dorzolamide: topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
dorzolamide : 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration). A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension. [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]
| ID Source | ID |
|---|---|
| PubMed CID | 5284549 |
| CHEMBL ID | 218490 |
| CHEBI ID | 4702 |
| SCHEMBL ID | 24061 |
| MeSH ID | M0173578 |
| Synonym |
|---|
| BIDD:GT0306 |
| AKOS005576255 |
| AB00514687-06 |
| AB00514687-07 |
| BRD-K48617017-003-03-1 |
| CHEMBL218490 |
| dorzolamide, trans-(-)- |
| (4s,6s)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide |
| BSPBIO_001252 |
| PRESTWICK3_001116 |
| BPBIO1_001377 |
| PRESTWICK2_001116 |
| AB00514687 |
| dorzolamide |
| C06969 |
| 120279-96-1 |
| (4s-trans)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide |
| DB00869 |
| 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide |
| (4s,6s)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide |
| bdbm10884 |
| dorzolamide (dza) |
| 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda6-thieno[2,3-b]thiopyran-2-sulfonic acid amide |
| (2s,4s)-4-(ethylamino)-2-methyl-1,1-dioxo-2h,3h,4h-1$l^{6},7-thieno[2,3-b]thiopyran-6-sulfonamide |
| (4s,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide |
| 4s,6s-dorzolamide |
| 1CIL |
| trusopt (tn) |
| 4-ethylamino-5,6-dihydro-6-methyl-7,7-dioxide-4h-thieno(2,3-b)thiopyran-2-sulfonamide |
| 5,6-dihydro-4-ethylamino-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide |
| dorzolamide [inn:ban] |
| 4h-thieno(2,3-b)thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4s-trans)- |
| 4h-thieno(2,3-b)thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4s,6s)- |
| SPBIO_003116 |
| PRESTWICK1_001116 |
| PRESTWICK0_001116 |
| HMS2089O06 |
| CHEBI:4702 , |
| D07871 |
| dorzolamide (inn) |
| STK645522 |
| 4h-thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4s,6s)- |
| A804484 |
| (4s,6s)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide |
| unii-9jdx055tw1 |
| 9jdx055tw1 , |
| NCGC00179244-04 |
| (4s,6s)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide |
| dorzolamide [who-dd] |
| dorzolamide [mi] |
| dorzolamide [inn] |
| dorzolamide [vandf] |
| gtpl6810 |
| 4-ethylamino-6-methyl-7,7-dioxo-5,6-dihydro-4h-thieno[5,4-b]thiopyran-2-sulfonamide |
| HY-B0109 |
| CS-1859 |
| SCHEMBL24061 |
| (4s,6s)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide |
| IAVUPMFITXYVAF-XPUUQOCRSA-N |
| smr004703245 |
| MLS006011430 |
| Q-201042 |
| AB00514687_08 |
| DTXSID7022960 , |
| (2s,4s)-4-(ethylamino)-2-methyl-1,1-dioxo-2h,3h,4h-1$l^{6},7-thieno[2,3-b][1$l^{6}]thiopyran-6-sulfonamide |
| J-520426 |
| sr-05000001449 |
| SR-05000001449-1 |
| dorzolamide, >=98% (hplc) |
| 139066-77-6 |
| 4h-thieno[2,3-b]thiopyran-2-sulfonamide,4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4s,6s)- |
| AS-14731 |
| Q415401 |
| (2s,4s)-4-(ethylamino)-2-methyl-1,1-dioxo-2h,3h,4h-1lambda6-thieno[2,3-b]thiopyran-6-sulfonamide |
| EN300-19766577 |
| unii 9jdx055tw1 |
| dtxcid802960 |
| 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno(2,3-b)thiopyran-2-sulfonic acid amide |
| dorzolamida |
| s01ec03 |
| dorzolamidum |
| (4s,6s)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide |
| 4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda6-thieno(2,3-b)thiopyran-2-sulfonic acid amide |
| dorzolamid |
| (4s,6s)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno(2,3-b)thiopyran-2-sulfonic acid amide |
| (4s,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide |
Dorzolamide is a powerful inhibitor of carbonic anhydrase (CA) II. It penetrates the sclera and cornea to reach the ciliary process and lowers formation of HCO3 and aqueous humor. The site of action is local within the eye.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dorzolamide hydrochloride is a carbonic anhydrase inhibitor that reduces intraocular pressure (IOP) by decreasing the production of aqueous humour in the ciliary body. " | ( Assessment of retinal hemodynamics with the Canon laser blood flowmeter after a single dose of 2% dorzolamide hydrochloride eyedrops. Buys, YM; Faingold, D; Flanagan, J; Guan, K; Hudson, C; Rawji, M; Trope, GE, 2004) | 1.98 |
| "Dorzolamide is a carbonic anhydrase inhibitor, which reduces intraocular pressure by suppressing aqueous production." | ( Erythema multiforme after use of topical dorzolamide. Ahluwalia, H; Munshi, V, 2008) | 1.33 |
| "Dorzolamide is an effective ocular hypotensive agent that accelerates blood velocity in the retinal and superficial optic nerve head without an apparent effect upon retrobulbar hemodynamics." | ( Effects of topical dorzolamide on retinal and retrobulbar hemodynamics. Arend, O; Arend, S; Harris, A; Martin, B, 1996) | 2.07 |
| "Dorzolamide is a powerful inhibitor of carbonic anhydrase (CA) II that penetrates the sclera and cornea to reach the ciliary process and lowers formation of HCO3 and aqueous humor. " | ( Ocular absorption, blood levels, and excretion of dorzolamide, a topically active carbonic anhydrase inhibitor. Conroy, CW; Levy, NS; Maren, TH; Wynns, GC, 1997) | 1.99 |
| "Dorzolamide is a local carbonic anhydrase inhibitor which lacks the systemic side effects seen after oral administration of carbonic anhydrase inhibitors." | ( [Four new drugs for glaucoma: apraclonidine, brimonidine, dorzolamide and latanoprost]. Hoyng, PF; Rasker, MT, 1998) | 1.27 |
| "Dorzolamide is a very potent inhibitor of CA-II and its site of action is local within the eye." | ( Pharmacological and ocular hypotensive properties of topical carbonic anhydrase inhibitors. Sugrue, MF, 2000) | 1.03 |
| "Dorzolamide hydrochloride is a potent inhibitor of human CA isoenzyme II, with an IC50 value of 0.18 nM in vitro." | ( [Pharmacological profiles of the potent carbonic anhydrase inhibitor dorzolamide hydrochloride, a topical antiglaucoma agent]. Kobayashi, M; Naito, K, 2000) | 1.26 |
| "Dorzolamide/timolol is a well tolerated and effective fixed combination for lowering IOP in the treatment of open-angle glaucoma and is likely to be useful in those patients who do not respond adequately to first-line monotherapy. " | ( Topical dorzolamide 2%/timolol 0.5%: a review of its use in the treatment of open-angle glaucoma. McClellan, K; Ormrod, D, 2000) | 2.18 |
| "Dorzolamide is a carbonic anhydrase inhibitor for topical ophthalmic application. " | ( Clinical pharmacokinetics of dorzolamide. Banditt, P; Martens-Lobenhoffer, J, 2002) | 2.05 |
Dorzolamide has been approved in a number of countries for use in patients with ocular hypertension or open-angle glaucoma. It was as effective as pilocarpine 2% 4 times daily as adjunctive therapy in patients receiving timolol.
| Excerpt | Reference | Relevance |
|---|---|---|
| "2% dorzolamide) has to be kept at about 5.65, and to increase the topical bioavailability of the drug from Trusopt the contact time of the drug with the eye surface is increased by increasing the viscosity of the eye drops to 100 cps." | ( Cyclodextrin formulation of dorzolamide and its distribution in the eye after topical administration. Eysteinsson, T; Gudmundsdóttir, E; Loftsson, T; Sigurdsson, HH; Stefánsson, E; Thorsteinsdóttir, M, 2005) | 1.14 |
| "Dorzolamide has been approved in a number of countries for use in patients with ocular hypertension or open-angle glaucoma." | ( The preclinical pharmacology of dorzolamide hydrochloride, a topical carbonic anhydrase inhibitor. Sugrue, MF, 1996) | 1.3 |
| "Dorzolamide has additive ocular hypotensive effects when used in conjunction with topical beta-adrenergic antagonists and was as effective as pilocarpine 2% 4 times daily as adjunctive therapy in patients receiving timolol." | ( Dorzolamide. A review of its pharmacology and therapeutic potential in the management of glaucoma and ocular hypertension. Balfour, JA; Wilde, MI, 1997) | 2.46 |
| "Dorzolamide has no short-term effect on accommodation or pupillary function." | ( [Effect of dorzolamide on accommodation and pupillary reaction?]. Pek, H; Wilhelm, H, 2000) | 2.14 |
| "Dorzolamide/timolol has been compared with concomitant administration of timolol 0.5% and the IOP lowering miotic drug, pilocarpine 2.0%." | ( Topical dorzolamide 2%/timolol 0.5%: a review of its use in the treatment of open-angle glaucoma. McClellan, K; Ormrod, D, 2000) | 1.46 |
Dorzolamide may increase peripapillary choroidal perfusion in non-exudative AMD patients. The drug appears to enhance contrast sensitivity in normal subjects during physiologic hypercapnia and hypocapnia at 4 and 1 cpd.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dorzolamide may increase peripapillary choroidal perfusion in non-exudative AMD patients. " | ( The effects of dorzolamide on choroidal and retinal perfusion in non-exudative age related macular degeneration. Ciulla, TA; Garzozi, HJ; Harris, A; Kagemann, L; Piper, HC; Pratt, LM; Rechtman, E, 2003) | 2.11 |
| "Dorzolamide lead to increase of peak systolic velocity." | ( Effects of glaucoma drugs on ocular hemodynamics in normal tension glaucoma: a randomized trial comparing bimatoprost and latanoprost with dorzolamide [ISRCTN18873428]. Galambos, P; Klemm, M; Matthiessen, ET; Reuss, J; Richard, G; Wagenfeld, L; Wiermann, A; Zeitz, O, 2005) | 1.25 |
| "Dorzolamide appears to enhance contrast sensitivity in normal subjects during physiologic hypercapnia and hypocapnia at 4 and 1 cpd, respectively. " | ( Dorzolamide hydrochloride and visual function in normal eyes. Elliott, WR; Harris, A; Harrison, J; Kavanagh, J; Sponsel, WE; Trigo, Y, 1997) | 3.18 |
In dorzolamide-treated eyes, increases in the peripapillary superficial retinal VD, especially in the superior-nasal area, were significant; however, no RNFL thickness changes were observed. Dorzolamide 2% for 12 weeks led to an increase in OPP (P < 0.001) and a significant increase in end diastolic velocity (EDV) in all major ophthalmic arteries.
