Isoniazid (INH) is a synthetic drug used primarily to treat tuberculosis (TB) and is considered one of the most effective drugs available for this purpose. It is a prodrug that inhibits the synthesis of mycolic acids, essential components of the mycobacterial cell wall. The synthesis of isoniazid involves the reaction of hydrazine with isonicotinic acid. Isoniazid is typically administered orally and is metabolized in the liver. It is often used in combination with other drugs to treat TB, particularly multidrug-resistant strains. Isoniazid is also used to prevent TB in people who are at high risk of infection. It is a first-line drug for treating TB and its importance lies in its effectiveness, low cost, and availability. Ongoing research is aimed at understanding the mechanisms of resistance to isoniazid, optimizing its use, and developing new drugs based on its structure to combat drug-resistant TB. The drug can cause various side effects such as liver damage, peripheral neuropathy, and drug-induced lupus. It is important to note that isoniazid should only be used under the supervision of a healthcare professional.'
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). [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 | 3767 |
| CHEMBL ID | 64 |
| CHEBI ID | 6030 |
| SCHEMBL ID | 228 |
| SCHEMBL ID | 2998929 |
| MeSH ID | M0011772 |
| Synonym |
|---|
| BIDD:GT0140 |
| BB 0240534 |
| UPCMLD0ENAT5791176:001 |
| isonicotinic acid hydrazide(isoniazide) |
| isonicotinic acid hydrazide (isoniazid) |
| isonicotinhydrazide |
| bdbm50336507 |
| isoniazid (inh) |
| 4-pyridinecarbohydrazide(isoniazid) |
| isonicotinic acid hydrazide(isoniazid) |
| 4-pyridinecarbohydrazide |
| isonicotinsaeurehydrazid |
| CHEBI:6030 , |
| isonicotinoylhydrazide |
| pyridine-4-carboxylic acid hydrazide |
| MLS000069444 , |
| DIVK1C_000070 |
| KBIO1_000070 |
| inchi=1/c6h7n3o/c7-9-6(10)5-1-3-8-4-2-5/h1-4h,7h2,(h,9,10 |
| SPECTRUM_000853 |
| BPBIO1_001322 |
| vederon |
| tisiodrazida |
| tibivis |
| sanohidrazina |
| antimicina |
| percin |
| hidrulta |
| defonin |
| chemiazid |
| pyreazid |
| wln: t6nj dvmz |
| INH , |
| hidrun |
| isolyn |
| retozide |
| tibusan |
| l 1945 |
| tekazin |
| ebidene |
| unicocyde |
| nicotibine |
| isidrina |
| zinadon |
| 4-pyridinecarboxylic acid hydrazide |
| tubicon |
| robisellin |
| isonide |
| tuberian |
| nsc 9659 |
| nsc9659 |
| hyzyd |
| antituberkulosum |
| hia , |
| tubecotubercid |
| stanozide |
| nicazide |
| hydrazide |
| tibemid |
| nicetal |
| isobicina |
| 4-pyridylcarbonylhydrazide |
| isonico |
| neo-tizide |
| tibinide |
| isozide |
| nicizina |
| tb-vis |
| gink |
| isohydrazide |
| fimalene |
| azuren |
| nidaton |
| tibison |
| hidranizil |
| laniazid |
| sauterzid |
| andrazide |
| isonicotinylhydrazine |
| isonin |
| raumanon |
| isonizide |
| isocid |
| armazide |
| isotinyl |
| rimifon |
| isozyd |
| isonilex |
| zonazide |
| isonicotinhydrazid |
| isonicotinic hydrazide |
| usaf cb-2 |
| robiselin |
| cortinazine |
| hydrazid |
| inizid |
| razide |
| pycazide |
| isoniacid |
| nitebannsc 9659 |
| nevin |
| nicotisan |
| nydrazid |
| teebaconin |
| nicozide |
| isonicotinoyl hydrazide |
| niadrin |
| tebilon |
| fsr 3 |
| nidrazid |
| in-73 |
| ido-tebin |
| armazid |
| isotebezid |
| bacillin |
| isonicotinic acid hydrazide |
| 5015 r.p. |
| neoxin |
| ertuban |
| preparation 6424 |
| nsc-9659 |
| roxifen |
| unicozyde |
| isonerit |
| sauterazid |
| evalon |
| hidrasonil |
| tebexin |
| neoteben |
| tibizide |
| niconyl |
| atcotibine |
| isonindon |
| zidafimia |
| nikozid |
| rimicid |
| rimiphone |
| niplen |
| tebecid |
| inah |
| diforin |
| vazadrine |
| nyscozid |
| isonicotan |
| tubilysin |
| chemidon |
| tebenic |
| isocidene |
| dibutin |
| isotebe |
| ditubin |
| isoniazid sa |
| armacide |
| tisin |
| isonikazid |
| pyricidin |
| tubazid |
| tb-phlogin |
| tebos |
| pyrizidin |
| tibazide |
| isocotin |
| ru-ef-tb |
| neumandin |
| isoniton |
| isonicotinohydrazide |
| cotinizin |
| cemidon |
| cotinazin |
| dinacrin |
| isonidrin |
| tb-razide |
| tizide |
| nitadon |
| tubeco |
| 4-pyridinecarboxylic acid, hydrazide |
| isonex |
| isonirit |
| tubazide |
| isonicazide |
| eralon |
| isoniazide , |
| laniozid |
| nicotibina |
| pelazid |
| iscotin |
| tyvid |
| cedin |
| isonicid |
| isonicotinyl hydrazide |
| idrazil |
| isonicotil |
| rimitsid |
| phthisen |
| bp 5015 |
| mybasan |
| hycozid |
| eutizon |
| pyridicin |
| ismazide |
| tubomel |
| hyozid |
| PRESTWICK_578 |
| NCGC00016244-01 |
| cas-54-85-3 |
| SPECTRUM5_000876 |
| BSPBIO_000021 |
| BSPBIO_002204 |
| BPBIO1_000025 |
| pyridine-4-carbohydrazide |
| fsr-3 |
| inhd20 |
| rp-5015 |
| OPREA1_396155 |
| IDI1_000070 |
| BIOMOL-NT_000288 |
| PRESTWICK3_000161 |
| PRESTWICK2_000161 |
| STK086288 |
| NCGC00022648-03 |
| continazine |
| 5015 rp |
| niteban |
| bacillen |
| i.a.i. |
| tebemid |
| isonizida |
| frs-3 |
| rp 5015 |
| anidrasona |
| hydra |
| isonicotinoylhydrazine |
| isokin |
| fetefu |
| ry-ef-tb |
| inh-burgthal |
| tubizid |
| tibiazide |
| tubercid |
| isotamine |
| abdizide |
| AB00052025 |
| MLS001055327 |
| hsdb 1647 |
| isonicotinsaeurehydrazid [german] |
| einecs 200-214-6 |
| dow-isoniazid |
| isoniazida [inn-spanish] |
| ccris 351 |
| 4-pyridinecarbonylhydrazine |
| idrazide dell'acido isonicotinico [italian] |
| isoniazidum [inn-latin] |
| 4-(hydrazinocarbonyl)pyridine |
| isozid |
| cedin (aerosol) |
| ai3-23936 |
| 4-pyridinecarboxylic hydrazide |
| ISONIAZID , |
| 54-85-3 |
| C07054 |
| lanizid |
| DB00951 |
| laniazid (tn) |
| D00346 |
| isoniazid (jp17/usp/inn) |
| NCGC00022648-05 |
| NCGC00022648-06 |
| NCGC00022648-04 |
| smr000059082 |
| KBIOSS_001333 |
| KBIO2_006469 |
| KBIO3_001424 |
| KBIO2_001333 |
| KBIOGR_000423 |
| KBIO2_003901 |
| SPBIO_001942 |
| SPECTRUM2_000107 |
| PRESTWICK0_000161 |
| PRESTWICK1_000161 |
| SPBIO_000094 |
| SPECTRUM4_000022 |
| NINDS_000070 |
| SPECTRUM3_000472 |
| SPECTRUM1500355 |
| azt + isoniazid |
| NCGC00016244-02 |
| hydrazide, isonicotinic acid |
| isonicotinate hydrazide |
| isonicotinylhydrazide |
| HMS2091N19 |
| HMS2089I16 |
| CHEMBL64 , |
| isoniazidum |
| ipcazide |
| dianicotyl |
| HMS500D12 |
| I0138 , |
| HMS1920H09 |
| HMS1568B03 |
| AKOS000119062 |
| NCGC00022648-07 |
| KUC109571N |
| ksc-27-048 |
| HMS2095B03 |
| HMS3259E19 |
| BBL008409 |
| NCGC00258919-01 |
| dtxsid8020755 , |
| NCGC00254094-01 |
| tox21_300193 |
| dtxcid20755 |
| tox21_201367 |
| tox21_113640 |
| A830384 |
| nsc-757078 |
| pharmakon1600-01500355 |
| nsc757078 |
| HMS2234G04 |
| CCG-39710 |
| NCGC00016244-06 |
| NCGC00016244-05 |
| NCGC00016244-12 |
| NCGC00016244-08 |
| NCGC00016244-10 |
| NCGC00016244-03 |
| NCGC00016244-07 |
| NCGC00016244-04 |
| NCGC00016244-11 |
| NCGC00016244-09 |
| isonicotinyl hydrazine |
| FT-0670476 |
| isoniazida |
| v83o1voz8l , |
| unii-v83o1voz8l |
| idrazide dell'acido isonicotinico |
| isoniazid [usp:inn:ban:jan] |
| F0391-0007 |
| FT-0627424 |
| NCGC00016244-14 |
| PS-4129 |
| 4-pyridinecarboxylic acid hydrazide [who-ip] |
| isonicotinic acid hydrazide [who-ip] |
| isonicotinic acid hydrazide [iarc] |
| isoniazid [inn] |
| isoniazid [vandf] |
| isoniazid [ep impurity] |
| isoniazid [jan] |
| isoniazid [mi] |
| isoniazid component of rifamate |
| rifamate component isoniazid |
| isoniazid [usp-rs] |
| isoniazid [mart.] |
| isoniazid [usp monograph] |
| isoniazid component of rifater |
| isoniazid [hsdb] |
| isoniazidum [who-ip latin] |
| isoniazid [who-ip] |
| isoniazid [orange book] |
| isoniazid [who-dd] |
| isoniazid [ep monograph] |
| rifater component isoniazid |
| EPITOPE ID:141801 |
| S1937 |
| HMS3373O01 |
| HY-B0329 |
| isonicotinicacid hydrazide |
| niz , |
| NC00513 |
| SCHEMBL228 |
| tox21_113640_1 |
| NCGC00016244-15 |
| SCHEMBL2998929 |
| AB00052025-20 |
| AB00052025-21 |
| isonicotinic acid hydrazone |
| rifater (salt/mix) |
| mayambutol |
| component of niadox (salt/mix) |
| 4-pyridylcarbonyl hydrazide |
| [(4-pyridinylcarbonyl)oxy]hydrazine |
| AE-641/02310003 |
| STR00210 |
| isoniazid, pharmaceutical??secondary??standard;??certified??reference??material |
| AB00052025_23 |
| AB00052025_25 |
| AB00052025_24 |
| OPERA_ID_454 |
| AB00052025_22 |
| mfcd00006426 |
| isoniazid, certified reference material, tracecert(r) |
| SR-01000003025-2 |
| sr-01000003025 |
| isoniazid, united states pharmacopeia (usp) reference standard |
| isoniazid, european pharmacopoeia (ep) reference standard |
| isoniazid, analytical standard, >=99% (tlc) |
| HMS3655L03 |
| D70582 |
| isoniazid, vetec(tm) reagent grade, 98% |
| SR-01000003025-3 |
| SBI-0051419.P003 |
| HMS3712B03 |
| Z58981801 |
| SY010614 |
| SW196752-3 |
| isonicotinic acid hydrazid |
| Q423169 |
| gtpl12761 |
| isoniazid (tubizid) |
| isoniazid(tubizid) |
| soniazid,(s) |
| BCP13791 |
| BRD-K87202646-001-26-8 |
| EN300-18498 |
| isoniazid; pyridine-4-carbohydrazide |
| anti-tnf monoclonal antibody & inh |
| isonicotinicacidhydrazide |
| isoniazida (inn-spanish) |
| isonicotinsaurehydrazid |
| isoniazid (usp:inn:ban:jan) |
| t.b. razide |
| isoniazid (usp-rs) |
| isoniazid (ep impurity) |
| isonicotinic acid hydrazide (iarc) |
| isozin |
| isoniazid (mart.) |
| isoniazidum (inn-latin) |
| isoniazid (ep monograph) |
| dinocrin |
| ((4-pyridinylcarbonyl)oxy)hydrazine |
| isoniazid (usp monograph) |
| isoniazid 300 mg |
Isoniazid is a cornerstone of modern tuberculosis (TB) therapy and targets the enoyl ACP reductase InhA, a key enzyme in mycolic acid biosynthesis. Excessive usage can lead to serious consequences such as hepatotoxicity, neurotoxicity, and even coma and death.
Isoniazid-resistant TB has a good prognosis in DK. Isoniazide has a high penetration rate into the pleural effusion in most patients.
