multiple Sclerosis [NCT02466074] | Phase 2 | 5 participants (Actual) | Interventional | 2016-08-17 | Terminated(stopped due to Inadequate recruitment; termination of funding) | ||
| Effect of Acetazolamide on Right Heart Function at Rest in Lowlanders With Chronic Obstructive Pulmunary Disease (COPD) Traveling to High Altitude [NCT04915365] | Phase 3 | 100 participants (Anticipated) | Interventional | 2021-05-01 | Recruiting | ||
| Effect of Acetazolamide on Central Sleep Apnea Related to Opium Consumption [NCT02371473] | Phase 4 | 12 participants (Anticipated) | Interventional | 2014-11-30 | Enrolling by invitation | ||
| Effect of Acetazolamide on Exercise Performance in Patients With Chronic Obstructive Pulmonary Disease at Altitude, Assessed by Maximal Cycling Spiroergometry: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03177837] | Phase 4 | 176 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Carbonic Anhydrase Inhibitors and Carbonation: A Novel Approach to Reduce Soda Consumption [NCT06110078] | Early Phase 1 | 44 participants (Anticipated) | Interventional | 2023-12-01 | Not yet recruiting | ||
| Managing Opioid Related Sleep Apnea With Acetazolamide [NCT06043830] | Phase 2 | 34 participants (Anticipated) | Interventional | 2023-10-18 | Recruiting | ||
| Endotypic Traits and Obstructive Sleep Apnea Surgery [NCT05953610] | Phase 2 | 150 participants (Anticipated) | Interventional | 2023-12-01 | Not yet recruiting | ||
| Central Sleep Apnea: Physiologic Mechanisms to Inform Treatment [NCT04118387] | Phase 4 | 200 participants (Anticipated) | Interventional | 2021-01-07 | Recruiting | ||
| A Short Term Open, Randomized Cross Over Trial Trial Exploring the Effect of Carbonic Anhydrase Inhibition by Acetazolamide on Sleep Apnea Associated Hypertension [NCT02220803] | Phase 2 | 13 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
| The Effect of Carbonic Anhydrase Inhibitors on the Pulmonary System Response to Muscle Fatigue. [NCT02758470] | Phase 4 | 13 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
| Cerebrovascular Reserve Measurements in Sickle Cell Disease: an MRI Study [NCT02824406] | 60 participants (Anticipated) | Observational | 2014-08-31 | Recruiting | |||
| Chronic Clinical Effect of Acetazolamide in Pulmonary Hypertension [NCT02755298] | Phase 2/Phase 3 | 24 participants (Anticipated) | Interventional | 2016-10-31 | Completed | ||
| A Single-center Pilot Study Evaluating the Immediate Effects of Low-dose Acetazolamide on Respiratory Control in Subjects With Treatment Emergent Sleep Disordered Breathing [NCT02670096] | 0 participants (Actual) | Interventional | 2016-01-31 | Withdrawn | |||
| Acute Hemodynamic Effect of Acetazolamide in Pulmonary Hypertension [NCT02755259] | Phase 2/Phase 3 | 33 participants (Actual) | Interventional | 2017-01-01 | Completed | ||
| Therapeutic Trial of Potassium and Acetazolamide in Andersen-Tawil Syndrome [NCT00839501] | Phase 1 | 3 participants (Actual) | Interventional | 2008-12-31 | Terminated(stopped due to Unable to recruit sufficient number of participants) | ||
| Treatment of Orthostatic Intolerance [NCT00262470] | Phase 1/Phase 2 | 150 participants (Anticipated) | Interventional | 1997-04-30 | Active, not recruiting | ||
| Continuous Positive Airway Pressure (CPAP) and Acetazolamide for Treatment of Patients With the Obstructive Sleep Apnea Syndrome at Altitude [NCT00928655] | Phase 4 | 51 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Augmentation of Medical Readiness and Physical Performance at High Altitude Using Pharmacological Countermeasures [NCT05300477] | Phase 4 | 18 participants (Anticipated) | Interventional | 2022-05-27 | Recruiting | ||
| Effect of Acetazolamide on Lung Water Content by Ultrasound in Lowlanders Older Than 40 Years at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03539367] | Phase 4 | 100 participants (Anticipated) | Interventional | 2018-06-01 | Active, not recruiting | ||