| Excerpt | Reference | Relevance |
|---|---|---|
| "In dorzolamide-treated eyes, increases in the peripapillary superficial retinal VD, especially in the superior-nasal area, were significant; however, no RNFL thickness changes were observed. " | ( Optical Coherence Tomography Angiography Vessel Density Changes in Normal-tension Glaucoma Treated With Carteolol, Brimonidine, or Dorzolamide. Chen, LC; Chuang, LH; Huang, SM; Lin, YH; Su, WW, 2021) | 1.45 |
| "In dorzolamide-treated cats, mean AHFR after the treatment phase (3.47 ± 1.5 μL/min) was significantly lower than the value prior to treatment (5.90 ± 2.2 μL/min) and mean IOP during the treatment phase (11.1 ± 1.0 mm Hg) was significantly lower than the baseline mean IOP (14.9 ± 1.0 mm Hg)." | ( Effects of ocular administration of ophthalmic 2% dorzolamide hydrochloride solution on aqueous humor flow rate and intraocular pressure in clinically normal cats. Allbaugh, RA; Crumley, WR; Rankin, AJ, 2012) | 1.15 |
| "Dorzolamide-treated eyes demonstrated a significant increase in mean sensitivity of + 1.55 dB (p = 0.04); placebo-treated eyes showed no significant change (+ 0.58 dB; p = 0.10). " | ( Topical dorzolamide increases pericentral visual function in age-related maculopathy: pilot study findings with short-wavelength automated perimetry. Arend, O; Remky, A; Sponsel, WE; Weber, A, 2005) | 2.21 |
| "Dorzolamide-treated eyes were not significantly different from placebo-treated eyes in corneal deswelling rate, expressed as the percent recovery per hour (55.7% +/- 13.6% versus 59.6% +/- 14.5%; P > or = 0.10), open eye steady state thickness, swelling induced by hypoxia, and corneal autofluorescence. " | ( Effect of dorzolamide on corneal endothelial function in normal human eyes. Bourne, WM; Egan, CA; Hodge, DO; McLaren, JW, 1998) | 2.15 |
| "Dorzolamide treatment was associated with higher perimetry mean deviation values under each treatment condition and was statistically significant (P < .05) at baseline." | ( Dorzolamide hydrochloride and visual function in normal eyes. Elliott, WR; Harris, A; Harrison, J; Kavanagh, J; Sponsel, WE; Trigo, Y, 1997) | 2.46 |
| "Dorzolamide pretreatment significantly reduced FLI in dorsomedial Vc." | ( Neurobiological and psychophysical mechanisms underlying the oral sensation produced by carbonated water. Carstens, E; Carstens, MI; Dessirier, JM; O'Mahony, M; Simons, CT, 1999) | 1.02 |
| "In dorzolamide-treated patients the IOP dropped from 18 mmHg to 15.5 mmHg after 9 months therapy (p < 0.01) and the visual field improved significantly by 18% (p < 0.05). " | ( [Ocular hemodynamics and visual field in glaucoma treated with dorzolamide]. Bernd, AS; Böhm, AG; Pillunat, LE; Richard, G; Schmidt, KG, 2001) | 1.17 |
| "Treatment with dorzolamide 2% for 12 weeks led to a significant increase in OPP (P < 0.001) and a significant increase in end diastolic velocity (EDV) in all major ophthalmic arteries like ophthalmic artery (OA), central retinal artery (CRA), and short posterior ciliary artery (SPCA) (P < 0.001, P = 0.04, and P = 0.0075, respectively)." | ( Efficacy of dorzolamide in improving ocular blood flow in patients with open-angle glaucoma: The Indian carbonic anhydrase inhibitor trial. Ariga, M; Chithra, MR; Das, S; Gohil, P; Jaideep, G; Nivean, PD, 2022) | 1.44 |
| "Treatment with dorzolamide for 1 week significantly increased the diameter of retinal arterioles in normal persons, and breathing in of a hypercapnic gas mixture reduced this response. " | ( Dilatation of Retinal Arterioles Induced by Topical Dorzolamide for One Week Is Impaired in Patients with Type 1 Diabetes and Mild Retinopathy. Bek, T; Tilma, KK, 2020) | 1.16 |
| "Pretreatment with dorzolamide 2% or brimonidine 0.2% reduce the intraocular pressure rise after Nd: YAG laser capsulotomy in pseudophakic patients with glaucoma." | ( [Intraocular pressure after ND: YAG laser capsulotomy in pseudophakic patients with glaucoma]. Jurisić, D; Lacmnovic-Loncar, V; Mandić, Z; Petric, I; Sesar, A; Sesar, I; Tomić, Z, 2006) | 0.67 |
| "Treatment with dorzolamide or a placebo (the vehicle of dorzolamide) in one or both eyes." | ( Predictive factors for open-angle glaucoma among patients with ocular hypertension in the European Glaucoma Prevention Study. Adamsons, I; Cunha-Vaz, J; Miglior, S; Pfeiffer, N; Torri, V; Zeyen, T, 2007) | 0.69 |
| "Treatment with dorzolamide or placebo (the vehicle of dorzolamide) in 1 or both eyes." | ( Central corneal thickness in the European Glaucoma Prevention Study. Adamsons, I; Cunha-Vaz, J; Miglior, S; Pfeiffer, N; Torri, V; Zeyen, T, 2007) | 0.69 |
| "Treatment with dorzolamide resulted in corneal edema and a significant increase in central corneal thickness, whereas the treatment with latanoprost resulted in neither corneal edema nor corneal thickness changes." | ( [Comparative study of the effects of two anti-glaucomatous drugs on the corneal thickness in rabbits with corneal autografts]. Casiraghi, JF; Chiaradia, PA; Fischbarg, J; Lavena, PI, 2008) | 0.7 |
| "Pretreatment with dorzolamide, acetazolamide, or placebo. " | ( Topical 2.0% dorzolamide vs oral acetazolamide for prevention of intraocular pressure rise after neodymium:YAG laser posterior capsulotomy. Baltatzis, S; Kokolakis, SN; Ladas, ID; Panagiotidis, D; Theodossiadis, GP; Zafirakis, P, 1997) | 1 |
| "Treatment with dorzolamide reduced aqueous flow by 17%, and a maximum dose of acetazolamide alone reduced flow by 29%. " | ( Aqueous humor flow in human eyes treated with dorzolamide and different doses of acetazolamide. Alm, A; Larsson, LI, 1998) | 0.91 |
| "Treatment with dorzolamide reduced aqueous humor flow statistically significantly (2.50 microL/min vs 3.00 microL/min; P=.001) compared with placebo, but less than a maximum dose ofacetazolamide. " | ( Aqueous humor flow in human eyes treated with dorzolamide and different doses of acetazolamide. Alm, A; Larsson, LI, 1998) | 0.91 |
Latanoprost is safe and equally effective to a fixed combination of dorzolamide and timolol in the treatment of uveitic glaucoma. Ocular burning was noted with dorZolamide more than any other adverse event with either drug.