Isoniazid (INH) has been a first-line drug for the treatment of tuberculosis for more than 40 years. The mechanism by which isoniazids mediates disruption of heme synthesis has been unclear. IsoniazID neurotoxicity has never been reported to cause bilateral dentate hyperintensities.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Isoniazid-resistant TB has a good prognosis in DK. " | ( Isoniazid-resistant tuberculosis in Denmark: mutations, transmission and treatment outcome. Andersen, AB; Andersen, PH; Bang, D; Thomsen, VØ, 2010) | 3.25 |
| "As isoniazide has a high penetration rate into the pleural effusion in most patients, continuous oral administration of isoniazid has been sufficient to achieve an effective treatment concentration, and intrapleural injection of isoniazide may seem unnecessary for non-drug-resistant tuberculosis pleurisy." | ( [Determination of isoniazide concentration in pleural effusion and its pleural permeability in patients with tuberculous pleurisy]. Huang, G; Li, G; Liu, S; Liu, Y; Zhang, J; Zhang, Q; Zhu, S, 2012) | 1.33 |
| "Isoniazid has a low therapeutic margin and produces life threatening signs in dogs ingesting single 300 mg human tablets." | ( Treatment of acute isoniazid overdose in dogs. Barret, GH; Buck, WB; Holding, J; Knight, MK; Villar, D, 1995) | 1.34 |
| "Isoniazid(INH, H) has been a key drug for treating drug-susceptible tuberculosis (TB) for nearly seventy years. " | ( [Association between isoniazid induced hepatotoxicity and host N-acetyltransferase 2 polymorphisms]. Guo, JQ; Tang, S; Yan, XF; Yang, S, 2022) | 2.48 |
| "Isoniazid has recently been reported to upregulate Alas1 but downregulate Fech protein levels in mice; however, the mechanism by which isoniazid mediates disruption of heme synthesis has been unclear." | ( The Isoniazid Metabolites Hydrazine and Pyridoxal Isonicotinoyl Hydrazone Modulate Heme Biosynthesis. Brewer, CT; Chen, T; Edwards, A; Lee, RE; Low, J; Lu, Y; Wu, J; Yang, L, 2019) | 1.79 |
| "Isoniazid neurotoxicity has never been reported to cause bilateral dentate hyperintensities, for which the differentials are few and include metronidazole toxicity." | ( Isoniazid-induced cerebellitis: a disguised presentation. John, M; Peter, P, 2014) | 2.57 |
| "Isoniazid has been the backbone of tuberculosis chemotherapy for 6 decades. " | ( Global and Regional Burden of Isoniazid-Resistant Tuberculosis. Becerra, MC; Jenkins, HE; Keshavjee, S; Rodriguez, CA; Yuen, CM, 2015) | 2.15 |
| "Isoniazid (INH) has been a first-line drug for the treatment of tuberculosis for more than 40 years. " | ( Protein Targets of Isoniazid-Reactive Metabolites in Mouse Liver in Vivo. Galeva, NA; Hanzlik, RP; Koen, YM; Metushi, IG; Uetrecht, J, 2016) | 2.21 |
| "Isoniazid (ISO) has been reported to inhibit the hepatic aldehyde dehydrogenase (ALDH) and to cause a disulfiram (DIS)-like reaction, albeit there are no reports demonstrating increased blood acetaldehyde levels after co-administration of ISO with alcohol. " | ( The Alcohol Intolerance Produced by Isoniazid Is Not Due to a Disulfiram-Like Reaction Despite Aldehyde Dehydrogenase Inhibition. Boumba, V; Karamanakos, PN; Marselos, M; Pappas, P; Vougiouklakis, T, 2016) | 2.15 |
| "Isoniazid-resistant TB has a good prognosis in DK. " | ( Isoniazid-resistant tuberculosis in Denmark: mutations, transmission and treatment outcome. Andersen, AB; Andersen, PH; Bang, D; Thomsen, VØ, 2010) | 3.25 |
| "Isoniazid (INH) has been the mainstay of treatment of latent tuberculosis infection for almost 50 years. " | ( Treatment of latent tuberculosis infection: An update. Lobue, P; Menzies, D, 2010) | 1.8 |
| "Isoniazid resistance has been described before in those who are immunocompromised." | ( Human bovine tuberculosis - remains in the differential. Bilal, S; Iqbal, M; Murphy, P; Power, J, 2010) | 1.08 |
| "As isoniazide has a high penetration rate into the pleural effusion in most patients, continuous oral administration of isoniazid has been sufficient to achieve an effective treatment concentration, and intrapleural injection of isoniazide may seem unnecessary for non-drug-resistant tuberculosis pleurisy." | ( [Determination of isoniazide concentration in pleural effusion and its pleural permeability in patients with tuberculous pleurisy]. Huang, G; Li, G; Liu, S; Liu, Y; Zhang, J; Zhang, Q; Zhu, S, 2012) | 1.33 |
| "Isoniazid has little significant or serious toxicity." | ( Isoniazid therapy in chronic ulcerative colitis; a preliminary report. SUSNOW, DA, 1954) | 2.4 |
| "Isoniazid (INH) has neurotoxic effects such as seizure, poor concentration, subtle reduction in memory, anxiety, depression and psychosis. " | ( The effects of isoniazid on hippocampal NMDA receptors: protective role of erdosteine. Cicek, E; Delibas, N; Gokalp, O; Ozcelik, N; Ozer, MK; Sutcu, R; Uz, E; Yilmaz, HR, 2005) | 2.12 |
| "Isoniazid has the potential to induce fever, and this is thought to be a hypersensitivity reaction." | ( Spiking fever induced by isoniazid. Davis, HL; Henderson, RP; Self, TH, 1983) | 1.29 |
| "(4) Isoniazid prophylaxis has been shown to be effective in reducing later reactivation of primary tuberculosis." | ( Tuberculosis surveillance of hospital personnel. Gaeuman, JV, 1981) | 0.74 |
| "Isoniazid has been shown by in vitro study to reduce Clinitest tablets. " | ( Noneffect of isoniazid on urine glucose tests. Self, TH; Wester, VL, ) | 1.94 |
| "Isoniazid has adverse effects including hepatitis and peripheral neuropathy (common) and convulsions (rare)." | ( Reversible seizures and mental status changes in a dialysis patient on isoniazid preventive therapy. Asnis, DS; Bhat, JG; Melchert, AF, 1993) | 1.24 |
| "Isoniazid has a low therapeutic margin and produces life threatening signs in dogs ingesting single 300 mg human tablets." | ( Treatment of acute isoniazid overdose in dogs. Barret, GH; Buck, WB; Holding, J; Knight, MK; Villar, D, 1995) | 1.34 |
| "Isoniazid has been the accepted drug for use as prophylaxis for TB in immunocompetent patients, and there is evidence that isoniazid is also effective in HIV-positive, PPD-positive patients." | ( Prophylaxis for tuberculosis in Europe--ongoing research. Carosi, G; Matteelli, A, 1996) | 1.02 |
| "Isoniazid for 6-12 mo has been the mainstay of treatment for LTBI in the United States for more than 30 yr." | ( Targeted tuberculin testing and treatment of latent tuberculosis infection. American Thoracic Society. , 2000) | 1.03 |
| "Isoniazid (INH) has been the mainstay of preventive therapy for 40 years, but its use is limited by concerns about toxicity and poor adherence." | ( New developments in the treatment of latent tuberculosis. Chaisson, RE, 2000) | 1.03 |
| "Isoniazid has been shown experimentally to be a strong inhibitor of DPH metabolism." | ( Interactions of antiepileptic drugs. Kutt, H, 1975) | 0.98 |
| "Isoniazid therapy has been proved an effective means of preventing overt clinical tuberculosis in persons with positive tuberculin skin tests, persons who are close contacts of active cases, and persons with inactive tuberculosis that were never treated. " | ( The Jewish Hospital of St. Louis therapeutic grand rounds number 10. Chemoprophylaxis of tuberculosis. Avioli, LV; Byrd, R; Lefrak, SS; Senior, RM, 1975) | 1.7 |
| "Isoniazid alone has no mitogenic activity." | ( Studies on immunomodulatory properties of isoniazid. I. Effect of isoniazid on mitogen- and anti-CD3 antibody-induced proliferation of human peripheral blood mononuclear cells and T cells. Kucharz, EJ; Sierakowski, SJ, 1990) | 1.26 |
| "Isoniazid (INH) has been widely used in the preventive therapy of tuberculosis since the early 1950's. " | ( Sustained release isoniazid tablets. I--Formulation and in vitro evaluation. Bulut-Oner, F; Capan, Y; Hincal, AA; Kas, S; Oner, L, ) | 1.91 |
| "Isoniazid has been demonstrated to be active as prophylactic therapy for tuberculosis at a daily dose of 300 mg (5-10 mg/kg in children) for 6-12 months." | ( Present status of chemotherapy for tuberculosis. Grosset, JH, ) | 0.85 |
Isoniazid is a leading cause of liver injury but it is not clear how many cases are reported or how many clinicians and patients adhere to American Thoracic Society guidelines. Isoniazids inhibit MAO II, III, IV and V forms in a non competitive fashion.
Isoniazid (INH) treatment can cause serious liver injury and autoimmunity. Treatment increased serum hepatotoxicity markers (alanine and aspartate transaminase) in young animals but not in old animals.
Toxic doses of acetylisoniazid and acetylhydrazine, radiolabeled in the acetyl group, were found to bind covalently to liver protein in vivo. The rate of discontinuation of isoniazid due to adverse effects was substantially higher than reported earlier.
The study evaluated the pharmacokinetics of isoniazid (INH) associated with optimal early bactericidal activity (EBA) The influence of N-acetyltransferase-2 (NAT2) subtype on the ability of pulmonary tuberculosis (PTB) patients to reach the identified pharmacokinetic values after INH doses.
Rifampicin and isoniazid are first line combination drugs for treatment of tuberculosis. They negatively interact with each other upon simultaneous release in acidic environment. Three months of treatment with rifabutin proved to be a valid candidate for tuberculosis preventive therapy.
The development of bacterial resistance may be attributed to poor quality and reduced bioavailability of fixed-dose combination (FDC) formulations. Compared with isoniazid tablets, aconiazide's relative bioavailability (based on the area under the serum concentration-time curve) was 50.
The isoniazid dosage was never too low to inhibit sensitive organisms. The drug was either abruptly stopped or dosage lowered based only on clinical expertise, which could potentially lead to further resistance to Mycobacterium tuber.