| Effect of Acetazolamide on Right Heart Function During Exercise in Lowlanders Older Than 40 Years at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03537924] | Phase 4 | 100 participants (Anticipated) | Interventional | 2018-06-01 | Active, not recruiting | ||
| Treatment of Patients With the Obstructive Sleep Apnea Syndrome at Altitude [NCT00714740] | Phase 4 | 49 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Effectiveness of Oral Acetazolamide, Brimonidine Tartarate, and Anterior Chamber Paracentesis for Ocular Hypertension Control After Intravitreal Bevacizumab Injection: Preliminary Results [NCT00804921] | Phase 2 | 0 participants | Interventional | Completed | |||
| Effectiveness of Oral Acetazolamide, Brimonidine Tartarate, and Anterior Chamber Paracentesis for Ocular Hypertension Control After Intravitreal Bevacizumab Injection [NCT00864838] | Phase 2 | 56 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Pilot Study of Acetazolamide to Prevent Post Operative Cerebrospinal Fluid (CSF) Leak in Patients Undergoing Endoscopic Skull Base Surgery [NCT02902133] | Phase 2 | 0 participants (Actual) | Interventional | 2016-09-01 | Withdrawn(stopped due to No participants were identified per inclusion/exclusion criteria) | ||
| Tadalafil and Acetazolamide Versus Acetazolamide in Acute Mountain Sickness Prevention [NCT01060969] | 55 participants (Actual) | Interventional | 2006-01-31 | Completed | |||
| Acetazolamide as add-on Therapy to Obstructive Sleep Apnea Surgery (ACTOS): a Parallel-group, Double-blind, Placebo-controlled, Randomized Trial [NCT04227093] | Phase 4 | 74 participants (Anticipated) | Interventional | 2020-01-22 | Recruiting | ||
| Novel Approach to Prevention of Altitude-related Illness in Patients With Chronic Obstructive Pulmonary Disease [NCT04913389] | Phase 3 | 100 participants (Anticipated) | Interventional | 2021-06-01 | Active, not recruiting | ||
| Immediate Anterior Chamber Paracentesis With A 30-Gauge Needle for Acute Primary Angle - Closure [NCT01923454] | 15 participants (Actual) | Interventional | 2005-12-31 | Completed | |||
| [NCT00000115] | Phase 2 | 0 participants | Interventional | 1990-12-31 | Completed | ||
| [NCT00517426] | Phase 4 | 20 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| Open Controled Randomized Pilot Study on the Use of Acetazolamide and Dexamethasone for the Acute Phase of Perilesional Edema in Calcified Neurocysticercosis [NCT02945527] | Phase 2/Phase 3 | 4 participants (Actual) | Interventional | 2015-12-04 | Terminated(stopped due to Low recruitment) | ||
| Evaluation of a Compliance Marker A Supplement to: U01DA029580-02 Opioid-Induced Hyperalgesia In Prescription Opioid Abusers: Effects of Pregabalin [NCT02276989] | Phase 2 | 0 participants (Actual) | Interventional | 2014-12-31 | Withdrawn(stopped due to poor recruitment) | ||
| Acetazolamide for Obstructive Sleep Apnea to Improve Heart Health [NCT05616260] | Phase 2 | 46 participants (Anticipated) | Interventional | 2022-12-02 | Recruiting | ||
| Treating Residual OSA With Endotype-directed Pharmacotherapy (Aim 3) [NCT05293600] | Phase 1/Phase 2 | 70 participants (Anticipated) | Interventional | 2022-09-01 | Not yet recruiting | ||
| A Randomised Controlled Trial of the Effectiveness of Acetazolamide in Reducing Cerebrospinal Fluid Pressure for Patients Undergoing Thoracic-abdominal Aortic Repair [NCT01889498] | Phase 4 | 100 participants (Anticipated) | Interventional | 2014-07-31 | Recruiting | ||
| A Single-center, Single-arm, Open, Prospective, and Exploratory Clinical Study on the Efficacy of Acetazolamide Combined With Levamisole in the Treatment of Advanced HCC [NCT04611373] | Phase 3 | 50 participants (Anticipated) | Interventional | 2020-05-01 | Recruiting | ||