The aim of the present study was to assess the pharmacodynamic equivalence (lowering of intraocular pressure) of two preparations of eye drops containing 20 mg dorzolamide and 5 mg timolol. The aim of this study is to develop and optimize self-assembled nanostructures of dorZolamide hydrochloride and L-α-Phosphatidylcholine.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Following a single-dose, open-label, pilot pharmacokinetic study in six subjects, the systemic pharmacokinetics and metabolic effects of dorzolamide after topical ocular administration were investigated in a double-blind, randomised, placebo-controlled study in 12 healthy volunteers." | ( Whole-blood pharmacokinetics and metabolic effects of the topical carbonic anhydrase inhibitor dorzolamide. Biollaz, J; Brunner-Ferber, F; Buclin, T; Gervasoni, JP; Jaquet, F; Magnin, JL; Munafo, A, 1995) | 0.71 |
| " This allowed for quantification of pharmacokinetic variables." | ( Non-invasive assessment of ocular pharmacokinetics using Confocal Raman Spectroscopy. Bauer, NJ; Hendrikse, F; March, WF; Motamedi, M; Webers, CA; Wicksted, JP, 1999) | 0.3 |
| " This review summarises the pharmacokinetic and pharmacodynamic properties of dorzolamide and its metabolite in eye tissues and in the systemic circulation." | ( Clinical pharmacokinetics of dorzolamide. Banditt, P; Martens-Lobenhoffer, J, 2002) | 0.83 |
| " Pharmacokinetic parameters (C(max), T(max), and AUC(0-24)) were estimated by noncompartmental analysis." | ( Ocular pharmacokinetics of dorzolamide and brinzolamide after single and multiple topical dosing: implications for effects on ocular blood flow. Jadhav, G; Kadam, RS; Kompella, UB; Ogidigben, M, 2011) | 0.67 |
| "The aim of the present study was to assess the pharmacodynamic equivalence (lowering of intraocular pressure) of two preparations of eye drops containing 20 mg dorzolamide (CAS 120279-96-1) and 5 mg timolol (CAS 26839-75-8)." | ( Pharmacodynamic equivalence study of two preparations of eye drops containing dorzolamide and timolol in healthy volunteers. Demircheva, I; Gatchev, E; Hristova, R; Kolev, E; Koytchev, R; Petrov, A; Richter, W; Tegel, F; Thyroff-Friesinger, U, 2011) | 0.79 |
| " In order to investigate the pharmacodynamic equivalence of both products, the two-sided 95% confidence interval was calculated for the difference of the primary target parameter (absolute decrease in IOP 2 h post dose), by means of a parametric (ANOVA) statistical method." | ( Pharmacodynamic equivalence study of two preparations of eye drops containing dorzolamide and timolol in healthy volunteers. Demircheva, I; Gatchev, E; Hristova, R; Kolev, E; Koytchev, R; Petrov, A; Richter, W; Tegel, F; Thyroff-Friesinger, U, 2011) | 0.6 |
| " The aim of this study is to develop and optimize self-assembled nanostructures of dorzolamide hydrochloride and L-α-Phosphatidylcholine to improve the pharmacokinetic parameters and extend the drug pharmacological action." | ( Enhancement of pharmacokinetic and pharmacological behavior of ocular dorzolamide after factorial optimization of self-assembled nanostructures. Afify, AEMR; Afify, EAMR; Elsayed, I; Gad, MK; Mohamed, MI, 2018) | 0.94 |
A Snovel method for the simultaneous separation and determination of two antiglaucoma drugs. Dorzolamide hydrochloride (DOR) and timolol maleate (TIM) in aqueous humor samples (AH) was developed by using salting-out assisted liquid-liquid microextraction (SALLME) combined with HPLC-UV method.
| Excerpt | Reference | Relevance |
|---|---|---|
| "We investigated the dose-escalation profile of dorzolamide used in combination with other antiglaucoma agents in patients with primary glaucoma and ocular hypertension." | ( The efficacy and safety of dose escalation of dorzolamide used in combination with other topical antiglaucoma agents. Araie, M; Azuma, I; Hamanaka, T; Kitazawa, Y; Origasa, H; Shirato, S; Tomita, G, 2003) | 0.83 |
| "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) | 0.87 |
| "5% alone or combined with latanoprost in reducing IOP in a real-world setting." | ( Effectiveness and safety of dorzolamide-timolol alone or combined with latanoprost in open-angle glaucoma or ocular hypertension. Bastien, NR; Koulis, T; Lesk, MR; Sampalis, F; Sampalis, JS, 2008) | 0.64 |
| "A Snovel method for the simultaneous separation and determination of two antiglaucoma drugs namely, dorzolamide hydrochloride (DOR) and timolol maleate (TIM) in aqueous humor samples (AH) was developed by using salting-out assisted liquid-liquid microextraction (SALLME) combined with HPLC-UV method." | ( Simultaneous determination of dorzolomide and timolol in aqueous humor: a novel salting out liquid-liquid microextraction combined with HPLC. Abdel-Wadood, HM; Mohamed, AM; Mousa, HS, 2014) | 0.62 |
| "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 |
| "To examine the relevance of concentration of benzalkonium chloride (BAK) on the cornea, we investigated the effects of latanoprost containing BAK alone and in combination with other antiglaucoma drug classes on corneal epithelium in vitro in a cultured rabbit corneal cell line (SIRC) and in vivo, using a corneal resistance device (CRD)." | ( In vitro and in vivo corneal effects of latanoprost combined with brimonidine, timolol, dorzolamide, or brinzolamide. Fukuda, M; Sasaki, H; Shibata, N; Shibata, S; Shibata, T; Sugiyama, K; Takeda, N, 2016) | 0.66 |
The objective of this study was to formulate in situ gel of chitosan nanoparticles to enhance the bioavailability and efficacy of dorzolamide in the glaucoma treatment. The objectives of the current study are to maximize the ocular bioavailability of DZD.
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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) | 0.31 |
| "65, and to increase the topical bioavailability of the drug from Trusopt the contact time of the drug with the eye surface is increased by increasing the viscosity of the eye drops to 100 cps." | ( Cyclodextrin formulation of dorzolamide and its distribution in the eye after topical administration. Eysteinsson, T; Gudmundsdóttir, E; Loftsson, T; Sigurdsson, HH; Stefánsson, E; Thorsteinsdóttir, M, 2005) | 0.62 |
| "The objectives of the current study are (i) to maximize the ocular bioavailability of dorzolamide hydrochloride (DZD) through; (a) enhancement of the DZD corneal transport using various concentrations of selected natural terpene-4-ol enhancers, (b) increasing the contact time of the drug with the absorbing tissues of the eye using selected carbopol-934 (C-934) as mucoadhesive to reduce the extensive pre-corneal loss of the installed dose due to the physiologically normal fast tear-washout, and (ii) to assess the in vivo intraocular pressure (IOP) lowering effects of the gel test formulations using normotensive New Zealand albino rabbits." | ( Influence of various concentrations of terpene-4-ol enhancer and carbopol-934 mucoadhesive upon the in vitro ocular transport and the in vivo intraocular pressure lowering effects of dorzolamide ophthalmic formulations using albino rabbits. Abdel-Naim, AB; Afouna, MI; Al-Marzoqi, A; Khedr, A, 2010) | 0.78 |
| " However, low drug-contact time and poor ocular bioavailability of drugs due to drainage of solution, tear turnover and its dilution or lacrimation limits its uses." | ( Hyaluronic acid modified chitosan nanoparticles for effective management of glaucoma: development, characterization, and evaluation. Paliwal, R; Paliwal, SR; Vyas, SP; Wadhwa, S, 2010) | 0.36 |
| "Improvement of both ocular bioavailability and duration of action for dorzolamide hydrochloride was the aim of this study." | ( Development of dorzolamide hydrochloride in situ gel nanoemulsion for ocular delivery. Ammar, HO; Ghorab, M; Mahmoud, AA; Salama, HA, 2010) | 0.95 |
| " Aqueous eye drop formulations that improve their topical bioavailability and reduce their eye irritation can improve their clinical efficacy." | ( Topical drug delivery to the eye: dorzolamide. Jansook, P; Loftsson, T; Stefánsson, E, 2012) | 0.66 |
| " The objective of this study was to formulate in situ gel of chitosan nanoparticles to enhance the bioavailability and efficacy of dorzolamide in the glaucoma treatment." | ( In situ gelling dorzolamide loaded chitosan nanoparticles for the treatment of glaucoma. Ali, A; Aqil, M; Chuttani, K; Katiyar, S; Mishra, AK; Mondal, RS; Pandit, J; Sultana, Y, 2014) | 0.95 |
| "Poor drug penetration and rapid clearance after topical instillation of a drug formulation into the eyes are the major causes for the lower ocular bioavailability from conventional eye drops." | ( Dorzolamide-loaded PLGA/vitamin E TPGS nanoparticles for glaucoma therapy: Pharmacoscintigraphy study and evaluation of extended ocular hypotensive effect in rabbits. Ahmad, FJ; Anwar, M; Garg, V; Jain, GK; Khar, RK; Talegaonkar, S; Warsi, MH, 2014) | 1.85 |
| " We propose to develop drug-eluting contact lenses for managing glaucoma with increased bioavailability and improved compliance." | ( Dual drug delivery from vitamin E loaded contact lenses for glaucoma therapy. Carbia, BE; Chauhan, A; Hsu, KH; Plummer, C, 2015) | 0.42 |
| "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 |
Dorzolamide dosed twice or three times daily was as effective as adjunctive therapy with latanoprost (P =.00) The only variation in method between the two studies was the dosage of 2% dorZolamide.