| Role | Description |
|---|---|
| antitubercular agent | A substance that kills or slows the growth of Mycobacterium tuberculosis and is used in the treatment of tuberculosis. |
| drug allergen | Any drug which causes the onset of an allergic reaction. |
| [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 |
|---|---|
| carbohydrazide | A hydrazide consisting of hydrazine carrying one or more carboacyl groups. |
| [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 (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 1.0000 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 26.0140 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 5.0119 | 0.0072 | 15.7588 | 89.3584 | AID411 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 50.1187 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 21.1317 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
| GLS protein | Homo sapiens (human) | Potency | 31.6228 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 27.1656 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 22.3757 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743063 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 0.2282 | 0.0010 | 22.6508 | 76.6163 | AID1224838 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.0010 | 0.0013 | 10.1577 | 42.8575 | AID1259253 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 21.1508 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 29.5953 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075 |
| 67.9K protein | Vaccinia virus | Potency | 3.1623 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 89.1251 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 0.1900 | 0.0237 | 23.2282 | 63.5986 | AID743223 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 22.3872 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 10.1090 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 12.5893 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 35.4813 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 11.4367 | 0.0003 | 23.4451 | 159.6830 | AID743065 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 2.0338 | 0.0006 | 27.2152 | 1,122.0200 | AID743202 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 14.1254 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| geminin | Homo sapiens (human) | Potency | 0.7943 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 9.9150 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 9.9150 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [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) |
|---|---|---|---|---|---|---|---|
| 3-oxoacyl-[acyl-carrier-protein] synthase 3 | Escherichia coli | IC50 (µMol) | 1,000.0000 | 2.1000 | 4.2000 | 6.3000 | AID1639213 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
| Polyphenol oxidase 2 | Agaricus bisporus | IC50 (µMol) | 1,000.0000 | 0.0340 | 3.9871 | 10.0000 | AID1265266 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1,000.0000 | 0.4000 | 2.7500 | 8.6000 | AID1209456 |
| Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 567.0000 | 0.1100 | 7.1903 | 10.0000 | AID1209455; AID1443980; AID1449628; AID1473738 |
| Myeloperoxidase | Homo sapiens (human) | IC50 (µMol) | 4.8500 | 0.0200 | 1.8811 | 7.6800 | AID1337095; AID1337096 |
| Cytochrome P450 1A2 | Homo sapiens (human) | Ki | 56.0000 | 0.0056 | 1.1534 | 9.0000 | AID589218 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 36.0000 | 0.0001 | 1.4162 | 9.9000 | AID589165 |
| DNA gyrase subunit A | Escherichia coli K-12 | IC50 (µMol) | 1,000.0000 | 0.0239 | 0.5629 | 5.2300 | AID1639212 |
| DNA gyrase subunit B | Escherichia coli K-12 | IC50 (µMol) | 1,000.0000 | 0.0050 | 0.4398 | 5.2300 | AID1639212 |
| Cytochrome P450 2C8 | Homo sapiens (human) | Ki | 374.0000 | 0.0018 | 0.3873 | 3.3000 | AID589253 |
| Cytochrome P450 2A6 | Homo sapiens (human) | Ki | 60.0000 | 0.0056 | 1.5271 | 7.5000 | AID589229 |
| Macrophage migration inhibitory factor | Homo sapiens (human) | IC50 (µMol) | 400.0000 | 0.0380 | 3.0910 | 9.8000 | AID1877334 |
| Cytochrome P450 2C19 | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.8300 | 10.0000 | AID589250 |
| DNA gyrase subunit B | Mycobacterium tuberculosis H37Rv | IC50 (µMol) | 50.0000 | 0.0150 | 2.4676 | 10.0000 | AID1272956 |
| DNA gyrase subunit A | Mycobacterium tuberculosis H37Rv | IC50 (µMol) | 50.0000 | 0.0150 | 3.4773 | 10.0000 | AID1272956 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis H37Rv | IC50 (µMol) | 8.2900 | 0.0300 | 2.2864 | 10.0000 | AID1639206 |
| Putative FAD-containing monooxygenase MymA | Mycobacterium tuberculosis H37Rv | IC50 (µMol) | 4.9000 | 4.9000 | 4.9000 | 4.9000 | AID1802256 |
| Dihydrofolate reductase | Mycobacterium tuberculosis H37Rv | Ki | 0.0010 | 0.0010 | 0.0010 | 0.0010 | AID576936 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
| [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) |
|---|---|---|---|---|---|---|---|
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis H37Rv | MIC99 | 0.0700 | 0.0700 | 0.0700 | 0.0700 | AID1697972 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID746725 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.A1 cells at 1 MOI assessed as intracellular bacterial growth inhibition at 1 uM after 1 hr by luciferase reporter gene assay relative to control | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Biological evaluation of bisbenzaldehydes against four Mycobacterium species. |
| AID780897 | Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 harboring katG mutant after 7 days by REMA assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids. |
| AID509430 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic ahpC-12 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID1708494 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Click synthesis of 1,2,3-triazole based imidazoles: Antitubercular evaluation, molecular docking and HSA binding studies. |
| AID649902 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 14 days | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold. |
| AID1687474 | Antimycobacterial activity against Mycobacterium avium assessed as inhibition of microbial growth incubated for 1 week by MABA method | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents. |
| AID775554 | Antimycobacterial activity against Mycobacterium smegmatis ATCC 700084 after 3 days | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | New derivatives of salicylamides: Preparation and antimicrobial activity against various bacterial species. |
| AID1071102 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by broth microdilution assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III. |
| AID353148 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth index at 6.25 ug/mL after 4 days by radiometric method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Design, synthesis, biological evaluation and molecular modelling studies of novel quinoline derivatives against Mycobacterium tuberculosis. |
| AID721560 | Cytotoxicity against human HepG2 cells | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Synthesis and antimycobacterial evaluation of pyrazinamide derivatives with benzylamino substitution. |
| AID1593371 | Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth by microplate alamar blue assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II. |
| AID143695 | Antimycobacterial activity against Mycobacterium avium (NIHJ1605) | 2003 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17 | Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin. |
| AID520108 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv at assessed as growth inhibition at 10 mg/kg following 24 days oxygen depletion by Wayne method relative to control | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo. |
| AID1246817 | Antimycobacterial activity against Mycobacterium tuberculosis BE11677 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1602078 | Antibacterial activity against Staphylococcus aureus ATCC 6538 measured after overnight incubation | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Design, synthesis and anti-bacterial studies of piperazine derivatives against drug resistant bacteria. |
| AID718942 | Cytotoxicity against HEK293T cells assessed as cellular growth at 100 uM by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis. |
| AID1393796 | Antibacterial activity against Mycobacterium smegmatis after 7 days by two fold dilution assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Fluoroquinolone derivatives and their anti-tubercular activities. |
| AID1608991 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv 331/88 after 21 days | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds. |
| AID1224131 | Acute toxicity in mouse administered as single po dose | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis and antituberculosis activity of novel 5-styryl-4-(hetero)aryl-pyrimidines via combination of the Pd-catalyzed Suzuki cross-coupling and S(N)(H) reactions. |
| AID1247199 | Anti-tubercular activity against rifampicin, isoniazid, ethambutol and pyrazinamide-sensitive dormant phage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells by neutral red assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Design and synthesis of 11α-substituted bile acid derivatives as potential anti-tuberculosis agents. |
| AID576919 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 harboring pYUB1062 plasmid overexpressing Mycobacterium tuberculosis Rv3777 probable oxidoreductase gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID535775 | Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to RLU count by real-time luminescence method | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains. |
| AID1612597 | Antibacterial activity against Mycobacterium tuberculosis H37Rv | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents. |
| AID425189 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | A microwave-assisted facile regioselective Fischer indole synthesis and antitubercular evaluation of novel 2-aryl-3,4-dihydro-2H-thieno[3,2-b]indoles. |
| AID616940 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 2 weeks by BACTEC 460 radiometric method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues. |
| AID1292712 | Drug excretion in human subject rapid inactivator assessed as total isonicotinoyl compound level in urine at 670 mg, iv infused at constant rate 5.2min measured 296 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1400027 | Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC100 for replicating Mycobacterium tuberculosis H37Rv by MABA | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | An antimycobacterial pleuromutilin analogue effective against dormant bacilli. |
| AID1185146 | Antimicrobial activity against moxicillin resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase G88N mutant | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing. |
| AID1890848 | Selectivity index, ratio of MIC90 for antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC::PDFMtb overexpression mutant to MIC90 for antimycobacterial activity against wild type Mycobacterium smegmatis mc2 155 | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives. |
| AID356042 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by Microplate Alamar Blue Assay | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | New antimycobacterial and antimalarial 8,9-secokaurane diterpenes from Croton kongensis. |
| AID1143273 | Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis harboring DprE1 C-G mutant assessed as growth inhibition by resazurin assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
| AID1383954 | Antimycobacterial activity against MDR Mycobacterium tuberculosis isolate 591 after 15 days by MABA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID1292631 | Drug metabolism in human slow inactivators assessed as excretion of alpha-ketoglutaric acid isonicotinoylhydrazone in urine at 1 g, iv by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID669844 | Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv by microplate alamar blue assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis. |
| AID625692 | Antimycobacterial activity against Mycobacterium avium CNTC My 330/88 after 21 days | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | New series of isoniazid hydrazones linked with electron-withdrawing substituents. |
| AID326162 | Antimalarial activity against Plasmodium falciparum Dd2 expressing katG | 2007 | The Journal of biological chemistry, Aug-31, Volume: 282, Issue:35 | X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. |
| AID1852779 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth for 5 weeks by spot culture growth inhibition assay | 2022 | RSC medicinal chemistry, Nov-16, Volume: 13, Issue:11 | Synthesis, biological evaluation and computational studies of pyrazole derivatives as |
| AID780667 | Selectivity index, ratio of CC50 for African green monkey Vero C1008 cells to MIC for Mycobacterium tuberculosis H37Rv | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Rational drug design based synthesis of novel arylquinolines as anti-tuberculosis agents. |
| AID144564 | In vitro anti-mycobacterial activity against Mycobacterium smegmatis was determined | 2004 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6 | Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480. |
| AID768290 | Antibacterial activity against Enterococcus faecalis 2920 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID569256 | Antimycobacterial activity against Mycobacterium bovis BCG str. Tokyo 172 | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3 | Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives. |
| AID1635761 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv grown on serum isolated from 10 mg/kg, po treated BALB/c mouse for 30 to 120 mins assessed as reduction in bacterial growth followed by bacterial addition incubated for 7 days by alamar b | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection. |
| AID1730994 | Antitubercular activity against isoniazid/rifampin/levofloxacin/ofloxacin/kanamycin extensively drug resistance Mycobacterium tuberculosis TF274 XDR by MABA assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules. |
| AID1733369 | Antitubercular activity against isoniazid,streptomycin,rifampicin,ethambutol,para-aminosalicylate,prothionamide,capreomycin-resistant Mycobacterium tuberculosis 14862 assessed as bacterial growth inhibition | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition. |
| AID768289 | Antibacterial activity against Acinetobacter baumannii 122 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID287745 | Antimycobacterial activity against Mycobacterium avium 330/88 after 14 days | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | A new modification of anti-tubercular active molecules. |
| AID589638 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Microwave assisted one-pot synthesis of highly potent novel isoniazid analogues. |
| AID1335980 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 8 to 9 days by BacT/Alert MP bottle assay | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains. |
| AID1316914 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis. |
| AID1593375 | Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in multidrug-resistant Mycobacterium tuberculosis KZN494 assessed as reduction in bacterial growth by microplate alamar blue assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II. |
| AID551508 | Antimycobacterial activity against Mycobacterium phlei ATCC 19249 after 72 hrs by broth microtiter dilution method | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones. |
| AID1706442 | Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 27294 | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Anti-tubercular profile of new selenium-menadione conjugates against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain and multidrug-resistant clinical isolates. |
| AID1063977 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 14 days | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity. |
| AID159988 | Effect on plasma amine oxidase (0.1 uM) after 30 min of incubation at pH 7.2 | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids. |
| AID378983 | Antimicrobial activity against Mycobacterium tuberculosis H37Ra by microplate alamar blue assay | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | 2-substituted furans from the roots of Polyalthia evecta. |
| AID1191496 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 7 days by microdilution method | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Synthesis and in vitro biological evaluation of 2-(phenylcarbamoyl)phenyl 4-substituted benzoates. |
| AID1403701 | Inhibition of recombinant N-terminal His-tagged Bacillus subtilis subsp. subtilis 168 glutamate racemase expressed in Escherichia coli BL21(DE3) using D-Glutamate as substrate in presence of NADH by spectrophotometric based GDH enzyme coupled assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors. |
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| AID1381960 | Genotoxicity in Salmonella typhimurium TA100 assessed as increase in revertant colonies at 0.5 uM preincubated for 20 mins followed by addition of top agar and minimal agar and measured after 72 hrs in presence of S9 metabolic activation system by Ames te | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
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| AID683316 | Antibacterial activity against Enterococcus faecalis ATCC 29212 by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776. |
| AID1609014 | Cytostatic activity against human HepG2 cells preincubated for overnight in serum free medium followed by compound wash out and further incubated for 72 hrs in presence of serum by MTT assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds. |
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| AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
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| AID649901 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 7 days | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold. |
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| AID619394 | Cytotoxicity against human PBMC measured after overnight incubation by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | New fluorine-containing hydrazones active against MDR-tuberculosis. |
| AID1137532 | Antitubercular activity against 1-ethyl-3-(6-(pyrimidin-5-yl)-5-((tetrahydrofuran-3-yl)methoxy)thiazolo[5,4-b]pyridin-2-yl)urea-resistant Mycobacterium tuberculosis H37Rv clone 8.2 harboring DNA gyraseB ATP domain Ala92Ser mutant assessed as growth inhibi | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B. |
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| AID1730952 | Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Structure based design, synthesis, and biological evaluation of imidazole derivatives targeting dihydropteroate synthase enzyme. |
| AID1381951 | Genotoxicity in Salmonella typhimurium TA100 assessed as increase in revertant colonies at 0.5 uM preincubated for 20 mins followed by addition of top agar and minimal agar and measured after 72 hrs in absence of S9 metabolic activation system by Ames tes | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
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| AID326163 | Antimalarial activity against Plasmodium falciparum Dd2 | 2007 | The Journal of biological chemistry, Aug-31, Volume: 282, Issue:35 | X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. |
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| AID1891913 | Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy. |
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| AID528963 | Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 300 mg/kg, po once daily measured on day 8 after starting standard TB therapy | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8 | Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. |
| AID1458323 | Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by spectrophotometric analysis | 2017 | Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16 | Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery. |
| AID671455 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth at 1 ug/ml by radiometric-BACTEC assay | 2012 | Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13 | Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors. |