| Evaluation and Treatment of Autonomic Failure. [NCT00223691] | Phase 1 | 389 participants (Actual) | Interventional | 2002-03-31 | Completed | ||
| Efficacy of Oral Acetazolamide as Add-on Diuretic Therapy in Decongestion in Patients With Heart Failure and Diuretic Resistance [NCT05940220] | Phase 3 | 130 participants (Anticipated) | Interventional | 2023-12-30 | Not yet recruiting | ||
| Double-blind Randomized Acetazolamide Trial in Normal Pressure Hydrocephalus [NCT04975269] | Phase 2 | 50 participants (Anticipated) | Interventional | 2022-02-17 | Recruiting | ||
| Multizenterstudie Der European Assessment Group for Lysis in the Eye (EAGLE) Zur Behandlung Des Zentralarterienverschlusses (ZAV): Lysetherapie Versus Konservative Therapie [NCT00637468] | Phase 3 | 84 participants (Actual) | Interventional | 2002-09-30 | Terminated(stopped due to Due to results of conditional power analysis performed at the first interim analysis and due to observed spectrum of adverse events.) | ||
| Effect of Acetazolamide and Furosemide on Obesity-induced Glomerular Hyperfiltration [NCT01146288] | 13 participants (Actual) | Interventional | 2010-07-31 | Completed | |||
| Diuretic Treatment in Acute Heart Failure With Volume Overload Guided by Serial Spot Urine Sodium Assessment [NCT05411991] | Phase 4 | 104 participants (Anticipated) | Interventional | 2022-06-12 | Recruiting | ||
| Evaluation of the Effect of Acetazolamide, Mannitol and N-acetylcysteine on Cisplatin-Induced Nephrotoxicity [NCT02760901] | Phase 2 | 52 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
| The Effect of Carbonic Anhydrase Inhibitors on the Pulmonary System Response to Hypoxia [NCT02760121] | Phase 4 | 14 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
| Acetazolamide and Statins for the Treatment of Chronic Mountain Sickness in Highlanders: A Randomized Controlled Trial [NCT04251364] | 60 participants (Anticipated) | Interventional | 2020-02-15 | Recruiting | |||
| Double Blind, Placebo Controlled Randomised Trial of Acetazolamide Versus Placebo in the Prevention of Acute Mountain Sickness During Rapid Ascent [NCT01418157] | Phase 4 | 380 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| Treatment of Sleep Related Breathing Disorders in Patients With Pulmonary Hypertension (CSRPH) [NCT01427192] | Phase 2 | 23 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
| Effect of Acetazolamide in Prevention of Contrast Nephropathy [NCT00634491] | Phase 2 | 240 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
| A Randomized, Double-blind, Placebo-controlled Study Evaluating Acetazolamide Efficacy in Ataxia in PMM2-CDG [NCT04679389] | Phase 2/Phase 3 | 26 participants (Anticipated) | Interventional | 2021-03-17 | Active, not recruiting | ||
| Pharmacodynamic and Pharmacokinetic Interactions Between Intravenous Cocaine and Acetazolamide or Quinine [NCT01851473] | Phase 1 | 14 participants (Actual) | Interventional | 2012-10-24 | Completed | ||
| Evaluating the Effect of Acetazolamide Administration and Prone Positioning Following Lumbosacral Spinal Surgery in Preventing Cerebro Spinal Fluid Leakage and Collection and Wound Dehiscence in Children. [NCT01867268] | Phase 2 | 144 participants (Anticipated) | Interventional | 2012-10-31 | Recruiting | ||
| EFFECTS OF IMMEDIATE ARGON LASER PERIPHERAL IRIDOPLASTY Versus CONVENTIONAL SYSTEMIC MEDICAL THERAPY ON OPTIC NERVE HEAD STRUCTURE AND FUNCTION OF ACUTE PRIMARY ANGLE CLOSURE EYES [NCT00485238] | Phase 4 | 60 participants (Anticipated) | Interventional | 2007-02-28 | Recruiting | ||
| [NCT00497120] | 0 participants | Interventional | Recruiting | ||||
| Rescuing OSA Patients Unable to Tolerate CPAP Using Endotype-Targeted Combination Drug Therapy: a Randomized, Double-Blind, Placebo-Controlled Trial [NCT04639193] | Phase 2 | 20 participants (Anticipated) | Interventional | 2020-01-01 | Recruiting | ||