| 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. |
| antihypertensive agent | Any drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism. |
| antiglaucoma drug | Any drug which can be used to prevent or alleviate glaucoma, a disease in which the optic nerve is damaged, resulting in progressive, irreversible loss of vision. It is often, though not always, associated with increased pressure of the fluid in the eye. |
| [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. |
| thiophenes | Compounds containing at least one thiophene ring. |
| [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] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Carbonic anhydrase 2 | Homo sapiens (human) | Kd | 0.0000 | 0.0000 | 0.4157 | 5.5500 | AID1200901 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Carbonic anhydrase | Brucella suis 1330 | Kinact | 0.0210 | 0.0170 | 0.8628 | 5.8700 | AID459696 |
| Carbonic anhydrase 12 | Homo sapiens (human) | Kinact | 0.0035 | 0.0030 | 0.6674 | 9.6000 | AID299547; AID408472 |
| Carbonic anhydrase 1 | Homo sapiens (human) | Kinact | 50.0000 | 0.0100 | 0.9387 | 8.6000 | AID299242; AID299538; AID408469; AID468530 |
| Carbonic anhydrase 2 | Homo sapiens (human) | Kinact | 0.0090 | 0.0030 | 0.7946 | 10.0000 | AID299243; AID299539; AID408470; AID468531 |
| Carbonic anhydrase 3 | Homo sapiens (human) | Kinact | 8.0000 | 3.3000 | 6.1657 | 8.0000 | AID299540 |
| Carbonic anhydrase 4 | Homo sapiens (human) | Kinact | 8.5000 | 0.0740 | 2.3934 | 8.5900 | AID299541 |
| Carbonic anhydrase 6 | Homo sapiens (human) | Kinact | 0.0100 | 0.0009 | 0.7261 | 5.3000 | AID299544 |
| Carbonic anhydrase 5A, mitochondrial | Homo sapiens (human) | Kinact | 0.0420 | 0.0200 | 0.8580 | 9.4000 | AID299542 |
| Carbonic anhydrase 7 | Homo sapiens (human) | Kinact | 0.0035 | 0.0002 | 0.2852 | 5.7300 | AID299545 |
| Carbonic anhydrase 9 | Homo sapiens (human) | Kinact | 0.0520 | 0.0050 | 0.3197 | 6.6700 | AID299546; AID408471; AID468532 |
| Carbonic anhydrase 13 | Mus musculus (house mouse) | Kinact | 0.0180 | 0.0130 | 0.5669 | 8.2300 | AID299548 |
| Carbonic anhydrase 14 | Homo sapiens (human) | Kinact | 0.0270 | 0.0002 | 1.4495 | 8.5900 | AID299549 |
| Carbonic anhydrase 5B, mitochondrial | Homo sapiens (human) | Kinact | 0.0330 | 0.0090 | 0.9231 | 9.0400 | AID299543 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| AID1796687 | In vitro binding of inhibitor to hCA-II 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 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. |
| 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. |
| AID47739 | Tested for ability to inhibit human erythrocyte carbonic-anhydrase-II- (HCA II) catalyzed carbon dioxide hydration | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| AID167101 | Tested for ex vivo distribution in ciliary process after topical administration in albino rabbits (Ocular tissue concentration after 1 hr) | 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. |
| 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. |
| 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. |
| AID644380 | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins 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. |
| 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. |
| AID1570390 | Reduction of intraocular pressure in ocular normotensive New Zealand White rabbit at 2% administered topically to the eye measured for 0.5 to 8 hrs by by tonometry | 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. |
| 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. |
| 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. |
| 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. |
| AID21708 | Solubility (hydrochloride salt) in buffer at pH 7.4 and at 25 degree celsius. | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| AID75403 | In vivo intraocular pressure lowering in Glaucomatous Rabbits after the administration at a pH of 5.5, at time interval 90 min | 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. |
| 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. |
| 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. |
| AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID263049 | Inhibition of human CA2 | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | QSAR study on topically acting sulfonamides incorporating GABA moieties: a molecular connectivity approach. |
| AID166125 | Fall of in vivo intraocular pressure (IOP) of glaucomatous rabbits at 0 min after treatment with one drop (50 uL) solution of 2% of CA inhibitor directly into eye | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| 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. |
| 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? |
| 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. |
| 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. |
| 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. |
| AID146522 | In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 90 min | 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. |
| 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. |
| 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. |
| AID166728 | Tested for in vivo IOP-lowering of glaucomatous rabbits after topical administration at the specified interval( 90 min) at pH 5.5 | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166596 | Tested for in vivo IOP-lowering of glaucomatous rabbits after topical administration at the specified interval( 60 min) at pH 5.5 | 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. |
| AID166106 | Tested ex vivo for ocular tissue concentration against aqueous humor after 1 hour of treatment with 50 uL | 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. |
| AID1323834 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
| 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. |
| 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. |
| AID1605093 | Antiglaucoma activity in hypertonic saline solution-induced New Zealand albino rabbit model of ocular hypertension assessed as reduction in intraocular pressure at 1% administered topically to eye measured after 120 mins by pneumotonometric- method | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166028 | The compound was evaluated for fall in intraocular pressure (IOP) of Normotensive rabbits (20.2+/-2.3 mmHg) after treatment with one drop (50 microL) of a 2% solution at 90 min (pH 5.5) | 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. |
| 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. |
| 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. |
| AID165830 | Compound was evaluated in vivo in glaucomatous rabbits (33.5+/-3.0 mmHg) for the intraocular pressure (IOP) lowering 60 min after topical administration with one drop of Carbonic anhydrase at a pH 5.5 | 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. |
| AID47922 | 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. |
| 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. |
| 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. |
| AID166350 | Tested in vivo for lowering IOP (Intraocular Pressure)in Normotensive Rabbits at pH 5.5 after treatment with 50 uL, activity at 30 minutes | 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. |
| AID166956 | 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? |
| 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. |
| AID1350483 | Anti-glaucoma activity in hypertonic saline-induced hypertensive New Zealand albino rabbit model assessed as decrease in intraocular pressure at 1% instilled into eye vitreous measured at 60 mins post administration by pneumatonometric analysis | 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. |
| AID167105 | Tested for ex vivo distribution in cornea after topical administration into albino rabbits (Ocular tissue concentration after 1 hr) | 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. |
| AID1323835 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
| 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. |
| AID166333 | Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 60 min at a pH of 5.5 | 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. |
| 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. |
| AID1200902 | Inhibition of human carbonic anhydrase 2 assessed as reduction in enzyme activity incubated for 30 mins by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID27322 | In vitro corneal permeability when cornea is intact | 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. |
| 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. |
| 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. |
| 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. |
| AID166339 | Tested in vivo for lowering IOP (Intraocular Pressure)in Glaucomatous Rabbits at pH 5.5 after treatment with 50 uL, activity at 60 minutes | 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. |
| 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? |
| AID311027 | Inhibition of human carbonic anhydrase 5A | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID1605092 | Antiglaucoma activity in hypertonic saline solution-induced New Zealand albino rabbit model of ocular hypertension assessed as reduction in intraocular pressure at 1% administered topically to eye measured after 60 mins by pneumotonometric- method | 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. |
| 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. |
| AID47935 | Inhibitory activity against human recombinant carbonic anhydrase II | 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? |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID47750 | Inhibitory activity against 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. |
| AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| 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. |
| 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. |
| AID19227 | Partition coefficient (logP) | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| 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. |
| AID28833 | Solubility in buffer at pH 5.5 | 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. |
| AID311030 | Inhibition of human carbonic anhydrase 7 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID167102 | Tested for ex vivo distribution in ciliary process after topical administration in albino rabbits (Ocular tissue concentration after 2 hr) | 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. |
| AID166352 | Tested in vivo for lowering IOP (Intraocular Pressure)in Normotensive Rabbits at pH 5.5 after treatment with 50 uL, activity at 90 minutes | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166108 | Tested ex vivo for ocular tissue concentration against ciliary process after 1 hour of treatment with 50 uL | 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. |
| 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. |
| AID1245276 | Inhibition of human recombinant carbonic anhydrase-9 expressed in Escherichia coli incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents. |
| 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. |
| AID445829 | Reduction of intraocular pressure in normotensive New Zealand white rabbit at 55 mM | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| 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. |
| 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. |
| AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| 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. |
| AID27588 | Partition coefficient as hydrochloride, at pH 5.8 | 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. |
| 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. |
| AID47744 | Compound was evaluated for the inhibitory activity against Human Carbonic anhydrase II (HCA II) | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Application of the three-dimensional structures of protein target molecules in structure-based drug design. |
| AID48281 | Inhibitory activity against bovine lung microsomes carbonic anhydrase isozyme IV (bCA IV). | 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? |
| 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. |
| AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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). |
| 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. |
| 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. |