| AID689772 | Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 10 days in anaerobic condition followed by 48 hrs incubation in aerobic condition by LORA assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis. |
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| AID495236 | Antimicrobial activity against Mycobacterium tuberculosis NJT210GAC harboring embB406 GGC-GAC(Gly-Asp) mutation in embB gene after 4 weeks | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 | Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis. |
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| AID1825030 | Antitubercular activity against Mycobacterium smegmatis mc2155 ATCC 700084 cultured in GAST-Fe media incubated for 24 hrs by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition. |
| AID1400026 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | An antimycobacterial pleuromutilin analogue effective against dormant bacilli. |
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| AID1076821 | Antitubercular activity against extensive drug-resistant Mycobacterium tuberculosis clinical isolate 4 assessed as growth inhibition by microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents. |
| AID1055746 | Antimycobacterial activity against Mycobacterium smegmatis MC2 155 ATCC 14468 after 32 hrs by turbidimetry | 2013 | European journal of medicinal chemistry, , Volume: 70 | Design, diversity-oriented synthesis and structure activity relationship studies of quinolinyl heterocycles as antimycobacterial agents. |
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| AID1178731 | Antimicrobial activity against Candida albicans after 48 hrs by agar dilution method | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis of novel 4-nitropyrrole-based semicarbazide and thiosemicarbazide hybrids with antimicrobial and anti-tubercular activity. |
| AID1292660 | Drug excretion in human subject slow inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 681 mg, iv infused at constant rate 5.4 min measured 648 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID576935 | Ratio of MIC for Mycobacterium tuberculosis H37RV harboring pMV261::InhA plasmid to MIC for wild-type Mycobacterium tuberculosis H37Rv | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
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| AID465566 | Cytotoxicity against african green monkey Vero C1008 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Novel molecular hybrids of cinnamic acids and guanylhydrazones as potential antitubercular agents. |
| AID145300 | In vitro anti-mycobacterial activity against Mycobacterium tuberculosis ATCC 27294 was determined | 2004 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6 | Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480. |
| AID1576559 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in media containing 7H9/DPPC/casitone/Tyloxapol assessed as reduction in bacterial growth incubated for 14 days by Alamar blue reagent based assay | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Dual-target inhibitors of mycobacterial aminoacyl-tRNA synthetases among |
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| AID1853081 | Bactericidal activity against Mycobacterium bovis BCG ATCC 35734 assessed as reduction on colony forming unit at 15 uM measured upto 14 days by time killing assay | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12 | Alkyltriphenylphosphonium turns naphthoquinoneimidazoles into potent membrane depolarizers against |
| AID644320 | Antitubercular activity against Multidrug-resistant Mycobacterium tuberculosis after 7 days by resazurin assay | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents. |
| AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
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| AID1244178 | Cytotoxicity against African green monkey Vero cells after 72 hrs by CCK8 assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents. |
| AID725968 | Cytotoxicity against HEK293T cells assessed as growth inhibition at 25 uM by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Discovery of novel inhibitors targeting the Mycobacterium tuberculosis O-acetylserine sulfhydrylase (CysK1) using virtual high-throughput screening. |
| AID1381938 | Cytotoxicity against mouse J774A.1 cells assessed as decrease in cell viability at 10 nM after 20 hrs by resazurin dye-based fluorimetric method | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
| AID433906 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra after 5 days by microplate alamar blue assay | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Synthesis and antitubercular screening of imidazole derivatives. |
| AID683321 | Antibacterial activity against drug-resistant Mycobacterium tuberculosis 926 by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776. |
| AID1510690 | Acute toxicity in ICR mouse assessed as animal survival at 500 mg/kg, po administered as single dose measured for 7 days | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents. |
| AID1155865 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 to 8 days by BACTEC 12B method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis, antibacterial and antitubercular activities of benzimidazole bearing substituted 2-pyridone motifs. |
| AID1406779 | Antitubercular activity against Mycobacterium tuberculosis H37Rv after 1 week by microplate alamar blue assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents. |
| AID362955 | Antimycobacterial activity against Mycobacterium smegmatis MC2 by agar dilution method | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Discovery of antimycobacterial spiro-piperidin-4-ones: an atom economic, stereoselective synthesis, and biological intervention. |
| AID1225688 | Cytotoxicity against human A549 assessed as inhibition of cell proliferation by MTT assay | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Discovery of target based novel pyrrolyl phenoxy derivatives as antimycobacterial agents: an in silico approach. |
| AID1292673 | Drug excretion in human subject slow inactivator assessed as total isonicotinoyl compound level in urine at 681 mg, iv infused at constant rate 5.4 min measured 305 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1289083 | Clearance in healthy Chinese subject (8 subjects) with heterozygous mutant of NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID287815 | Antimicrobial activity against Mycobacterium kansasii My 235/80 after 21 days | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities. |
| AID1901706 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as reduction in log10 CFU in lungs at 25 mg/kg, po administered 5 times a week from day 10 to 30 | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis. |
| AID1309354 | Antimycobacterial activity against Mycobacterium avium after 24 hrs by microbroth dilution method | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines. |
| AID1411652 | Antimycobacterial activity against Mycobacterium tuberculosis | 2017 | MedChemComm, Nov-01, Volume: 8, Issue:11 | The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents. |
| AID535773 | Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K carrying the luxAB gene under the hsp60 promoter agar dilution method | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains. |
| AID1061104 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv by low oxygen recovery assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | A novel indigoid anti-tuberculosis agent. |
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| AID1202228 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by broth microdilution method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Development of selective DprE1 inhibitors: Design, synthesis, crystal structure and antitubercular activity of benzothiazolylpyrimidine-5-carboxamides. |
| AID1596876 | Antibacterial activity against Acinetobacter baumannii BAA1605 incubated for 16 to 18 hrs by broth microdilution assay | |||
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| AID1418313 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by rapid direct susceptibility test | |||
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| AID144887 | Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium tuberculosis | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity. |
| AID1705577 | Antimycobacterial activity against INH-resistant Mycobacterium tuberculosis mc2497 after 10 to 14 days | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and evaluation of thiophene based small molecules as potent inhibitors of Mycobacterium tuberculosis. |
| AID1261247 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate Alamar Blue assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis, antimycobacterial and antibacterial activity of fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety. |
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1437028 | Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition at 50 uM after 72 hrs by MTT assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis. |
| AID265985 | Activity against Mycobacterium tuberculosis H37Rv infected in CD1 mouse assessed as decrease in bacterial load relative to control in lung at 25 mg/kg, ip | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Discovery of new antitubercular oxazolyl thiosemicarbazones. |
| AID1437025 | Inhibition of Mycobacterium tuberculosis His6-tagged InhA expressed in Escherichia coli BL21 (DE3) assessed as decrease in NADH oxidation to NAD+ using 2-trans-decenoyl-CoA as substrate preincubated for 2 hrs followed by substrate and NADH addition measur | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis. |
| AID1299850 | Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis RS-032 clinical isolate harboring katG S315T mutant assessed as reduction in bacterial growth after 7 days by resazurin assay | 2016 | ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3 | 2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains. |
| AID1181078 | Antibacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate Alamar Blue assay | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | NRPS substrate promiscuity leads to more potent antitubercular sansanmycin analogues. |
| AID325128 | Antimicrobial activity against Mycobacterium tuberculosis TB19 isolate at 0.1 ug/ml after 1 week | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1692253 | Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16995 clinical isolate assessed as inhibition of bacterial growth incubated for 7 days by MABA assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Identification of benzothiazinones containing 2-benzyl-2,7-diazaspiro[3.5]nonane moieties as new antitubercular agents. |
| AID729922 | Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 24 hrs by MTS assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents. |
| AID316447 | Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 by agar dilution method | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation. |
| AID1299849 | Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth after 7 days by resazurin assay | 2016 | ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3 | 2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains. |
| AID1444302 | Antimycobacterial activity against Mycobacterium kansasii isolate 6509/96 after 14 days by micromethod | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Structure-activity relationship studies on 3,5-dinitrophenyl tetrazoles as antitubercular agents. |
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
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| AID1514453 | Antitubercular activity against moxifloxacin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety. |
| AID310489 | Solubility at pH 6.0 by shake-flask method | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Discovery of novel isoxazolines as anti-tuberculosis agents. |
| AID1247200 | Anti-tubercular activity against rifampicin, isoniazid, ethambutol and pyrazinamide-sensitive active phage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells by neutral red assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Design and synthesis of 11α-substituted bile acid derivatives as potential anti-tuberculosis agents. |
| AID464245 | Antituberculosis activity against Mycobacterium tuberculosis H37Ra after 4 days by Alamar blue assay | 2010 | Journal of natural products, Jan, Volume: 73, Issue:1 | Oblongolides from the endophytic fungus Phomopsis sp. BCC 9789. |
| AID1348985 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 days by rapid direct susceptibility test | |||
| AID1577319 | Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 14 days | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase. |
| AID613874 | Antimycobacterial activity against 6-weeks nutrient starved phase cultures of Mycobacterium tuberculosis H37Rv treated for 7 days measured after 4 weeks by agar dilution method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Synthesis of various 3-nitropropionamides as Mycobacterium tuberculosis isocitrate lyase inhibitor. |
| AID534422 | Antibacterial activity against Mycobacterium bovis BCG-japan | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics. |
| AID1767888 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 7 days by MABA assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis. |
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| AID1064521 | Lipophilicity, log K of the compound by HPLC analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Alkylamino derivatives of pyrazinamide: synthesis and antimycobacterial evaluation. |
| AID333960 | Antimycobacterial activity against Mycobacterium tuberculosis at 20 ug/disk by disk diffusion assay | 1997 | Journal of natural products, Nov, Volume: 60, Issue:11 | Antimycobacterial polyynes of Devil's Club (Oplopanax horridus), a North American native medicinal plant. |
| AID363986 | Antimycobacterial activity against Mycobacterium smegmatis mc2 155 after 48 hrs by microdilution resazurin assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial. |
| AID1265274 | Inhibition of tyrosinase in mouse B16F10 cell lysates using DOPA as substrate relative to control | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase. |
| AID1399839 | Antibacterial activity against Mycobacterium smegmatis ATCC 19420 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase. |
| AID353152 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth index at 6.25 ug/mL after 8 days by radiometric method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Design, synthesis, biological evaluation and molecular modelling studies of novel quinoline derivatives against Mycobacterium tuberculosis. |
| AID1373655 | Antimycobacterial activity against Mycobacterium bovis BCG | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis. |
| AID1575584 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in human THP-1 cells assessed as reduction in microbial growth after 4 days by ten-fold serial dilution method | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | 3D QSAR-based design and liquid phase combinatorial synthesis of 1,2-disubstituted benzimidazole-5-carboxylic acid and 3-substituted-5 |
| AID1053481 | Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA M103I mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis. |
| AID1596895 | Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 18 hrs by broth microdilution assay | |||
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| AID1759473 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate alamar blue assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis. |
| AID1296084 | Antimycobacterial activity against Mycobacterium tuberculosis mc'2-7000x assessed as inhibition of mycobacterial growth at 500 ug/ml | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul |
| AID309277 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by Agar dilution method | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Design, synthesis and antitubercular activity of diarylmethylnaphthol derivatives. |
| AID311487 | Antituberculosis activity against Mycobacterium tuberculosis H37Ra by microplate alamar blue assay | 2007 | Journal of natural products, Sep, Volume: 70, Issue:9 | Bioactive constituents of the roots of Polyalthia cerasoides. |
| AID1132600 | Antitubercular against Mycobacterium tuberculosis H37Rv infected in mouse assessed as host survival at 2.5 mg/kg/day administered with food for 19 days measured on day 30 | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | Antitubercular 2,8-bis(alkylaminomethyl)phenazines. |
| AID1524921 | Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 transformed with pSMT1 luciferase reporter plasmid reduction in bacterial multiplication incubated for 7 days by luminometric assay | 2019 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10 | Double prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID1287502 | Antitubercular activity against active state Mycobacterium bovis BCG ATCC 35734 assessed as viable cells after 8 days by nitrate reductase assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents. |
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| AID287811 | Antimicrobial activity against Mycobacterium avium My 330/88 after 14 days | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities. |
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| AID774992 | Cytotoxicity against human GM637 cells after 4 days by WST-1 assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Synthesis and evaluation of α-ketotriazoles and α,β-diketotriazoles as inhibitors of Mycobacterium tuberculosis. |
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| AID294760 | Antibacterial activity against Mycobacterium avium 724S after 2 weeks by broth dilution method | 2007 | Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9 | Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus. |
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| AID589229 | Mechanism based inhibition of human cytochrome P450 2A6 measured by coumarin 7-hydroxylation | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
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| AID1917330 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured by microplate alamar blue assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors. |
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| AID1593909 | Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay | |||
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| AID419344 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 weeks | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis, antitubercular activity and docking study of novel cyclic azole substituted diphenyl ether derivatives. |
| AID474485 | Lipophilicity, log D of the compound | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Radiosynthesis and bioimaging of the tuberculosis chemotherapeutics isoniazid, rifampicin and pyrazinamide in baboons. |
| AID1458328 | Cytotoxicity against human MDM cells assessed as reduction in cell viability after 3 days by AlamarBlue assay | 2017 | Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16 | Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery. |
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| AID1332964 | Cytotoxicity against human MRC5 cells measured after 24 hrs by resazurin based fluorescence method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis. |
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| AID1668222 | Inhibition of Electrophorus electricus AChE at 100 uM using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 10 mins by Ellman's method (Rvb = 7 +/- 7.1%) | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10 | Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation. |
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| AID1570246 | Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 2 incubated for 7 days by rapid direct susceptibility test | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. |
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| AID634040 | Antituberculosis activity against multidrug-resistant Mycobacterium tuberculosis isolate Spec. 192 by twofold serial dilution method | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis of novel 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds and their evaluation for tuberculostatic activity. |