| Administration of Acetazolamide to Prevent Remifentanil Induced Hyperalgesia: Randomize Double Blind Clinical Trial [NCT02992938] | Phase 4 | 50 participants (Actual) | Interventional | 2016-12-31 | Completed | ||
| Pathophysiology-Guided Therapy for Sleep Apnea in the Elderly [NCT02703220] | Phase 4 | 100 participants (Anticipated) | Interventional | 2015-07-03 | Recruiting | ||
| Sleep Apnea: Mechanism and Cerebrovascular Consequences [NCT00108602] | 0 participants (Actual) | Interventional | 2007-05-31 | Withdrawn(stopped due to This study of the overall grant was not pursued as the aims were changed) | |||
| Targeting Chemoreceptor Control of Breathing During Sleep to Mitigate Opioid-Associated Sleep Disordered Breathing [NCT05589753] | Phase 1/Phase 2 | 150 participants (Anticipated) | Interventional | 2019-05-02 | Recruiting | ||
| Urinary Chemistry and Acid-Base Effects of Potassium Citrate in Children With Idiopathic Hypercalciuria and Urolithiasis [NCT00120731] | 0 participants (Actual) | Interventional | 2005-07-31 | Withdrawn(stopped due to Determined not feasible) | |||
| Optimal Dosage of Acetazolamide for Obstructive Sleep Apnea Treatment: a Parallel-group, Double-blind, Placebo-controlled, Randomized Trial [NCT04726982] | Phase 4 | 100 participants (Anticipated) | Interventional | 2021-04-20 | Recruiting | ||
| Investigation of the Efficacy and Safety of Preoperative Intraocular Pressure (IOP) Reduction With Preservative-free COSOPT-S® (Dorzolamide/Timolol, MSD) Eye Drops Versus Oral Acetazolamide and Dexamethasone Eye Drops [NCT01228149] | Phase 4 | 62 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| Prospective Clinical Trial to Evaluate the Efficacy of Acetazolamide for the Treatment of Cystoid Fluid Collections in Retinoschisis: The AXIS Trial [NCT06114537] | Phase 2 | 22 participants (Anticipated) | Interventional | 2023-01-20 | Recruiting | ||
| Acetazolamide for Respiratory Failure in Combination With Metabolic Alkalosis [NCT00222534] | Phase 4 | 70 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
| Diuresis Efficacy in Ambulatory Chronic Heart Failure Patients With Volume Overload- Intra -Patient Comparison of Three Diuretics Regimens [NCT05904808] | Phase 4 | 42 participants (Actual) | Interventional | 2023-04-19 | Active, not recruiting | ||
| Treatment of High-altitude Sleep Disturbance: A Double-blind Comparison of Temazepam Versus Acetazolamide. [NCT01519544] | 34 participants (Actual) | Interventional | 2012-03-31 | Completed | |||
| Controlled Hyperventilation as Prophylaxis for Acute Mountain Sickness: A Randomized Controlled Trial [NCT02972411] | 30 participants (Anticipated) | Interventional | 2016-10-31 | Recruiting | |||
| Comparing Eye Pressure Using Maximal Tolerated Local Therapy or Systemic Acetazolamide. A Possible Pretreatment for Trabeculectomy Surgery. [NCT01274039] | 0 participants | Observational | 2009-02-28 | Completed | |||
| A Noninvasive Arterial Input Estimation Method for O-15 PET and Integrated PET/MR Scanning [NCT03806751] | Early Phase 1 | 6 participants (Anticipated) | Interventional | 2025-02-01 | Not yet recruiting | ||
| A Randomized Controlled Trial of Acetazolamide for Patients With Treatment Resistant Schizophrenia [NCT04887792] | Phase 1/Phase 2 | 60 participants (Anticipated) | Interventional | 2022-02-01 | Recruiting | ||
| The Effect of Acetazolamide on the Severity of REM Obstructive Sleep Apnea [NCT05589792] | Phase 1/Phase 2 | 10 participants (Anticipated) | Interventional | 2023-01-30 | Recruiting | ||
| Cerebral Vascular Reserve in Small Vessel Disease and Alzheimers Disease [NCT05443308] | 50 participants (Anticipated) | Observational | 2022-06-21 | Recruiting | |||