| AID166731 | Tested for in vivo IOP-lowering of normotensive albino rabbits after topical administration at the specified interval (30 min) at pH 5.5 | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166107 | Tested ex vivo for ocular tissue concentration against aqueous humor after 2 hour of treatment with 50 uL | 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. |
| AID166351 | Tested in vivo for lowering IOP (Intraocular Pressure)in Normotensive Rabbits at pH 5.5 after treatment with 50 uL, activity at 60 minutes | 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. |
| AID167705 | In vitro transcorneal accession rate (intact cornea) of compound was determined | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166318 | Prolonged IOP lowering by the compound in glaucomatous rabbit for 3 hours | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one? |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID47916 | Binding affinity against human carbonic anhydrase II (hCA -II) | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID75400 | In vivo intraocular pressure lowering in Glaucomatous Rabbits after the administration at a pH of 5.5, at time interval 0 min | 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. |
| AID19232 | Partition coefficient (logD) (chloroform/buffer) | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| AID1245274 | Inhibition of human recombinant carbonic anhydrase-1 expressed in Escherichia coli incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents. |
| AID1350484 | Anti-glaucoma activity in hypertonic saline-induced hypertensive New Zealand albino rabbit model assessed as decrease in intraocular pressure at 1% instilled into eye vitreous measured at 2 hrs post administration by pneumatonometric analysis | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID311026 | Inhibition of human carbonic anhydrase 4 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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). |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID747802 | Antiglaucoma activity in hypertensive New Zealand albino rabbit model assessed as decrease in carbomer-induced intraocular pressure at 2% administered to eye after 1 hr by tanometric analysis (Rvb = 35 to 40 mmHg) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID50370 | Inhibitory activity against human cloned carbonic anhydrase isozyme I (hCA I, cytosolic form). | 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? |
| 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. |
| 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. |
| AID311031 | Inhibition of human carbonic anhydrase 9 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID166441 | In vivo intraocular pressure (IOP) lowering at 30 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| AID598020 | Inhibition of carbomer-induced ocular hypertension in New Zealand rabbits assessed as time for maximal IOP lowering efficacy at 2 % in 50 uL administered into eye after 2 to 3 weeks of carbomer challenge | 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. |
| 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. |
| AID166246 | Fall of in vivo intraocular pressure (IOP) of glaucomatous rabbits at 30 min after treatment with one drop (50 uL) solution of 2% of CA inhibitor directly into eye | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID27323 | In vitro corneal permeability when corneal epithelium is absent | 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. |
| 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. |
| 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. |
| AID299540 | Inhibition of human CA3 | 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. |
| AID18313 | In vitro permeability through intact cornea | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| 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. |
| 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. |
| AID1245278 | Antiglaucoma activity in New Zealand albino rabbit model of carbomer-induced hypertensive eye glaucoma assessed as time duration showing reduction in intraocular pressure at 2% directly instilled into conjunctive pocket measured 24 hrs post drug administr | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents. |
| 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. |
| 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 | |||
| 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. |
| 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. |
| AID165828 | Compound was evaluated in vivo in glaucomatous rabbits (33.5+/-3.0 mmHg) for the intraocular pressure (IOP) lowering 30 min after topical administration with one drop of Carbonic anhydrase at a pH 5.5 | 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. |
| AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| 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. |
| AID480752 | Inhibition of carbonic anhydrase 4 | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166198 | Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 30 min at a pH of 5.5 | 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. |
| AID1681923 | Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after 24 hrs by dual luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer. |
| 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. |
| 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. |
| AID47917 | Compound was evaluated for the affinity towards Human Carbonic anhydrase II (HCA II) | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Application of the three-dimensional structures of protein target molecules in structure-based drug design. |
| 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. |
| AID1245277 | Inhibition of human recombinant carbonic anhydrase-12 expressed in Escherichia coli incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents. |
| AID1194930 | Reduction in intraocular pressure in glaucoma patient | 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. |
| AID311024 | Inhibition of human carbonic anhydrase 2 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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 | |||
| AID166576 | Reduction of intraocular pressure in normotensive rabbits after treatment with 50 uL of compound (as HCl salt) at pH 5.5 in eye after 60 min from administration, to that of controls | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| AID50363 | Inhibition of human cloned Carbonic anhydrase I | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1183614 | Antiglaucoma activity in New Zealand rabbit model of hypertonic saline-induced ocular hypertension assessed as reduction in intraocular pressure dosed with 50 uL of 2% compound solution and measured after 1 hr | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Furazan and furoxan sulfonamides are strong α-carbonic anhydrase inhibitors and potential antiglaucoma agents. |
| AID480923 | Inhibition of carbonic anhydrase in Dutch belted rabbit iris ciliary body homogenate at 0.1 uM by titration assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. |
| 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. |
| 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. |
| AID166196 | Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 240 min at a pH of 5.5 | 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. |
| 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. |
| 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. |
| 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). |
| 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 | |||
| 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 | |||
| 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. |
| AID166126 | Fall of in vivo intraocular pressure (IOP) of glaucomatous rabbits at 120 min after treatment with one drop (50 uL) solution of 2% of CA inhibitor directly into eye | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| 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. |
| 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. |
| AID311033 | Inhibition of mouse carbonic anhydrase 13 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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. |
| 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. |
| 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. |
| AID166438 | In vivo intraocular pressure (IOP) lowering at 120 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| AID166340 | Tested in vivo for lowering IOP (Intraocular Pressure)in Glaucomatous Rabbits at pH 5.5 after treatment with 50 uL, activity at 90 minutes | 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. |
| AID167756 | Compound was evaluated for ocular hypotensive effects (intraocular pressure, IOP) by administering 2% of the drug three times daily | 1997 | Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18 | New approaches to antiglaucoma therapy. |
| 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. |
| 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. |
| AID166194 | Change in intraocular pressure (IOP) was measured in the normotensive pigmented rabbit | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| 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. |
| AID23540 | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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). |
| 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. |
| AID445823 | Inhibition of human carbonic anhydrase 2 by CO2 hydrase stopped flow assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID311032 | Inhibition of human carbonic anhydrase 12 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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. |
| 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. |
| AID1200901 | Binding affinity to human carbonic anhydrase 2 incubated for 1 hr using labeled BODIPY558/568-acetazolamide as tracer by fluorescence polarization tight binding assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure. |
| 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. |
| AID167100 | Tested for ex vivo distribution in aqueous humor after topical administration in albino rabbits (Ocular tissue concentration after 2 hr) | 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. |
| 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). |
| 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. |
| 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. |
| 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. |
| 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? |
| 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. |
| 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. |
| 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. |
| AID25799 | Rate of corneal penetration for reaching ciliary processes | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one? |
| 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. |
| 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). |
| 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 | |||
| 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. |
| 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. |
| AID311025 | Inhibition of human carbonic anhydrase 3 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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. |
| 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. |
| 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. |
| AID165874 | Compound was evaluated in vivo in normotensive rabbits (23.5+/-2.6 mmHg) for the intraocular pressure (IOP) lowering 60 min after topical administration with one drop of Carbonic anhydrase inhibitor at a pH 5.5 | 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. |
| 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. |
| 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. |
| 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. |
| AID238256 | 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. |
| AID480922 | Thermodynamic solubility at pH 6.5 after 4 hrs by HPLC analysis | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. |
| AID48131 | Inhibition of bovine Carbonic anhydrase IV determined by esterase method | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| AID48289 | Inhibition of bovine carbonic anhydrase IV from bovine lung microsomes | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10 | Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV. |
| 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. |
| 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. |
| 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. |