| AID1335982 | Antibacterial activity against rifampin-resistant Mycobacterium tuberculosis after 8 to 9 days by BacT/Alert MP bottle assay | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains. |
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| AID1152777 | Antimycobacterial activity against 5-(((3S,4R)-3-Fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA D89N mutant | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis. |
| AID1326672 | Growth inhibition of mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors. |
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| AID467612 | Fraction unbound in human plasma | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
| AID594923 | Antibacterial activity against Mycobacterium vanbaalenii assessed as growth inhibition at 30 uM after 72 hrs by microplate reader | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Identification of novel potential antibiotics for tuberculosis by in silico structure-based drug screening. |
| AID1296380 | Antimycobacterial activity against Mycobacterium kansasii CNCTC My 6509/96 after 21 days by microdilution method | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis. |
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| AID1224129 | Antimycobacterial activity against Mycobacterium terrae after 10 days by microbroth dilution method | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis and antituberculosis activity of novel 5-styryl-4-(hetero)aryl-pyrimidines via combination of the Pd-catalyzed Suzuki cross-coupling and S(N)(H) reactions. |
| AID717690 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | A regio- and stereoselective 1,3-dipolar cycloaddition for the synthesis of new-fangled dispiropyrrolothiazoles as antimycobacterial agents. |
| AID392605 | Antimycobacterial activity against Mycobacterium kansasii MTCC 3058 by agar dilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | 5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species. |
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| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID408873 | Protection index, ratio of MNTD50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis 103471 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
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| AID515919 | Antibacterial activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID694365 | Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis MS-115 under anaerobic condition assessed as growth inhibition at 0.1 ug/ml by BACTEC method | 2012 | Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22 | The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives. |
| AID493953 | Antimicrobial activity aagainst Mycobacterium sp. Mc2 in log phase assessed as inhibition of growth | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | 5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures. |
| AID1323722 | Growth inhibition of Mycobacterium tuberculosis H37Ra at 1 ug/ml after 6 days by microplate alamar blue assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID1360819 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by Two-fold serial dilution assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Benzo[d]thiazole-2-carbanilides as new anti-TB chemotypes: Design, synthesis, biological evaluation, and structure-activity relationship. |
| AID297113 | Antibacterial activity against Mycobacterium bovis BCG Tokyo after 18 hrs by agar plate dilution method | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17 | Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens. |
| AID287747 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 14 days | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | A new modification of anti-tubercular active molecules. |
| AID1412768 | Antimycobacterial activity against Mycobacterium avium subsp. avium Chester ATCC 15769 incubated in dark for 5 days by Alamar Blue assay | 2018 | MedChemComm, Apr-01, Volume: 9, Issue:4 | Design, synthesis and antimycobacterial activity of hybrid molecules combining pyrazinamide with a 4-phenylthiazol-2-amine scaffold. |
| AID1435650 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 131 after 14 days by micromethod | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents. |
| AID1890844 | Antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC::PDFMtb overexpression mutant assessed as inhibition of mycobacterial growth incubated for 3 to 5 days by resazurin microtiter assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives. |
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| AID1484377 | Antimycobacterial activity against Mycobacterium tuberculosis infected in C57BL/6 mouse assessed as colony forming units per lung at 25 mg/kg administered via gavage for 2 days measured last post dose (Rvb = 6.53 +/- 0.16 log10CFU) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Isoniazid derivatives and their anti-tubercular activity. |
| AID576915 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 harboring pYUB1062 plasmid overexpressing Mycobacterium tuberculosis Rv0091 Mtn/Sah gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
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| AID1601486 | Antimycobacterial activity against Mycobacterium bovis assessed as 90 percent growth inhibition measured after 120 hrs by turbidometric analysis | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 | Synthesis and evaluation of a novel quinoline-triazole analogs for antitubercular properties via molecular hybridization approach. |
| AID1536935 | Protective index, ratio of MNTD50 for HEK293T cells to MIC for Mycobacterium tuberculosis H37Rv | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4 | Synthesis and evaluation of novel substituted 1,2,3-triazolyldihydroquinolines as promising antitubercular agents. |
| AID1491512 | Genotoxicity in Salmonella typhimurium TA104 harboring Pr1 lux operon fusion at 1.28 to 128 uM measured every 5 mins for 4 hrs in presence of S9 liver fraction by vitotox assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones. |
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| AID1272956 | Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors. |
| AID325135 | Antimicrobial activity against Mycobacterium tuberculosis TB19 isolate at 0.4 ug/ml after 4 weeks | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID768296 | Antibacterial activity against Escherichia coli 1777 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID461171 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate Alamar blue assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. |
| AID352248 | Antimycobacterial activity against Mycobacterium tuberculosis CNCTC My 331/88 after 21 days | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10 | New antituberculotics originated from salicylanilides with promising in vitro activity against atypical mycobacterial strains. |
| AID580321 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by tetrazolium microplate assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents. |
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| AID1337095 | Inhibition of human MPO | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | From Dynamic Combinatorial Chemistry to |
| AID1536933 | Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 1 week by microplate alamar blue assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4 | Synthesis and evaluation of novel substituted 1,2,3-triazolyldihydroquinolines as promising antitubercular agents. |
| AID1614907 | Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 16995 after 7 days by microplate alamar blue assay | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties. |
| AID392601 | Antimycobacterial activity against Mycobacterium microti MTCC 1727 by agar dilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | 5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species. |
| AID1614909 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties. |
| AID721562 | Antimycobacterial activity against Mycobacterium avium CNCTC My 152/73 after 10 to 14 days by microdilution panel method | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Synthesis and antimycobacterial evaluation of pyrazinamide derivatives with benzylamino substitution. |
| AID445334 | Selectivity for Mycobacterium tuberculosis H37Rv over human MRC5 cells | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis. |
| AID669186 | Antitubercular activity against Mycobacterium tuberculosis H37Rv in aerobic conditions after 7 days by microplate-based alamar blue assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
| AID1476364 | Antitubercular activity against streptomycin resistant Mycobacterium tuberculosis H37Rv ATCC 35820 after 24 hrs by MABA method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity. |
| AID458158 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 14 days by micromethod | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains. |
| AID576927 | Antimicrobial activity against Mycobacterium smegmatis MC2 5071 overexpressing InhA gene assessed as growth inhibition at 120 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID634615 | Antimycobacterial activity against Mycobacterium tuberculosis TN3183 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID634621 | Antimycobacterial activity against Mycobacterium tuberculosis W4 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1292656 | Drug excretion in human subject slow inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 681 mg, iv infused at constant rate 5.4 min measured 524 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID721635 | Growth inhibition of Mycobacterium smegmatis at 100 uM after 24 hrs | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Identification of novel antimycobacterial chemical agents through the in silico multi-conformational structure-based drug screening of a large-scale chemical library. |
| AID316438 | Antimicrobial activity against Mycobacterium tuberculosis ATCC 2729411 by Almar blue assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Synthesis and antimycobacterial evaluation of new trans-cinnamic acid hydrazide derivatives. |
| AID532960 | Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 4 | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates. |
| AID1338197 | Antimycobacterial activity against GFP-fused Mycobacterium tuberculosis H37Rv in liquid broth culture medium | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and structure-activity studies of side chain analogues of the anti-tubercular agent, Q203. |
| AID1564635 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial cell growth incubated for 7 days by microplate alamar blue assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents. |
| AID649900 | Antimycobacterial activity against Mycobacterium kansasii 235/80 after 21 days | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold. |
| AID1411651 | Antimycobacterial activity against Mycobacterium smegmatis | 2017 | MedChemComm, Nov-01, Volume: 8, Issue:11 | The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents. |
| AID290254 | Cytotoxicity against Vero cells after 72 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7 | N-Hydroxythiosemicarbazones: synthesis and in vitro antitubercular activity. |
| AID408345 | Antibacterial activity against Bacillus subtilis ATCC 6633 after 36 hrs visualized by MTT staining by broth macrodilution assay | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis of methyl 5-S-alkyl-5-thio-D-arabinofuranosides and evaluation of their antimycobacterial activity. |
| AID430084 | Antitubercular activity against Mycobacterium tuberculosis isolate UC0802 by microplate alamar blue assay | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies. |
| AID1178141 | Selectivity index, ratio of I50 for mouse J774A1 cells to GI50 for Mycobacterium tuberculosis H37Rv | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 2,4-Dialkyl-8,9,10,11-tetrahydrobenzo[g]pyrimido[4,5-c]isoquinoline-1,3,7,12(2H,4H)-tetraones as new leads against Mycobacterium tuberculosis. |
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| AID1577324 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 7 days | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase. |
| AID440894 | Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis by agar dilution method | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | L-proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines. |
| AID1225686 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth after 5 days by Microplate Alamar Blue Assay | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Discovery of target based novel pyrrolyl phenoxy derivatives as antimycobacterial agents: an in silico approach. |
| AID446149 | Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development. |
| AID1703171 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in microbial growth under GAST/Fe medium after 1 week by two fold serial dilution method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and structure activity relationships of cyanopyridone based anti-tuberculosis agents. |
| AID445333 | Selectivity for Mycobacterium tuberculosis H37Rv over human A549 cells | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis. |
| AID1244382 | Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 after 7 days by serial dilution method | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Combating highly resistant emerging pathogen Mycobacterium abscessus and Mycobacterium tuberculosis with novel salicylanilide esters and carbamates. |
| AID545248 | Antimycobacterial activity against extensively drug resistant Mycobacterium tuberculosis Praha 131 after 14 days by micromethod | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | New amino acid esters of salicylanilides active against MDR-TB and other microbes. |
| AID1154544 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 C387S mutant assessed as growth inhibition after 5 days by microdilution method | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Lead optimization of 1,4-azaindoles as antimycobacterial agents. |
| AID1418316 | Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv | |||
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| AID1163983 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by MABA method | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety. |
| AID620091 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by resazurin assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties. |
| AID1861191 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as mycobacterial growth inhibition | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent. |
| AID1708493 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 28 days by agar dilution method | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Click synthesis of 1,2,3-triazole based imidazoles: Antitubercular evaluation, molecular docking and HSA binding studies. |
| AID1292706 | Drug excretion in human subject rapid inactivator assessed as total isonicotinoyl compound level in urine at 670 mg, iv infused at constant rate 5.2min measured 94 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
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| AID509437 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic katG295 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| 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). |
| AID310488 | Antituberculosis activity against Mycobacterium tuberculosis by microbroth dilution method | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Discovery of novel isoxazolines as anti-tuberculosis agents. |
| AID1624150 | Antitubercular activity against isoniazid/ethionamide resistant Mycobacterium tuberculosis isolate 2 after 7 days | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis. |
| AID1289113 | Antitubercular activity against Mycobacterium tuberculosis in tuberculosis patient assessed as compound level in serum required to cause 90% maximum early bactericidal activity at 0.2 to 12 mg/kg after 2 hrs | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1759474 | Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16995 clinical isolate incubated for 7 days by microplate alamar blue assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis. |
| AID1163985 | Antimycobacterial activity against isoniazid and rifampicin resistant Mycobacterium tuberculosis 11277 by MABA method | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety. |
| AID619393 | Cytotoxicity against human HepG2 cells measured after overnight incubation by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | New fluorine-containing hydrazones active against MDR-tuberculosis. |
| AID1426439 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis CF104 clinical isolate incubated for 7 days measured 24 hrs post incubation by resazurin microtiter assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis. |
| AID392599 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | 5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species. |
| AID730805 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 0.2 ug/ml | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | An efficient domino reaction in ionic liquid: synthesis and biological evaluation of some pyrano- and thiopyrano-fused heterocycles. |
| AID364836 | Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as zone of inhibition diameter at 1 mg/mL after 24 hrs by Kirby-Bauer disk diffusion assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | Synthesis of triazole-oxazolidinones via a one-pot reaction and evaluation of their antimicrobial activity. |
| AID546032 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in swiss mouse assessed as increase mouse survival at 25 mg/kg, po qd for 28 days measured on day 30 relative to control | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and optimization of antitubercular activities in a series of 4-(aryloxy)phenyl cyclopropyl methanols. |
| AID1339434 | Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis 242/2015 after 21 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Novel salicylanilides from 4,5-dihalogenated salicylic acids: Synthesis, antimicrobial activity and cytotoxicity. |
| AID1204849 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as parasite growth inhibition after 7 days by broth microdilution assay | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID1204022 | Cytotoxicity against PBMC (unknown origin) assessed as reduction in cell viability after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2,3-triazolylbenzohydrazides. |
| AID256831 | Viable number of Mycobacterium tuberculosis colonies in lungs of infected mice after 9 days of administration of 300 mg/kg | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | Synthesis and evaluation of cyclic secondary amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents. |
| AID571682 | Clearance in BALB/c mouse at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice. |
| AID653499 | Antimycobacterial activity against Mycobacterium tuberculosis | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Growth inhibition of Mycobacterium smegmatis by prodrugs of deoxyxylulose phosphate reducto-isomerase inhibitors, promising anti-mycobacterial agents. |
| AID1847064 | Inhibition of recombinant Mycobacterium tuberculosis MurE expressed in Pseudomonas putida KT2442 using UDPMurNAc-L-Ala-D-Glu as substrate incubated for 30 mins by HPLC analysis | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | The Mur Enzymes Chink in the Armour of Mycobacterium tuberculosis cell wall. |
| AID484736 | Antimycobacterial activity against Mycobacterium smegmatis under dormancy-inducing hypoxic condition | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Trichoderins, novel aminolipopeptides from a marine sponge-derived Trichoderma sp., are active against dormant mycobacteria. |
| AID1367136 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 21 days by micromethod | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Synthesis and biological evolution of hydrazones derived from 4-(trifluoromethyl)benzohydrazide. |
| AID289149 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis CIBIN 650 isolates | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines. |