| Hypoventilation and High Altitude Chronic Polycythemia: Acetazolamide as a Possible Treatment [NCT00424970] | Phase 4 | 55 participants (Anticipated) | Interventional | 2007-01-31 | Completed | ||
| Effects of Acetazolamide on the Duration of Mechanical Ventilation in Patients With Metabolic Alkalosis. Phase III Multicenter Double-blinded Clinical Trial. [NCT01499485] | Phase 3 | 140 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
| A Randomized Trial to Evaluate Effectiveness of Acetazolamide in COPD Patients Developing Metabolic Alkalosis During Invasive Mechanical Ventilation [NCT01627639] | Phase 4 | 380 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| Comparison of Combined Intravitreal Bevacizumab and Oral Acetazolamide Versus Intravitreal Bevacizumab Alone for the Treatment of Macular Edema Secondary to Retinal Vein Occlusions [NCT05290948] | Phase 2 | 57 participants (Anticipated) | Interventional | 2022-03-12 | Active, not recruiting | ||
| Acetazolamide for the Prevention of High Altitude Illness: a Comparison of Dosing [NCT01993667] | Phase 4 | 130 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| Basic Research on Acetazolamide´s Headache Inducing Characteristics and Effects on the Cerebral Arteries and Blood Flow in a Humane Experimental Headache Model [NCT01750723] | 12 participants (Actual) | Interventional | 2012-12-31 | Completed | |||
| C-arm Cone Beam CTA and CTP With Acetazolamide Challenge in Aneurysmal Subarachnoid Hemorrhage: Evaluating Predictability for Early Ischemia in Cerebral Vasospasm [NCT03377049] | Phase 4 | 11 participants (Actual) | Interventional | 2019-07-28 | Completed | ||
| Effect of Acetazolamide on Right Ventricular Function at Rest in Patients With Chronic Obstructive Pulmonary Disease at Altitude. A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03173508] | Phase 4 | 110 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Effect of Acetazolamide on Right Ventricular Function During Exercise in Patients With Chronic Obstructive Pulmonary Disease at Altitude. A Randomized, Placebo-controlled, Double-blind Parallel Trial. [NCT03167034] | Phase 4 | 110 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Effect of Orogastric Acetazolamide on Intraocular Pressure in Laparoscopic Donor Nephrectomies [NCT03005665] | 40 participants (Actual) | Interventional | 2016-02-29 | Completed | |||
| Sickness Evaluation at Altitude With Acetazolamide at Relative Doses [NCT03828474] | Phase 1 | 108 participants (Actual) | Interventional | 2019-08-09 | Completed | ||
| A Randomized Controlled Trial of Altitude Sickness Prevention and Efficacy of Comparative Treatments [NCT02604173] | Phase 3 | 103 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
| Diamox/Aldactone to Increase the URinary Excretion of Sodium: an Investigational Study in Congestive Heart Failure [NCT01973335] | Phase 4 | 34 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
| Patient-centered and Neurocognitive Outcomes With Acetazolamide for Sleep Apnea [NCT05804084] | Phase 2 | 60 participants (Anticipated) | Interventional | 2023-05-16 | Recruiting | ||
| Phase I, Open-Label, Study of Tumor Infiltrating Lymphocytes Engineered With Membrane Bound IL15 Plus Acetazolamide in Adult Patients With Metastatic Melanoma [NCT05470283] | Phase 1 | 30 participants (Anticipated) | Interventional | 2022-09-07 | Recruiting | ||
| Stent Implantation Versus Medical Therapy for Idiopathic IntracraniaL Hypertension (SIMPLE) [NCT05707442] | Phase 3 | 74 participants (Anticipated) | Interventional | 2022-10-31 | Recruiting | ||
| The Effect of Glyceryl Trinitrate (GTN) and Diamox on Cerebral Haemodynamics Judged With the Help of 3-Tesla MRI. [NCT00363571] | 12 participants | Interventional | 2006-08-31 | Not yet recruiting | |||