| AID1194931 | Antiglaucoma activity in New Zealand albino rabbit model of glaucoma assessed as reduction in intraocular pressure dosed as 2% eye drops immediately after injection of hypertonic saline measured 1 hr post dose | 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. |
| 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. |
| AID166025 | The compound was evaluated for fall in intraocular pressure (IOP) of Normotensive rabbits (20.2+/-2.3 mmHg) after treatment with one drop (50 microL) of a 2% solution at 0 min (pH 5.5) | 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. |
| AID48109 | Ex vivo inhibition of carbonic anhydrase II in iris - ciliary body of an albino rabbit at a concentration of 0.1% | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| 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. |
| 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. |
| AID311034 | Inhibition of human carbonic anhydrase 14 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID747804 | Antiglaucoma activity in normotensive New Zealand rabbit model assessed as decrease in intraocular pressure administered to eye vitreous by tanometric analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID311028 | Inhibition of human carbonic anhydrase 5B | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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. |
| AID167106 | Tested for ex vivo distribution in cornea after topical administration into albino rabbits (Ocular tissue concentration after 2 hr) | 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. |
| 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. |
| 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. |
| AID1461806 | Ocular hypotensive activity in New Zealand albino rabbit eye assessed as reduction in hypertonic saline-induced intraocular pressure at 2% administered as eye drop measured at 60 mins post administration by applanation tonometry | 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. |
| AID21493 | Solubility in pH 5.2 buffer | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| AID47906 | Tested for ability to compete with dansylamide for binding to human erythrocyte carbonic-anhydrase-II (HCA-II) | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| 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. |
| AID17876 | In vitro permeability through cornea without epithelium | 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. |
| 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. |
| 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. |
| AID408620 | Inhibition of carbonic anhydrase 2 | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis, in vitro antibacterial and carbonic anhydrase II inhibitory activities of N-acylsulfonamides using silica sulfuric acid as an efficient catalyst under both solvent-free and heterogeneous conditions. |
| 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. |
| AID166573 | Reduction of intraocular pressure in normotensive rabbits after treatment with 50 uL of compound (as HCl salt) at pH 5.5 in eye after 0 min from administration, to that of controls | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| 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. |
| 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. |
| AID1570392 | Toxicity in New Zealand White rabbit assessed as induction of eye lid closure at 2% administered topically to the eye | 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. |
| AID166027 | The compound was evaluated for fall in intraocular pressure (IOP) of Normotensive rabbits (20.2+/-2.3 mmHg) after treatment with one drop (50 microL) of a 2% solution at 60 min (pH 5.5) | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID75402 | In vivo intraocular pressure lowering in Glaucomatous Rabbits after the administration at a pH of 5.5, at time interval 60 min | 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. |
| 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. |
| 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. |
| 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. |
| AID238301 | Ki value against murine 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. |
| AID445830 | Reduction of intraocular pressure in normotensive New Zealand white rabbit assessed as time to reach maximal difference at 55 mM | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| 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. |
| AID167099 | Tested for ex vivo distribution in aqueous humor after topical administration in albino rabbits (Ocular tissue concentration after 1 hr) | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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). |
| 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. |
| 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. |
| AID445822 | Inhibition of human carbonic anhydrase 1 by CO2 hydrase stopped flow assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| 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. |
| 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. |
| AID166338 | Tested in vivo for lowering IOP (Intraocular Pressure)in Glaucomatous Rabbits at pH 5.5 after treatment with 50 uL, activity at 30 minutes | 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. |
| AID28733 | Partition coefficient (logD) (chloroform-buffer) | 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. |
| AID1570395 | Reduction of intraocular pressure in ocular normotensive New Zealand White rabbit administered topically to the eye measured for 0.5 to 8 hrs by by tonometry (Rvb = 12.00 +/- 6.81%) | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID263048 | Inhibition of human CA1 | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | QSAR study on topically acting sulfonamides incorporating GABA moieties: a molecular connectivity approach. |
| 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. |
| 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. |
| AID1183611 | Antiglaucoma activity in New Zealand rabbit model of carbomer-induced ocular hypertension assessed as reduction in intraocular pressure dosed with 50 uL of 2% compound solution and measured after 2 to 3 hrs | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Furazan and furoxan sulfonamides are strong α-carbonic anhydrase inhibitors and potential antiglaucoma agents. |
| 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. |
| 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 | |||
| 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. |
| AID26773 | Partition coefficient (logD) (chloroform-buffer) | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID47920 | Inhibition of human cloned Carbonic anhydrase II | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID48096 | Inhibition of human carbonic anhydrase II (hCA II) | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10 | Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV. |
| 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. |
| 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. |
| 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. |
| AID18312 | In vitro permeability through cornea without epithelium | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| AID445831 | Solubility at pH 6 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| AID166195 | Change in intraocular pressure (IOP) was measured in the normotensive pigmented rabbit in presence of MK-927 | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| 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. |
| AID1194932 | Antiglaucoma activity in New Zealand albino rabbit model of glaucoma assessed as reduction in intraocular pressure dosed as 2% eye drops immediately after injection of hypertonic saline measured 2 hrs post dose | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166593 | Tested for in vivo IOP-lowering of glaucomatous rabbits after topical administration at the specified interval( 30 min) at pH 5.5 | 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. |
| 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. |
| AID480751 | Inhibition of carbonic anhydrase 2 | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166026 | The compound was evaluated for fall in intraocular pressure (IOP) of Normotensive rabbits (20.2+/-2.3 mmHg) after treatment with one drop (50 microL) of a 2% solution at 30 min (pH 5.5) | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID311023 | Inhibition of human carbonic anhydrase 1 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| 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. |
| AID166247 | Fall of in vivo intraocular pressure (IOP) of glaucomatous rabbits at 60 min after treatment with one drop (50 uL) solution of 2% of CA inhibitor directly into eye | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| AID1461807 | Ocular hypotensive activity in New Zealand albino rabbit eye assessed as reduction in hypertonic saline-induced intraocular pressure at 2% administered as eye drop measured at 4 hrs post administration by applanation tonometry | 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. |
| AID17877 | In vitro permeability through intact cornea | 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. |
| AID146520 | In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 30 min | 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. |
| 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. |
| 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). |
| 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. |
| AID47713 | Inhibition of human carbonic anhydrase I (CAI) | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10 | Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV. |
| 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. |
| AID166435 | In vivo intraocular pressure (IOP) lowering at 0 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| AID166337 | Reduction of the elevated intraocular pressure (IOP) in alpha-chymotrypsin treated albino rabbit | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| 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). |
| AID48108 | Ex vivo inhibition of carbonic anhydrase II in iris - ciliary body of an albino rabbit at a concentration of 0.02% | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166577 | Reduction of intraocular pressure in normotensive rabbits after treatment with 50 uL of compound (as HCl salt) at pH 5.5 in eye after 90 min from administration, to that of controls | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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). |
| 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. |
| 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. |
| AID48128 | Compound was evaluated for binding affinity against bovine Carbonic anhydrase IV | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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). |
| 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. |
| 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. |
| 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. |
| AID166109 | Tested ex vivo for ocular tissue concentration against ciliary process after 2 hour of treatment with 50 uL | 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. |
| 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. |
| AID165938 | Compound was evaluated in vivo in glaucomatous rabbits (33.5+/-3.0 mmHg) for the intraocular pressure (IOP) lowering 90 min after topical administration with one drop of Carbonic anhydrase at a pH 5.5 | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID48284 | Inhibitory activity against bovine carbonic anhydrase IV (CA4), isolated from bovine lung microsomes | 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. |
| 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. |
| 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. |
| AID167706 | In vitro transcorneal accession rate (without epithelium) of compound was determined | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| 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. |
| 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. |
| AID166335 | Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 90 min at a pH of 5.5 | 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. |
| AID1200903 | Solubility of the compound | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure. |
| 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. |
| 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. |