| AID370069 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID394146 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids. |
| AID1871137 | Antitubercular activity against Multidrug-resistant Mycobacterium tuberculosis clinical isolate PT20 assessed as bacterial growth inhibition incubated for 7 days by resazurin dye based assay | 2022 | ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8 | Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties. |
| AID1427179 | Antimycobacterial activity against Mycobacterium avium 330/88 measured after 21 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Antimicrobial activity of rhodanine-3-acetic acid derivatives. |
| AID345804 | Cytotoxicity against HEK293 cells after 72 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24 | Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives. |
| AID625695 | Antimycobacterial activity against Mycobacterium kansasii CNTC My 335/80 after 21 days | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | New series of isoniazid hydrazones linked with electron-withdrawing substituents. |
| AID1888139 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD5 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains. |
| AID725971 | Inhibition of Mycobacterium tuberculosis CysK1 using O-acetyl-L-serine as substrate assessed as L-cycteine formation at 100 uM after 5 mins by spectrophotometric analysis relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Discovery of novel inhibitors targeting the Mycobacterium tuberculosis O-acetylserine sulfhydrylase (CysK1) using virtual high-throughput screening. |
| AID117754 | Antitubercular activity (12.5 mg/kg) in the 31-day murine mice model | 1981 | Journal of medicinal chemistry, Nov, Volume: 24, Issue:11 | Synthesis and antibacterial activity of 1-(arylamino)-1H-pyrroles and 4-(1H-pyrrol-1-ylimino)-2,5-cyclohexadienes. |
| AID353147 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth index at 6.25 ug/mL after 3 days by radiometric method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Design, synthesis, biological evaluation and molecular modelling studies of novel quinoline derivatives against Mycobacterium tuberculosis. |
| AID1057527 | Antimycobacterial activity in Mycobacterium tuberculosis H37Rv after 5 days by Alamar Blue assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Design, synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents. |
| AID1597869 | Selectivity index, ratio of IC50 for mouse J774.A1 cells to MIC for Mycobacterium tuberculosis INH R1 ATCC 35822 | |||
| AID1877334 | Inhibition of MIF tautomerase (unknown origin) using 4-HPP as substrate preincubated for 1 hr followed by substrate addition | 2022 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 55 | Repurposing old drugs as novel inhibitors of human MIF from structural and functional analysis. |
| AID1664592 | Antitubercular activity against Mycobacterium tuberculosis H37Ra assessed as bacterial growth inhibition at 1 ug/ml by MABA relative to control | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16 | The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives. |
| AID325124 | Antimicrobial activity against Mycobacterium tuberculosis TB7 isolate at 0.4 ug/ml after 1 week | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID362953 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Discovery of antimycobacterial spiro-piperidin-4-ones: an atom economic, stereoselective synthesis, and biological intervention. |
| AID1476350 | Antitubercular activity against isoniazid resistant Mycobacterium tuberculosis H37Rv ATCC 35822 after 24 hrs by MABA method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity. |
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| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
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| AID292298 | Antibacterial activity Enterococcus faecalis ATCC 29212 after 16 to 20 hrs by broth microdilution method | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs. |
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| AID1639211 | Cytotoxicity against HEK293 cells after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery and development of novel rhodanine derivatives targeting enoyl-acyl carrier protein reductase. |
| AID1888135 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD1 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains. |
| AID292296 | Antibacterial activity Streptococcus pyogenes ATCC 19615 after 16 to 20 hrs by broth microdilution method | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs. |
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| AID1244177 | Antitubercular activity against Mycobacterium tuberculosis H37Ra after 7 days by microplate alamar blue assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents. |
| AID1488560 | Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis 09710 by two fold dilution method | |||
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| AID1668220 | Inhibition of rat bone marrow myeloperoxidase using H2O2 as substrate at 10 uM after 20 mins by TMB based method (Rvb = - 1.4 +/- 12.7%) | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10 | Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation. |
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| AID1232407 | Cytotoxicity against mouse RAW264.7 cells | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides. |
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| AID145144 | In vitro minimum inhibitory concentration against Mycobacterium tuberculosis CIP 103471 was determined | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12 | N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480. |
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| AID768276 | Induction of apoptosis in human HCT8 cells assessed as viable cells at 50 ug/mL after 24 hrs by Annexin V-FITC and propidium iodide staining-based flow cytometric analysis (Rvb = 87.7%) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
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| 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. |
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| AID571680 | Volume of distribution in BALB/c mouse at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice. |
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| AID183970 | Brain mitochondrial activity measured at 120 min of incubation at 10 uM concentration | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids. |
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| AID529534 | Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. |
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| AID1854287 | Antitubercular activity against clinical isolate rifampicin-resistant Mycobacterium tuberculosis ATCC 35838 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant |
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| AID572890 | Antibacterial activity against Mycobacterium tuberculosis Erdman infected in gamma interferon gene knockout C57BL/6 mouse assessed as bacterial load in spleen at 25 mg/kg, po administered 18 days postinfection for 9 days measured on day 24 (Rvb= 6.57+/-0. | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
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| AID1289080 | Apparent half life in healthy Chinese subject (8 subjects) with heterozygous mutant of NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
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| AID657976 | Cmax in Wistar rat at 50 mg/kg, po administered as single dose | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Synthesis of highly potent novel anti-tubercular isoniazid analogues with preliminary pharmacokinetic evaluation. |
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| AID1236139 | Cytotoxicity against human THP1 cells assessed as cell growth inhibition after 48 hrs by resazurin dye reduction method | 2015 | Journal of natural products, Aug-28, Volume: 78, Issue:8 | Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity. |
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| AID574808 | Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 horboring rpoB S531L, katG R463L/E217G, gyrA D94N/S95T, rrs A1401G by CLSI method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India. |
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| AID548358 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | A regio- and stereoselective 1,3-dipolar cycloaddition for the synthesis of novel spiro-pyrrolothiazolyloxindoles and their antitubercular evaluation. |
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| AID774298 | Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis ATCC 35838 | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
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| AID719007 | Cytotoxicity against HEK293T cells assessed as cellular growth at 25 uM by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis. |
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| AID1612598 | Antibacterial activity against Mycobacterium tuberculosis H37Rv by resazurin dye-based assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
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| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
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| AID1832326 | Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis ATCC 35838 harboring RpoBS531L mutant assessed as bacterial growth inhibition measured after 5 days by serial dilution method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Novel C-3-(N-alkyl-aryl)-aminomethyl rifamycin SV derivatives exhibit activity against rifampicin-resistant Mycobacterium tuberculosis RpoB |
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| AID1265271 | Inhibition of tyrosinase in mouse B16F10 cells assessed as reduction of melanin production at 10 uM relative to control | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase. |
| AID753835 | Antimicrobial activity against Bacille Calmette-Guerin | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | 3-Anhydro-6-hydroxy-ophiobolin A, a new sesterterpene inhibiting the growth of methicillin-resistant Staphylococcus aureus and inducing the cell death by apoptosis on K562, from the phytopathogenic fungus Bipolaris oryzae. |
| AID1411650 | Selectivity ratio of MIC for Mycobacterium smegmatis to MIC for Mycobacterium tuberculosis | 2017 | MedChemComm, Nov-01, Volume: 8, Issue:11 | The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents. |
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| AID1418315 | Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay | |||
| AID1154353 | Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis clone 4.1 over expressing DprE1 mutant after 5 days by standard microdilution method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | 4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity. |
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| AID325113 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 0.4 ug/ml after 2 weeks by BACTED460 method | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1556639 | Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16995 clinical isolate assessed as reduction in bacterial cell viability incubated for 7 days by microplate alamar blue assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | hERG optimizations of IMB1603, discovery of alternative benzothiazinones as new antitubercular agents. |
| AID458166 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate Praha 1 after 14 days by micromethod | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains. |
| AID445289 | Antibacterial activity against Staphylococcus aureus by broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis. |
| AID1386453 | Antibacterial activity against Mycobacterium bovis BCG Pasteur infected in mouse J774A.1 cells assessed as reduction in bacterial burden at 0.1 ug/ml after 72 hrs post infection relative to control | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosis Survival and Infection Burden in Vivo. |
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| AID421760 | Antibacterial activity against Staphylococcus aureus SA1199B overexpressing NorA efflux pump after 72 hrs | 2009 | Journal of natural products, Mar-27, Volume: 72, Issue:3 | Bioactive pyridine-N-oxide disulfides from Allium stipitatum. |
| AID535776 | Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to RLU count by real-time luminescence method | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains. |
| AID1335283 | Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in BL21(DE3)pLysS cells assessed as inhibition of DNA supercoiling activity in presence of ATP measured after 30 mins by malachite green dye based assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB. |
| AID1365731 | Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv RIF-R2 ATCC 35828 after 5 days | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
| AID1246831 | Bactericidal activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1512378 | Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 6 days by resazurin dye based fluorescence assay | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10 | Novel Pyrazole-Containing Compounds Active against |
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| AID1738819 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse primary macrophage cells assessed as reduction in colony forming unit at 10 uM incubated for 48 hrs followed by macrophage lysis and measured after 3 weeks by alamar blu | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors. |
| AID246807 | Effective concentration required to reduce CFU of Mycobacterium tuberculosis Erdman (ATCC 35801) strain was determined in monolayers of mouse bone marrow macrophages | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | In vitro advanced antimycobacterial screening of cobalt(II) and copper(II) complexes of fluorinated isonicotinoylhydrazones. |
| AID634619 | Antimycobacterial activity against Mycobacterium tuberculosis BE11677 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID649895 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv 331/88 after 21 days | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold. |
| AID1383955 | Bactericidal activity against Mycobacterium tuberculosis H37Rv after 4 weeks by MABA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID1730993 | Antitubercular activity against isoniazid/rifampin resistance Mycobacterium tuberculosis KZN494 by MABA assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules. |
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| AID1174111 | Antimycobacterial activity against isoniazid, rifampin, ethambutol-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis. |
| AID302004 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at MIC | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase. |
| AID1292649 | Drug excretion in human subject slow inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 681 mg, iv infused at constant rate 5.4 min measured 305 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1383978 | Cytotoxicity against human THP1 cells assessed as cell viability at 37.48 ug/ml after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID392606 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | 5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species. |
| AID1890836 | Antimycobacterial activity against Mycobacterium abscessus CIP104536T with smooth morphotype assessed as inhibition of mycobacterial growth incubated for 3 to 5 days by resazurin microtiter assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives. |
| AID1504966 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by second incubation under aerobic condition for 28 hrs by LORA | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid. |
| AID1721014 | Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis. |
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| AID1557249 | Antitubercular activity against resistant Mycobacterium tuberculosis Bangladesh isolate harboring katG Ser315Thr mutant | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
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| AID1287501 | Antitubercular activity against dormant state Mycobacterium tuberculosis H37Ra assessed as viable cells after 12 days by XTT reduction menadione assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents. |
| AID1888655 | Antitubercular activity against multi-drug resistant Mycobacterium tuberculosis 16833 assessed as reduction in bacterial growth incubated for 7 days by Alamar blue assay | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents. |
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| AID768305 | Decrease in NAT1 gene expression in human HCT8 cells at 50 ug/mL after 24 hrs by RT-PCR analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID1767897 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse model of acute tuberculosis infection assessed as log change in bacterial burden in mouse lung at 25 mg/kg, po via gavage administered for 3 weeks starting from d | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis. |
| AID657974 | Cytotoxicity against human HepG2 cells at 20 to 25 uM after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Synthesis of highly potent novel anti-tubercular isoniazid analogues with preliminary pharmacokinetic evaluation. |
| AID768284 | Antibacterial activity against Acinetobacter baumannii 247 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID1891918 | Antimycobacterial activity against Streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 35820 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy. |
| AID1180437 | Antimycobacterial activity against Isoniazid, rifampicin, ofloxacin and ethambutol-resistant Mycobacterium avium 330/88 assessed as complete growth inhibition after 21 days | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates. |
| AID1385219 | Antitubercular activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by microplate alamar blue assay | |||
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| AID1812054 | Cytotoxicity against CHO cells | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Benzoheterocyclic Oxime Carbamates Active against |
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| AID1917331 | Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors. |
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| AID1601822 | Antimycobacterial activity against Mycobacterium bovis BCG | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Marine natural products as potential anti-tubercular agents. |
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| AID679795 | TP_TRANSPORTER: Branched DNA assay in vivo SD rat, liver | 2002 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 30, Issue:7 | Tissue distribution and chemical induction of multiple drug resistance genes in rats. |
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| AID1241002 | Cytotoxicity against human MRC5 cells after 24 hrs | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Guanidinium compounds with sub-micromolar activities against Mycobacterium tuberculosis. Synthesis, characterization and biological evaluations. |
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| AID1736274 | Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days by MABA method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors. |
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| AID1149231 | Antibacterial activity against Mycobacterium tuberculosis assessed as growth inhibition | 1976 | Journal of medicinal chemistry, Apr, Volume: 19, Issue:4 | Mode of action and quantitative structure-activity correlations of tuberculostatic drugs of the isonicotinic acid hydrazide type. |
| AID1690492 | Inhibition of Mycobacterium tuberculosis QcrB T313A mutant assessed as reduction in bacterial growth by resazurin reduction microplate assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents. |
| AID1292617 | Drug excretion in human slow inactivators urine assessed as isoniazid plus hydrazones level at 1 g, iv by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1193496 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID1784353 | Antimycobacterial activity against Mycobacterium tuberculosis H37RvMA in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in |