| A Prospective, Double-blind, Randomized, Placebo-controlled Trial of Acetazolamide on Subclinical High-Altitude Pulmonary Edema Detected by Lung Ultrasonography [NCT03490916] | Phase 4 | 18 participants (Actual) | Interventional | 2018-03-23 | Terminated(stopped due to PI was unable to continue to gather data during the trip during to medical illness) | ||
| Optimization Strategy for the Prevention of Acute Mountain Sickness by Remote Ischemic Preconditioning Combined With Acetazolamide [NCT05023941] | Phase 4 | 252 participants (Actual) | Interventional | 2021-12-01 | Completed | ||
| Effect of Acetazolamide on Postural Control in Lowlanders Older Than 40 Years at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03536429] | Phase 4 | 99 participants (Actual) | Interventional | 2018-05-15 | Completed | ||
| A Pilot Crossover Study in Healthy Volunteers to Assess the Effect of Acetazolamide on Intraocular Pressure After Being in the Trendelenburg Position. [NCT03107429] | 9 participants (Actual) | Interventional | 2015-03-01 | Completed | |||
| Effect of Acetazolamide on Postural Control in Patients With Chronic Obstructive Pulmonary Disease at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03177811] | Phase 4 | 127 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Effect of Acetazolamide on Sleep Disordered Breathing in Lowlanders Older Than 40 Years at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03536507] | Phase 4 | 185 participants (Actual) | Interventional | 2018-05-15 | Completed | ||
| Acetazolamide for Prevention of Altitude Related Illness in Patients With Chronic Obstructive Pulmonary Disease (COPD). Randomized, Placebo-Controlled, Double-Blind Trial. [NCT03156231] | Phase 4 | 185 participants (Actual) | Interventional | 2017-05-24 | Completed | ||
| Effect of Acetazolamide on Lung Water Content by Ultrasound in Patients With Respiratory Disease at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03540901] | Phase 4 | 112 participants (Actual) | Interventional | 2018-05-22 | Completed | ||
| Intracranial Pressure in Experimental Models of Headache [NCT01288781] | 23 participants (Actual) | Interventional | 2011-07-31 | Completed | |||
| Buspirone as a Potential Treatment for Recurrent Central Apneas [NCT00746954] | Phase 3 | 8 participants (Actual) | Interventional | 2008-09-30 | Terminated(stopped due to Patient recruitment and Funding inadequate to finish trial) | ||
| Effect of Acetazolamide on Visuo-motor Learning in Lowlanders Older Than 40 Years at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03536520] | Phase 4 | 59 participants (Actual) | Interventional | 2018-05-15 | Completed | ||
| Optimal Diuretic Therapies for Acute Heart Failure With Volume Overload - A Randomized Clinical Trial [NCT06166654] | Phase 4 | 939 participants (Anticipated) | Interventional | 2024-04-01 | Not yet recruiting | ||
| Pilot Study of Acetazolamide to Prevent Post Operative Cerebrospinal Fluid (CSF) Leak in Patients Undergoing Endoscopic Skull Base Surgery [NCT04351061] | Phase 2 | 0 participants (Actual) | Interventional | 2020-05-07 | Withdrawn(stopped due to No participants were identified per inclusion/exclusion criteria) | ||
| Altitude Sickness Prevention With Ibuprofen Relative to Acetazolamide and Treatment Efficacy [NCT03154645] | Phase 1 | 92 participants (Actual) | Interventional | 2017-08-12 | Completed | ||
| Impact of Acetazolamide in Reducing Referred Postoperative Pain After Robotic Assisted Laparoscopic Prostatectomy [NCT04470843] | Phase 1 | 33 participants (Actual) | Interventional | 2018-08-22 | Completed | ||
| Effect of Acetazolamide on Maximal Exercise Performance in Lowlanders Older Than 40 Years at Altitude: A Randomized, Placebo-controlled, Double-blind Parallel Trial [NCT03536455] | Phase 4 | 92 participants (Actual) | Interventional | 2018-05-15 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||