| 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. |
| AID166110 | Tested ex vivo for ocular tissue concentration against cornea after 1 hour of treatment with 50 uL | 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. |
| 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. |
| AID165876 | Compound was evaluated in vivo in normotensive rabbits (23.5+/-2.6 mmHg) for the intraocular pressure (IOP) lowering 90 min after topical administration with one drop of Carbonic anhydrase inhibitor at a pH 5.5 | 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. |
| 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. |
| AID165872 | Compound was evaluated in vivo in normotensive rabbits (23.5+/-2.6 mmHg) for the intraocular pressure (IOP) lowering 30 min after topical administration with one drop of Carbonic anhydrase inhibitor at a pH 5.5 | 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. |
| AID166565 | In vivo intraocular pressure (IOP) lowering at 60 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| AID47939 | Inhibitory activity against human recombinant carbonic anhydrase II (CA2) | 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. |
| 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). |
| 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. |
| 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. |
| 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. |
| AID48110 | Ex vivo inhibition of carbonic anhydrase II in iris - ciliary body of an albino rabbit at a concentration of 0.5% | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. |
| AID50374 | Inhibitory activity against human recombinant carbonic anhydrase I (CA1) | 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. |
| 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? |
| AID146519 | In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 0 min | 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. |
| 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. |
| 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. |
| 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. |
| AID644381 | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins 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. |
| 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. |
| 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. |
| 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? |
| 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. |
| 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. |
| 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). |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166574 | Reduction of intraocular pressure in normotensive rabbits after treatment with 50 uL of compound (as HCl salt) at pH 5.5 in eye after 240 min from administration, to that of controls | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| AID26782 | Partition coefficient of hydrochloride salt (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? |
| 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. |
| AID1350489 | Anti-glaucoma activity in hypertonic saline-induced hypertensive New Zealand albino rabbit model assessed as decrease in intraocular pressure at 1 % instilled into eye vitreous along with 0.25% timolol measured at 2 hrs post administration by pneumatonome | 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. |
| 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. |
| AID23532 | Compound was tested for solubility in pH 5.80 buffer, at 25 degree C.(As hydrochloride salts) | 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? |
| AID747799 | Antiglaucoma activity in hypertensive New Zealand albino rabbit model assessed as decrease in carbomer-induced intraocular pressure at 2% administered to eye after 150 mins by tanometric analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo. |
| AID1570394 | Toxicity in New Zealand White rabbit assessed as head shaking at 2% administered topically to the eye | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166575 | Reduction of intraocular pressure in normotensive rabbits after treatment with 50 uL of compound (as HCl salt) at pH 5.5 in eye after 30 min from administration, to that of controls | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties. |
| 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. |
| AID166111 | Tested ex vivo for ocular tissue concentration against cornea after 2 hour of treatment with 50 uL | 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. |
| 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. |
| AID445824 | Inhibition of human carbonic anhydrase 4 by CO2 hydrase stopped flow assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| 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. |
| AID166248 | Fall of in vivo intraocular pressure (IOP) of glaucomatous rabbits at 90 min after treatment with one drop (50 uL) solution of 2% of CA inhibitor directly into eye | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| AID166568 | In vivo intraocular pressure (IOP) lowering at 90 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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 | |||
| AID598017 | Antiglaucoma activity in New Zealand rabbits assessed as inhibition of carbomer-induced ocular hypertension at 2 % in 50 uL administered into eye after 2 to 3 weeks of carbomer challenge (Rvb = 35.4 +/- 0.8 mmHg) | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID166735 | Tested for in vivo IOP-lowering of normotensive albino rabbits after topical administration at the specified interval (60 min) at pH 5.5 | 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. |
| AID480924 | Inhibition of carbonic anhydrase in Dutch belted rabbit iris ciliary body homogenate at 10 uM by titration assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. |
| AID445825 | Selectivity ratio of Ki for human CA2 to Ki for human CA4 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Nitric oxide-donating carbonic anhydrase inhibitors for the treatment of open-angle glaucoma. |
| 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. |
| AID780318 | Selectivity ratio of Ki for human carbonic anhydrase9 to Ki for human carbonic anhydrase2 | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. |
| AID146521 | In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 60 min | 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. |
| AID1821402 | Antiglaucoma activity in New Zealand albino rabbit assessed as reduction in intraocular pressure administered topically as eye drops measured after 4 hrs by pneumotonometer-analysis | 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. |
| 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. |
| AID75401 | In vivo intraocular pressure lowering in Glaucomatous Rabbits after the administration at a pH of 5.5, at time interval 30 min | 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. |
| 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. |
| AID50360 | Binding affinity against human carbonic anhydrase I (hCA I) | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13 | Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1681924 | Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer. |
| 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. |
| AID263050 | Inhibition of bovine CA4 | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | QSAR study on topically acting sulfonamides incorporating GABA moieties: a molecular connectivity approach. |
| 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. |
| AID1245275 | Inhibition of human recombinant carbonic anhydrase-2 expressed in Escherichia coli incubated for 15 mins by stopped-flow CO2 hydration assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents. |
| 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). |
| 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. |
| 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 | |||
| 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. |
| 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. |
| 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. |
| AID166739 | Tested for in vivo IOP-lowering of normotensive albino rabbits after topical administration at the specified interval (90 min) at pH 5.5 | 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. |
| AID21970 | Tested for solubility as hydrochloride, at pH 5.8 | 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. |
| 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. |
| 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. |
| AID311029 | Inhibition of human carbonic anhydrase 6 | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Carbonic anhydrases as targets for medicinal chemistry. |
| AID28908 | The chloroform-buffer partition coefficient as sodium salts at pH 7 | 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. |
| 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. |
| AID47919 | Compound was evaluated for the inhibitory constant towards Human Carbonic anhydrase II (HCA II) | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Application of the three-dimensional structures of protein target molecules in structure-based drug design. |
| 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. |
| AID1350491 | Anti-glaucoma activity in hypertonic saline-induced hypertensive New Zealand albino rabbit model assessed as decrease in intraocular pressure at 1% instilled into eye vitreous along with 0.25% timolol measured at 4 hrs post administration by pneumatonomet | 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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) | 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? |
| AID1346202 | Human carbonic anhydrase 7 (4.2.1.1 Carbonate dehydratases) | 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. |
| AID1345957 | Human carbonic anhydrase 14 (4.2.1.1 Carbonate dehydratases) | 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. |
| 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. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 1994 | Protein science : a publication of the Protein Society, Jan, Volume: 3, Issue:1 | Positions of His-64 and a bound water in human carbonic anhydrase II upon binding three structurally related inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1994 | Protein science : a publication of the Protein Society, Jan, Volume: 3, Issue:1 | Positions of His-64 and a bound water in human carbonic anhydrase II upon binding three structurally related inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (0.13) | 18.7374 |
| 1990's | 144 (18.32) | 18.2507 |
| 2000's | 359 (45.67) | 29.6817 |
| 2010's | 223 (28.37) | 24.3611 |
| 2020's | 59 (7.51) | 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 (80.72) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 261 (31.22%) | 5.53% |
| Reviews | 58 (6.94%) | 6.00% |
| Case Studies | 103 (12.32%) | 4.05% |
| Observational | 5 (0.60%) | 0.25% |
| Other | 409 (48.92%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Multicenter, Double-Blind, Active Comparator-controlled Study to Evaluate the Safety and Efficacy of MK0507A in Patients With Glaucoma and Ocular Hypertension Who Are Inadequately Controlled on Beta-Blockers [NCT00449956] | Phase 3 | 474 participants (Actual) | Interventional | 2007-03-12 | Completed | ||
| A Non-inferiority in the Intraocular Pressure Decrease of the Preservative-free Ophthalmic Solution PRO-122 Versus Concomitant Therapy in Subjects With Uncontrolled Primary Open-angle Glaucoma [NCT03193333] | Phase 3 | 51 participants (Anticipated) | Interventional | 2017-11-06 | Recruiting | ||
| [NCT01111890] | Phase 4 | 70 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
| A Randomized Controlled Trial Comparing the Effect of Topical Dorzolamide-Timolol Versus Placebo Combined With Intravitreal Anti-Vascular Endothelial Growth Factor (VEGF) Injections in Patients With Neovascular Age-Related Macular Degeneration Who Are Inc [NCT03034772] | Phase 2/Phase 3 | 52 participants (Actual) | Interventional | 2017-02-08 | Completed | ||
| Clinical Study to Evaluate the Non-inferiority of PRO-122 an Ophthlamic Solution Manufactured by Laboratorios Sophia, Previous Treatment With Krytantek Ofteno ®, in Subjects With Primary Open-Angle Glaucoma or Ocular Hypertension. [NCT03257813] | Phase 3 | 60 participants (Actual) | Interventional | 2016-04-01 | Completed | ||
| Impact of Timolol/Dorzolamide Therapy on Autoregulation in Glaucoma Patients [NCT02053298] | Phase 4 | 30 participants (Anticipated) | Interventional | 2014-01-31 | Recruiting | ||