| AID287809 | Antimicrobial activity against Mycobacterium tuberculosis My 331/88 after 14 days | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities. |
| AID1061099 | Antimicrobial activity against Escherichia coli | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | A novel indigoid anti-tuberculosis agent. |
| AID574806 | Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 horboring rpoB S531L/G566R/I569L, katG S315T/R463L, gyrA A90V/S95T, rrs A1401G by CLSI method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India. |
| AID1333106 | Antimycobacterial activity against Mycobacterium smegmatis MC2 155 after 24 hrs by broth dilution assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties. |
| AID1624149 | Antitubercular activity against isoniazid/ethionamide resistant Mycobacterium tuberculosis isolate 1 after 7 days | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis. |
| AID1173785 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA assay | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 | An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition. |
| AID1339428 | Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis 234/2005 after 14 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Novel salicylanilides from 4,5-dihalogenated salicylic acids: Synthesis, antimicrobial activity and cytotoxicity. |
| AID1309353 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 24 hrs by microbroth dilution method | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines. |
| AID1868117 | Anti-tubercular activity against Mycobacterium tuberculosis CF76 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation. |
| AID569258 | Antimycobacterial activity against Mycobacterium avium subsp. hominissuis 104 | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3 | Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives. |
| AID576933 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv harboring pMV261::dfrA plasmid by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID641647 | Binding affinity to chicken blood dsDNA assessed as shift in Ep/mv at 1 x 10 '-3 M at pH 7.4 by cyclic voltammetry | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Electrochemical and spectroscopic investigations of isoniazide and its analogs with ds.DNA at physiological pH: evaluation of biological activities. |
| AID1459568 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | |||
| AID362954 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Discovery of antimycobacterial spiro-piperidin-4-ones: an atom economic, stereoselective synthesis, and biological intervention. |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID1246818 | Antimycobacterial activity against Mycobacterium tuberculosis E8133 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1332968 | Selectivity index, ratio of IC50 for mouse J774A.1 cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 27294 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis. |
| AID270292 | Antimycobacterial activity against INH-resistant Mycobacterium tuberculosis by agar dilution method | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Synthesis and evaluation of phenoxy acetic acid derivatives as [corrected] anti-mycobacterial agents. |
| AID1891920 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy. |
| AID529527 | Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 5041 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. |
| AID1289108 | Half life in healthy Japanese patient with high NAT2 activity at 10 mg/kg, po by spectrophotometrc method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1916622 | Antitubercular activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as bacterial growth inhibition by XTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Emerging impact of triazoles as anti-tubercular agent. |
| AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
| AID495233 | Antimicrobial activity against Mycobacterium tuberculosis NJT210CGG harboring embB497 CAG-CGG(Gln-Arg) mutation in embB gene after 4 weeks | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 | Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID768297 | Antibacterial activity against Proteus mirabilis 1751 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID1491514 | Antimycobacterial activity against Mycobacterium avium ssp. avium ATCC 15769 harboring pSMT1 carrying luxAB gene after 6 days by luminescence based serial dilution method | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones. |
| AID509681 | Antitubercular activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse spleen at 25 mg/kg, iv after 6 weeks | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs. |
| AID1244410 | Cytotoxicity against African green monkey Vero cells assessed as cell survival at 10 times MIC after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Design, synthesis of benzocoumarin-pyrimidine hybrids as novel class of antitubercular agents, their DNA cleavage and X-ray studies. |
| AID1772577 | Antimycobacterial activity against drug resistant Mycobacterium kansasii 235/80 assessed as minimal inhibitory concentration required for complete inhibition of mycobacterial growth incubated for 7 days | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Design and synthesis of 2-(2-isonicotinoylhydrazineylidene)propanamides as InhA inhibitors with high antitubercular activity. |
| AID384792 | Cytotoxicity against HEK293 cells by MTT assay | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Antimycobacterial activity of diphenylpyraline derivatives. |
| AID1706438 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth by resazurin reduction microplate assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Anti-tubercular profile of new selenium-menadione conjugates against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain and multidrug-resistant clinical isolates. |
| AID1323736 | Growth inhibition of Mycobacterium tuberculosis H37Ra at 0.012 ug/ml after 6 days by microplate alamar blue assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents. |
| AID644439 | Antibacterial activity against Mycobacterium tuberculosis H37Rv harboring pSMT1 encoding Vibrio harveyi luxAB gene infected in mouse J774.A1 cells at 1 uM after 5 days by luminometric analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | 1,4-diarylpiperazines and analogs as anti-tubercular agents: synthesis and biological evaluation. |
| AID1721020 | Antitubercular activity against linezolid-resistant Mycobacterium tuberculosis incubated for 7 days by microplate alamar blue assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis. |
| AID1564353 | Antibacterial activity against Streptococcus pneumoniae ATCC BAA-334 incubated for 24 hrs by resazurin dye based fluorimetric assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis. |
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| AID574582 | Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 obtained from sputum of patient at 0.1 ug/ml by Bactec MGIT960 modified proportion method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India. |
| AID526270 | Toxicity in African green monkey Vero cells | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Design, synthesis, and biological evaluation of 4-(5-nitrofuran-2-yl)prop-2-en-1-one derivatives as potent antitubercular agents. |
| AID1292695 | Drug excretion in human subject rapid inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 670 mg, iv infused at constant rate 5.2min measured 259 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID700528 | Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 at 0.3125 to 5 ug/mL after 7 days by Resazurin assay | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity. |
| AID287816 | Antimicrobial activity against Mycobacterium kansasii My 6509/96 after 7 days | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities. |
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| AID1573723 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2 | Synthesis and biological evaluation of 1H-pyrrolo[2,3-d]pyrimidine-1,2,3-triazole derivatives as novel anti-tubercular agents. |
| AID1163978 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis. |
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| AID384791 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 6.25 ug/ml by alamar blue assay | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Antimycobacterial activity of diphenylpyraline derivatives. |
| AID768300 | Antibacterial activity against Enterobacter cloacae 1845 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID1055938 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv under normoxic condition after 7 days by MABA assay in presence of 4% bovine serum albumin | 2013 | Journal of natural products, Nov-22, Volume: 76, Issue:11 | Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain. |
| AID576917 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 harboring pYUB1062 plasmid overexpressing Mycobacterium tuberculosis Rv1059 unknown gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID421756 | Antibacterial activity against Mycobacterium fortuitum after 72 hrs | 2009 | Journal of natural products, Mar-27, Volume: 72, Issue:3 | Bioactive pyridine-N-oxide disulfides from Allium stipitatum. |
| AID1181163 | Antimicrobial activity against clinical isolate Mycobacterium tuberculosis DKU220 assessed as growth inhibition after 7 days by turbidometry | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system. |
| AID1406216 | Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis after 7 days | |||
| AID1854276 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant |
| AID1739874 | Antimycobacterial activity against isoniazid/rifampicin/ethambutol/kanamycin/ofloxacin multidrug-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth under GAST medium condition after 7 to 14 days by broth microdilution method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Development of small-molecule inhibitors of fatty acyl-AMP and fatty acyl-CoA ligases in Mycobacterium tuberculosis. |
| 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). |
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| AID603130 | Antimycobacterial activity against Mycobacterium tuberculosis isolate 02TBDM039EP097 after 24 hrs by tetrazolium microplate assay | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | Dihydro-β-agarofuran sesquiterpenes isolated from Celastrus vulcanicola as potential anti-Mycobacterium tuberculosis multidrug-resistant agents. |
| AID1289089 | Apparent half life in healthy Chinese subject (8 subjects) with homozygous wild type NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
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| AID378857 | Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 | 2006 | Journal of natural products, Oct, Volume: 69, Issue:10 | Integerrimides A and B, cyclic heptapeptides from the latex of Jatropha integerrima. |
| AID1383953 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 10 days by MABA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID303469 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected CD1 mouse assessed as lung bacterial count at 25 mg/kg, ip after 35 days post infection | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid. |
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| AID1192652 | Inhibition of Mycobacterium tuberculosis H37Rv ATP synthase assessed as reduction in total ATP content at 0.5 ug/ml after 18 hrs by bead-vortexing settling method | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis. |
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| AID1070195 | Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis MTB985 clinical isolate by MTT assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones. |
| AID1765351 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition after 7 days by broth microdilution assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis. |
| AID40838 | Percent inhibition of [3H]- Diazepam binding to GABA-A Benzodiazepine receptor of rat frontal cortex membranes (ND = no data) | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | Orally active and potent inhibitors of gamma-aminobutyric acid uptake. |
| AID1339438 | Antimycobacterial activity against extensively drug resistant Mycobacterium tuberculosis Praha 131 after 21 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Novel salicylanilides from 4,5-dihalogenated salicylic acids: Synthesis, antimicrobial activity and cytotoxicity. |
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| AID325123 | Antimicrobial activity against Mycobacterium tuberculosis TB7 isolate at 0.1 ug/ml after 4 weeks | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1458325 | Intrinsic clearance in human liver microsomes at 1 uM by HPLC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16 | Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery. |
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| AID1073489 | Antibacterial activity against Mycobacterium tuberculosis W210 clinical isolate assessed as parasite growth inhibition after 6 days by microplate Alamar Blue assay | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | SAR studies on trisubstituted benzimidazoles as inhibitors of Mtb FtsZ for the development of novel antitubercular agents. |
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| AID1076895 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method in presence of efflux pump inhibitor verapamil | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development of antimycobacterial tetrahydrothieno[2,3-c]pyridine-3-carboxamides and hexahydrocycloocta[b]thiophene-3-carboxamides: Molecular modification from known antimycobacterial lead. |
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| AID689224 | Antimycobacterial activity against Mycobacterium against recombinant Mycobacterium tuberculosis H37Rv expressing luxAB incubated for 10 days in anaerobic condition followed by incubation for 28 hrs in aerobic condition by LORA assay | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
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| AID1601630 | Antitubercular activity against multi drug resistant Mycobacterium tuberculosis 16995 after 7 days by MABA method | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Synthesis and antitubercular evaluation of reduced lipophilic imidazo[1,2-a]pyridine-3-carboxamide derivatives. |
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| AID1181162 | Antimicrobial activity against clinical isolate Mycobacterium tuberculosis DKU211 assessed as growth inhibition after 7 days by turbidometry | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system. |
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| AID465569 | Cytotoxicity against african green monkey Vero C1008 cells assessed as cell viability at 125 ug/ml after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Novel molecular hybrids of cinnamic acids and guanylhydrazones as potential antitubercular agents. |
| AID509427 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic inhA-15 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID1143489 | Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 27294 | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity. |
| AID1772302 | Non-covalent inhibition of DprE1 in multidrug-resistant Mycobacterium tuberculosis clinical isolate 13946 measured after 7 days by microplate Alamar blue assay | |||
| AID1181167 | Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_1 assessed as fold shift in MIC relative to parent strain | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system. |
| AID1383957 | Ratio of MBC to MIC for Mycobacterium tuberculosis H37Rv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID619384 | Selectivity index, ratio of IC50 for human HepG2 cells to MIC for multidrug-resistant Mycobacterium tuberculosis A8 241 | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | New fluorine-containing hydrazones active against MDR-tuberculosis. |
| AID1292613 | Drug excretion in human rapid inactivators urine assessed as isoniazid plus hydrazones level at 1 g, iv by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID645540 | Antitubercular activity against streptomycin-resistant Mycobacterium tuberculosis by microbroth dilution assay | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity. |
| AID421757 | Antibacterial activity against Mycobacterium smegmatis after 72 hrs | 2009 | Journal of natural products, Mar-27, Volume: 72, Issue:3 | Bioactive pyridine-N-oxide disulfides from Allium stipitatum. |
| AID1514449 | Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety. |
| AID684292 | Antimycobacterial activity against Mycobacterium kansasii My 235/80 after 14 days by micromethod | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Synthesis and in vitro antimycobacterial activity of 2-methoxybenzanilides and their thioxo analogues. |
| AID674504 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by alamar blue broth microdilution assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | Antimycobacterial activity: a facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines. |
| AID1330414 | Inhibition of human ABCB1 expressed in mouse T-lymphoma cells assessed as rhodamine-123 accumulation by measuring fluorescence activity ratio at 1 uM by flow cytometry relative to control | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Discovery of novel N-phenyl 1,4-dihydropyridines with a dual mode of antimycobacterial activity. |
| AID1292686 | Drug excretion in human subject slow inactivator assessed as total isonicotinoyl compound level in urine at 681 mg, iv infused at constant rate 5.4 min measured 710 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID210952 | In vitro inhibition of translocase I; Not determined. | 2003 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17 | Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds. |
| AID509439 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic katG322 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID1063970 | Antimycobacterial activity against isoniazid, rifamycin, streptomycin, ethambutol and clofazimine-resistant Mycobacterium tuberculosis Praha 1 after 21 days | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity. |
| AID297114 | Antibacterial activity against Mycobacterium avium Flamingo after 18 hrs by agar plate dilution method | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17 | Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens. |
| AID1597873 | Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by resazurin microtiter assay | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1851922 | Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as bacterial growth inhibition incubated for 6 days under normoxic condition by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID344826 | Antimycobacterial activity against Mycobacterium bovis BCG by alamar blue assay | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23 | Synthesis of Arabino glycosyl triazoles as potential inhibitors of mycobacterial cell wall biosynthesis. |
| AID657984 | Plasma clearance in Wistar rat at 10 mg/kg, iv administered as single bolus dose | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Synthesis of highly potent novel anti-tubercular isoniazid analogues with preliminary pharmacokinetic evaluation. |
| AID1406742 | Inhibition of replicating Mycobacterium tuberculosis H37Rv InhA assessed as cell growth inhibition after 7 days by MABA method | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis of carbohydrazides and carboxamides as anti-tubercular agents. |
| AID1289100 | AUC in healthy Chinese subject (8 subjects) with homozygous mutant of NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1593374 | Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in multidrug-resistant Mycobacterium tuberculosis V2475 assessed as reduction in bacterial growth by microplate alamar blue assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II. |
| AID183966 | Brain mitochondrial activity measured at 0 min of incubation at 1 uM concentration | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids. |