| [NCT01284166] | Phase 3 | 0 participants (Actual) | Interventional | 2013-07-31 | Withdrawn(stopped due to Study was never initiated due to company decision. No study subjects were ever enrolled or treated.) | ||
| Choroidal Thickness and Its Correlations With Ocular Parameters in Cases With Primary Open-angle Glaucoma [NCT03966560] | Phase 4 | 96 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Comparative Clinical Study of The Safety And Efficacy of A New Fixed-Combination of Timolol-Brimonidine-Dorzolamide In Patients With Open Angle Glaucoma Or Ocular Hypertension [NCT01062971] | Phase 2 | 124 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| A Single Dose Patient Preference Study Comparison in Patients With Open-Angle Glaucoma or Ocular Hypertension [NCT00576342] | Phase 3 | 129 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
| Circadian Rhythms of Aqueous Humor Dynamics in Humans [NCT00572936] | Phase 2 | 30 participants (Actual) | Interventional | 2006-03-13 | Completed | ||
| Stop Retinal Ganglion Cell Dysfunction Study [NCT02390284] | Phase 3 | 500 participants (Anticipated) | Interventional | 2015-09-30 | Active, not recruiting | ||
| A Randomized, Open-label, Controlled, Comparative Study of Efficacy and Safety of Dorzol Eye Drops, 20 mg/mL (JGL dd, Croatia) vs Trusopt® Eye Drops, 20 mg/mL (Merck Sharp & Dohme, France) in Patients With Primary Open-angle Glaucoma [NCT05973305] | Phase 3 | 118 participants (Actual) | Interventional | 2017-04-05 | Completed | ||
| Phase IV, Multicenter, Double-blind, Randomized, Controlled, Parallel-group, Trial to Evaluate the Efficacy and Safety of Dozolamide 2%/Timolol 0,5% PF vs Dorzolamide 2%/Timolol 0,5% BAK-preserved in OAG or OH [NCT05857267] | Phase 4 | 84 participants (Anticipated) | Interventional | 2023-03-07 | Recruiting | ||
| Comparison of Brimonidine 0.15% Purite, Dorzolamide 2%, and Brinzolamide 1% as Adjunctive Therapy to Prostaglandin Analogs [NCT00675207] | Phase 4 | 120 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
| [NCT00822055] | Phase 4 | 140 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
| Prospective, Open-label, Single-arm Study to Evaluate Efficacy and Safety of Combination Therapy of Timolol and Dorzolamide (COSOPT) as Initial Treatment for Patients With Normal Tension Glaucoma [NCT00832377] | Phase 2 | 37 participants (Actual) | Interventional | 2009-04-24 | Completed | ||
| Phase IV Clinical Study to Compare the Efficacy of the Krytantek Ofteno PF® Plus Gaap Ofteno PF® Combination to the Krytantek Ofteno PF® Plus Gaap Ofteno PF® Combination, in Primary Open Angle Glaucoma or Ocular Hypertension Patients. [NCT04702789] | Phase 4 | 28 participants (Actual) | Interventional | 2021-10-19 | Terminated(stopped due to For interests of sponsor.) | ||
| Randomized, Double-Masked, Active Controlled, Crossover Phase III Equivalence Study of Dorzolamide 2% Eye Drops Solution In Subjects With Open Angle Glaucoma Or Ocular Hypertension [NCT00878917] | Phase 3 | 32 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| A Multicenter, Open-Label Study To Evaluate The Tolerability Of Preservative Free Dorzolamide-Timolol Therapy In Patients Untreated With Open-Angle Glaucoma Or Ocular Hypertension And Dry Eye(s) [NCT00545064] | Phase 4 | 176 participants (Actual) | Interventional | 2007-05-23 | Completed | ||
| 12-Month Stability of Diurnal IOP Control on Cosopt [NCT00379834] | Phase 4 | 10 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
| Effectiveness and Safety of Timolol and Dorzolamide Loaded Contact Lenses [NCT02852057] | Phase 1 | 2 participants (Actual) | Interventional | 2018-01-18 | Completed | ||
| Pharmacological Intervention Against Diabetic Retinal Flow Disturbances. [NCT00619034] | 87 participants (Actual) | Interventional | 2007-09-30 | Completed | |||
| 24-hour Efficacy and Ocular Surface Health With PF Tafluprost and Combined Therapy With PF Tafluprost and Dorzolamide/Timolol Fixed Combination in Open-angle Glaucoma Subjects Insufficiently Controlled With Latanoprost [NCT02802137] | Phase 4 | 43 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
| Phase I Clinical Study, to Evaluate the Safety and Tolerability of the Preservative-free Ophthalmic Solution PRO-122 Compared With Krytantek Ofteno®, Elaborated by Sophia Laboratories, S.A. of C.V. on the Ocular Surface of Ophthalmologically and Clinicall [NCT03966365] | Phase 1 | 24 participants (Actual) | Interventional | 2019-05-02 | Completed | ||
| Quality of 24-hour Intraocular Pressure Control Obtained With Dorzolamide/Timolol Fixed Combination (DTFC) Compared With the Brimonidine/Timolol Fixed Combination (BTFC) in Subjects With Primary Open-angle Glaucoma [NCT00972257] | Phase 4 | 64 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| A Comparative Analysis of the Effects of Cosopt® Versus Xalacom® on Ocular Hemodynamics and Intraocular Pressure in Patients With Primary Open-angle Glaucoma [NCT00815373] | 0 participants (Actual) | Interventional | 2008-12-31 | Withdrawn(stopped due to no participants recruded.) | |||
| [NCT00822081] | Phase 4 | 140 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
| Change in Optic Nerve Head Blood Flow,Optic Nerve Topography and Diurnal Fluctuation of Intraocular Pressure and Pulsatile Ocular Blood Flow in Glaucoma:Cosopt and Xalatan vs Xalatan Alone [NCT00957190] | Phase 4 | 25 participants (Actual) | Interventional | 2009-05-04 | Completed | ||
| Augmented Macular Pigment Supplement and Pericentral Visual Function: a Randomized Controlled Trial [NCT04676126] | Phase 4 | 0 participants (Actual) | Interventional | 2021-05-31 | Withdrawn(stopped due to IRB records show administrative closure on 12/16/21. No subjects enrolled.) | ||
| A Double-masked Comparison of the Effect of Dorzolamide and Timolol on Optic Disk Blood Flow in Patients With Open Angle Glaucoma [NCT00991822] | Phase 2/Phase 3 | 160 participants (Actual) | Interventional | 1999-05-31 | Completed | ||
| A 12 Week, Open-Label, Study to Evaluate the Effectiveness of Dorzolamide-Timolol as First Line Therapy to Reduce Intraocular Pressure in Patients With Untreated Open Angle Glaucoma (OAG) or Ocular Hypertension (OH) [NCT00546286] | Phase 3 | 170 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
| Brimonidine Purite 0.15% Versus Dorzolamide 2% Used as Adjunctive Therapy to Latanoprost [NCT00348400] | Phase 4 | 0 participants | Interventional | Completed | |||
| Trusopt and Cosopt; Ocular Perfusion Pressure and Blood Flow: New Long-term Prospective Data [NCT01145898] | 56 participants (Actual) | Observational | 2010-06-30 | Completed | |||
| A Prospective, Randomized Study Comparing the Effects of Topical Aqueous Suppressants on Intraocular Gas Duration Following Pars Plana Vitrectomy [NCT01257698] | 21 participants (Actual) | Interventional | 2010-02-28 | Completed | |||
| The Effect of Myocilin Genetic Variants on Intraocular Pressure and Blood Pressure Variation in Sitting and Supine Positions. [NCT00906087] | Phase 4 | 14 participants (Actual) | Interventional | 2009-08-04 | Completed | ||
| [NCT00333125] | Phase 3 | 319 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
| Patient Preference Comparison of AZARGA Versus COSOPT After Single Doses in Patients With Open-Angled Glaucoma or Ocular Hypertension [NCT01471158] | Phase 4 | 120 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| A Randomized, Open-label, 2-period, Parallel Group, Multiple-dose Study to Evaluate the Drug-drugs Interaction Between Dorzolamide and Brimonidine in Healthy Korean Male Volunteers [NCT02967614] | Phase 1 | 32 participants (Actual) | Interventional | 2016-12-31 | Completed | ||
| [NCT00273442] | Phase 4 | 60 participants | Interventional | 2005-11-30 | Completed | ||
| [NCT00273481] | Phase 4 | 33 participants | Interventional | 2005-09-30 | Completed | ||
| Randomized, Multicenter, Dbl-Masked, Parallel Study Evaluating the 24 Hr. Diurnal Ocular Hypotensive Effect of 2% Dorzolamide Hydrochloride/0.5% Timolol Maleate Combo. Ophthalmic Sol. in Patients w/ Open Angle Glaucoma or Ocular Hypertension [NCT00108017] | Phase 3 | 330 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
| Treatment of Cystoid Macular Edema in Patients With Retinal Degeneration [NCT00716586] | Phase 4 | 44 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
| Effects of Common Topical Glaucoma Therapy on Optic Nerve Head Blood Flow Autoregulation During Increased Arterial Blood Pressure and Artificially Elevated Intraocular Pressure in Healthy Humans [NCT00275756] | 0 participants (Actual) | Interventional | 2008-09-30 | Withdrawn | |||
| 24-hour IOP With DTFC and LTFC Monotherapies and the Adjunctive Therapy of DTFC and Latanoprost in Open-angle Glaucoma Insufficiently Controlled With Latanoprost Monotherapy. [NCT00397241] | Phase 4 | 33 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
| Ocular Blood Flow Measured by HRF and CLBF in Newly Diagnosed and Early Glaucoma Patients Before and After Instillation of Dorzolamide 2% [NCT00152932] | 17 participants (Anticipated) | Interventional | 2005-05-31 | Recruiting | |||
| Earlier Intraocular Pressure Control After Ahmed Glaucoma Valve Implantation for Glaucoma [NCT00869141] | Phase 4 | 52 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Effect of Topical Aqueous Suppressants on Response to Intravitreal Anti-vascular Endothelial Growth Factor Injections in Age-related Macular Degeneration (AMD), Retinal Vein Occlusions (RVO) or Diabetic Macular Edema (DME). [NCT02571972] | Phase 2 | 14 participants (Actual) | Interventional | 2015-02-01 | Completed | ||
| A Prospective, Randomized Study Comparing the Effects of Topical Aqueous Suppressants on Intraocular Gas Duration Following Scleral Buckling and Pneumatic Retinopexy. [NCT01843920] | 21 participants (Actual) | Interventional | 2011-06-30 | Completed | |||
| [NCT00273429] | Phase 4 | 0 participants | Interventional | 2005-04-30 | Completed | ||
| Patient Preference Comparison of AZARGA Versus COSOPT in Patients With Open-Angle Glaucoma or Ocular Hypertension [NCT01340014] | Phase 4 | 112 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| [NCT00273455] | Phase 4 | 34 participants | Interventional | 2006-01-31 | Completed | ||
| A Study of a Glaucoma Therapy to Treat Open-Angle Glaucoma or Ocular Hypertension [NCT00314171] | Phase 3 | 437 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
| The 24 Control of IOP in Ocular Hypertension: a Cross-over Study on Inflow Versus Outflow Drugs. [NCT01655758] | Phase 4 | 61 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
| A Phase IV Study of Travoprost + Brinzolamide to Treat Glaucoma or Ocular Hypertension [NCT00471380] | Phase 4 | 46 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
| Efficacy of Dorzolamide as an Adjuvant to Improve Visual Function After Focal Photocoagulation Treatment in Diabetic Patients With Clinically Significant Macular Edema [NCT02227745] | 60 participants (Anticipated) | Observational | 2014-01-31 | Recruiting | |||
| Combined Intravitreal Bevacizumab With Topical Timolol-Dorzolamide Eye Drops in Diabetic Macular Edema [NCT05083689] | Phase 2/Phase 3 | 62 participants (Anticipated) | Interventional | 2021-10-06 | Active, not recruiting | ||
| To Prove the Non-inferiority of Cosopt Compared to Xalatan in the Aspects of Intraocular Pressure and Ocular Perfusion Pressure in Subjects With Normal Tension Glaucoma [NCT01175902] | 44 participants (Actual) | Interventional | 2011-03-31 | Completed | |||
| Clinical Evaluation of Patients With X-linked Retinoschisis (XLRS) [NCT02331173] | 66 participants (Actual) | Observational | 2012-11-30 | Completed | |||
| Effect of Cosopt Versus Combigan on Retinal Vascular Autoregulation in Primary Open Angle Glaucoma (POAG) [NCT00824824] | 21 participants (Actual) | Interventional | 2009-01-31 | Completed | |||
| [NCT00811850] | Phase 4 | 15 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| Effect of Topical Anti-glaucoma Medications on Late Pupillary Light Reflex, as Evaluated by Pupillometry [NCT02522039] | 21 participants (Actual) | Interventional | 2014-05-31 | Completed | |||
| The Efficacy and Safety of Brinzolamide 1%/Timolol 0.5% Fixed Combination Versus Dorzolamide 1%/Timolol 0.5% in Patients With Open-Angle Glaucoma and Ocular Hypertension [NCT02325518] | Phase 4 | 218 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
| Efficacy and Safety of Prostaglandin Analogue and Carbonic Anhydrase Inhibitor for the Treatment of Pediatric Glaucoma [NCT01527682] | Phase 2 | 37 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||