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| AID1191017 | Antimycobacterial activity against Mycobacterium kansasii ATCC 12478 assessed as reduction in bacterial growth incubated for 6 days by MABA method | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043. |
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| AID145132 | In vitro antibacterial activity against Mycobacterium tuberculosis 103471 | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | New pyrrole derivatives as antimycobacterial agents analogs of BM212. |
| AID1483719 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-c D28N mutant supplemented with 4 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis. |
| AID1416771 | Selectivity ratio of MIC for Mycobacterium smegmatis to MIC for Mycobacterium tuberculosis H37Rv | 2018 | MedChemComm, Jan-01, Volume: 9, Issue:1 | Synthesis and |
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| AID780898 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by REMA assay | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids. |
| AID421787 | Antibacterial activity against Mycobacterium tuberculosis infected in GKO C57BL/6 mouse assessed as bacterial number in lung at 25 mg/kg/day administered 14 days postinfection via oral gavage for nine consecutive days measured on day 24 postinfection | 2009 | Journal of natural products, Mar-27, Volume: 72, Issue:3 | Bioactive pyridine-N-oxide disulfides from Allium stipitatum. |
| AID1772301 | Non-covalent inhibition of DprE1 in Mycobacterium tuberculosis H37Rv measured after 7 days by microplate Alamar blue assay | |||
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| AID665278 | Antitubercular activity against isoniazid, rifampicin and ethambutol-resistant Mycobacterium tuberculosis clinical isolate after 28 days by agar dilution method | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | A solvent free, four-component synthesis and 1,3-dipolar cycloaddition of 4(H)-pyrans with nitrile oxides: synthesis and discovery of antimycobacterial activity of enantiomerically pure 1,2,4-oxadiazoles. |
| AID1383956 | Bactericidal activity against MDR Mycobacterium tuberculosis isolate 591 after 4 weeks by MABA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID532968 | Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 12 | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates. |
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| AID1772574 | Antimycobacterial activity against drug resistant Mycobacterium kansasii 6509/96 assessed as minimal inhibitory concentration required for complete inhibition of mycobacterial growth incubated for 7 days | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Design and synthesis of 2-(2-isonicotinoylhydrazineylidene)propanamides as InhA inhibitors with high antitubercular activity. |
| AID458170 | Toxicity against human HCT8 cells after 72 hrs by XTT assay | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains. |
| AID1265270 | Cytotoxicity against mouse B16F10 cells assessed as cell survival at 50 uM after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase. |
| AID1070203 | Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 by MTT assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones. |
| AID1159306 | Cytotoxicity against African green monkey Vero cells assessed as survival at 50 ug/ml after 48 hrs by Cell-Titre Blue assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design, synthesis and docking studies of some novel (R)-2-(4'-chlorophenyl)-3-(4'-nitrophenyl)-1,2,3,5-tetrahydrobenzo[4,5] imidazo [1,2-c]pyrimidin-4-ol derivatives as antitubercular agents. |
| AID644433 | Antibacterial activity against Mycobacterium tuberculosis H37Rv harboring pSMT1 encoding Vibrio harveyi luxAB gene at 0.1 uM after 7 days by luminometric analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | 1,4-diarylpiperazines and analogs as anti-tubercular agents: synthesis and biological evaluation. |
| AID1484387 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 5 to 8 days | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Isoniazid derivatives and their anti-tubercular activity. |
| AID1143265 | Antimycobacterial activity against Mycobacterium tuberculosis D-211 assessed as growth inhibition after 2 to 3 weeks by turbidometry | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
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| AID1756869 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Antitubercular properties of thiazolidin-4-ones - A review. |
| AID1570240 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by rapid direct susceptibility test | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. |
| AID733452 | Selectivity index, ratio of IC50 for mouse J774.1 cells to MIC for Mycobacterium tuberculosis H37Rv | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Hybrid furoxanyl N-acylhydrazone derivatives as hits for the development of neglected diseases drug candidates. |
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| AID1287442 | Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis H37Rv clinical isolate 7 harboring katG S315T mutant | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold. |
| AID509429 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic ahpC-6 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID392603 | Antimycobacterial activity against Mycobacterium phlei MTCC 1724 by agar dilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | 5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species. |
| AID159987 | Effect on plasma amine oxidase (0.1 uM) after 15 min of incubation at pH 7.2 | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids. |
| AID1732052 | Antibacterial activity against Mycobacterium smegmatis VKPM Ac-1339 | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Discovery of novel N |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1564637 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 16833 assessed as reduction in bacterial cell growth incubated for 7 days by microplate alamar blue assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents. |
| AID1062066 | Antimicrobial activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin assay | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents. |
| AID326166 | Antimalarial activity against Plasmodium falciparum 3D7 | 2007 | The Journal of biological chemistry, Aug-31, Volume: 282, Issue:35 | X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. |
| AID1289107 | Half life in healthy Japanese patient with NAT2 defective activity at 10 mg/kg, po by spectrophotometrc method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID670861 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as minimum concentration required to inhibit 90% growth after 1 week by fluorescence-based microplate Alamar Blue assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents. |
| AID619390 | Antimycobacterial activity against Mycobacterium kansasii CNTC 6509/96 after 7 days | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | New fluorine-containing hydrazones active against MDR-tuberculosis. |
| AID468244 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by microplate Alamar blue assay | 2009 | Journal of natural products, Aug, Volume: 72, Issue:8 | Prenylxanthones and a bicyclo[3.3.1]nona-2,6-diene derivative from the fungus Emericella rugulosa. |
| AID1143263 | Antimycobacterial activity against Mycobacterium tuberculosis Beijing (E-47/94) assessed as growth inhibition after 2 to 3 weeks by turbidometry | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
| AID1194223 | Tuberculostatic activity against Mycobacterium tuberculosis Spec. 192 by two-fold classical test-tube method | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Novel 2-(2-phenalkyl)-1H-benzo[d]imidazoles as antitubercular agents. Synthesis, biological evaluation and structure-activity relationship. |
| AID1287436 | Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis H37Rv clinical isolate 2 harboring InhA promoter C-15T mutant | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold. |
| AID487839 | Antimycobacterial activity against Mycobacterium fortuitum after 48 hrs by microtiter plate method | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives. |
| AID1564357 | Selectivity index, ratio of MIC90 for antimycobacterial activity against Mycobacterium tuberculosis H37Ra lux to CC50 for cytotoxicity against mouse J774A.1 cells | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis. |
| AID1664584 | Antitubercular activity against Mycobacterium bovis BCG assessed as bacterial growth inhibition at 1 ug/ml by MABA relative to control | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16 | The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives. |
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| AID523290 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as 2 log reduction in bacterial burden in lungs orally treated in water upto 8 days | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 | Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis. |
| AID642350 | Binding affinity to chicken blood dsDNA at pH 4.7 by cyclic voltammetry | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Electrochemical and spectroscopic investigations of isoniazide and its analogs with ds.DNA at physiological pH: evaluation of biological activities. |
| AID1143270 | Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis 12119 assessed as growth inhibition after 2 to 3 weeks by turbidometry | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
| AID1488822 | Cytotoxicity against human ARPE19 cells assessed as reduction in cell viability up to 100 uM after 72 hrs by CellTiter-blue assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | The hydrolytic susceptibility of prochelator BSIH in aqueous solutions. |
| AID545234 | Antimycobacterial activity against multidrug-resistant Mycobacterium avium 330/88 after 14 days by micromethod | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | New amino acid esters of salicylanilides active against MDR-TB and other microbes. |
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| AID1593907 | Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis H37Rv assessed as complete inhibition of bacterial growth incubated for 7 days by rapid direct susceptibility test | |||
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| AID256076 | Log CFU in lungs of mice infected with H37Rv stain of Mycobacterium tuberculosis after administration at 25 mg/Kg | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20 | Synthesis and in vitro and in vivo antimycobacterial activity of isonicotinoyl hydrazones. |
| AID1185145 | Antimicrobial activity against 5-(((3S,4R)-3-fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase D89N mutant | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7 | Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing. |
| AID279783 | Clearance of Mycobacterium tuberculosis H37Rv in BALB/c mouse spleen at 25 mg/kg, po five times/week after 1 month relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Aspirin antagonism in isoniazid treatment of tuberculosis in mice. |
| AID1312204 | Antibacterial activity against nutrient-starved dormant Mycobacterium tuberculosis H37Rv assessed in log reduction in bacterial count at 10 ug/ml measured after 7 days by MPN assay relative to control | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors. |
| AID1364756 | Antibacterial activity against Mycobacterium marinum ATCC BAA-535 infected in Zebra fish assessed as log reduction in bacterial counts at 5 mg/kg, po administered for 7 days by MPN assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors. |
| AID1323724 | Growth inhibition of Mycobacterium bovis BCG at 1 ug/ml after 6 days by microplate alamar blue assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents. |
| AID404974 | Antimicrobial activity against Mycobacterium tuberculosis in mouse assessed as microbial kill activity | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Isoniazid bactericidal activity and resistance emergence: integrating pharmacodynamics and pharmacogenomics to predict efficacy in different ethnic populations. |
| 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). |
| AID1170646 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by MABA assay | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12 | Tetrahydroxanthene-1,3(2H)-dione derivatives from Uvaria valderramensis. |
| AID1511342 | Antitubercular activity against clinical drug sensitive Mycobacterium tuberculosis K14b00DS after 14 days in presence of middlebrook 7H9/BSA medium by eleven fold serial dilution method | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | C4-Phenylthio β-lactams: Effect of the chirality of the β-lactam ring on antimicrobial activity. |
| AID665340 | Bacteriostatic activity against Mycobacterium tuberculosis H37Rv at 1 ug/mL assessed as growth index after 3 days by radiometric growth assay (Rvb = 210 growth index) | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives. |
| AID733061 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by BacTiter-Gl Microbial Cell Viability assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents. |
| AID1191522 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Synthesis and in vitro biological evaluation of 2-(phenylcarbamoyl)phenyl 4-substituted benzoates. |
| AID465092 | Antibacterial activity against methicillin-resistant Staphylococcus aureus by modified NCCLS method | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Anti-infective discorhabdins from a deep-water alaskan sponge of the genus Latrunculia. |
| AID1453441 | Toxicity in ip dosed mouse | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Synthesis and biological evaluation of novel 5-aryl-4-(5-nitrofuran-2-yl)-pyrimidines as potential anti-bacterial agents. |
| AID1246813 | Antimycobacterial activity against Mycobacterium tuberculosis TN3183 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID670244 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13 | Synthesis and antimycobacterial activity of some phthalimide derivatives. |
| AID1076820 | Antitubercular activity against extensive drug-resistant Mycobacterium tuberculosis clinical isolate 5 assessed as growth inhibition by microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents. |
| AID1382187 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 7.8 ug/ml after 5 days by microplate alamar blue assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Synthesis of coumarin-theophylline hybrids as a new class of anti-tubercular and anti-microbial agents. |
| AID355908 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by microplate alamar blue assay | 2003 | Journal of natural products, May, Volume: 66, Issue:5 | Antimalarial dihydroisocoumarins produced by Geotrichum sp., an endophytic fungus of Crassocephalum crepidioides. |
| AID634038 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv by twofold serial dilution method | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis of novel 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds and their evaluation for tuberculostatic activity. |
| AID352250 | Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 21 days | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10 | New antituberculotics originated from salicylanilides with promising in vitro activity against atypical mycobacterial strains. |
| AID1333172 | Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 after 5 days by broth dilution assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties. |
| AID623645 | Antituberculosis activity against 5 x 10'4 bacilli per tube Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 0.20 ug/mL incubated for 24 hrs measured after 28 days | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | 1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study. |
| AID1224521 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 7 days by micromethod | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | 1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria. |
| AID640421 | Antitubercular activity against Mycobacterium bovis BCG infected in BALB/c mouse assessed as log reduction in CFU in spleen at 25 mg/kg, po qd administered 48 hrs post infection for 6 weeks measured after 6 weeks (Rvb = 4.79+/-0.25 log10CFU) | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design, synthesis and evaluation of novel molecules with a diphenyl ether nucleus as potential antitubercular agents. |
| AID1289081 | Cmax in healthy Chinese subject (8 subjects) with heterozygous mutant of NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID487840 | Antimycobacterial activity against Mycobacterium kansasii after 48 hrs by microtiter plate method | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives. |
| AID297110 | Antibacterial activity against Mycobacterium tuberculosis H37Rv after 18 hrs by agar plate dilution method | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17 | Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens. |
| AID1399840 | Antibacterial activity against Mycobacterium tuberculosis H37Rv | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase. |
| AID1901691 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured by MABA assay | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis. |
| AID669845 | Antibacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv by microplate alamar blue assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis. |
| AID1437024 | Inhibition of Mycobacterium tuberculosis His6-tagged InhA expressed in Escherichia coli BL21 (DE3) assessed as decrease in NADH oxidation to NAD+ at 10 uM using 2-trans-decenoyl-CoA as substrate preincubated for 2 hrs followed by substrate and NADH additi | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis. |
| AID1492905 | Intrinsic clearance in mouse liver microsomes | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Addressing the Metabolic Stability of Antituberculars through Machine Learning. |
| AID265977 | Cytotoxicity against Vero cell line | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Discovery of new antitubercular oxazolyl thiosemicarbazones. |
| AID1403737 | Antibacterial activity against Staphylococcus aureus ATCC 6538 after overnight incubation by microbroth dilution method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Amino acid conjugated antimicrobial drugs: Synthesis, lipophilicity- activity relationship, antibacterial and urease inhibition activity. |
| AID294763 | Antibacterial activity against methicillin-resistant Staphylococcus aureus 906 after 2 weeks by broth dilution method | 2007 | Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9 | Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus. |
| AID1416769 | Antimycobacterial activity against Mycobacterium smegmatis after 72 hrs by broth microdilution method | 2018 | MedChemComm, Jan-01, Volume: 9, Issue:1 | Synthesis and |
| AID344016 | Antitubercular activity against Mycobacterium tuberculosis H37Ra under hypoxic condition after 14 days by MTT method | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Halicyclamine A, a marine spongean alkaloid as a lead for anti-tuberculosis agent. |
| AID1289101 | Clearance in healthy Chinese subject (8 subjects) with homozygous mutant of NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1395196 | Antitubercular activity against multi-drug resistant Mycobacterium tuberculosis isolate 16995 after 7 days by Alamar blue assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety. |
| AID1265273 | Inhibition of tyrosinase in mouse B16F10 cells assessed as reduction of melanin production at 50 uM relative to control | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase. |
| AID538991 | Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 14 days by microdilution method | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Highly active antimycobacterial derivatives of benzoxazine. |
| AID325125 | Antimicrobial activity against Mycobacterium tuberculosis TB7 isolate at 0.4 ug/ml after 2 weeks | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1252459 | Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | 4-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation. |
| AID310491 | Stability in rat liver microsomes after 90 mins | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Discovery of novel isoxazolines as anti-tuberculosis agents. |
| AID1646892 | Antimycobacterial activity against Mycobacterium tuberculosis 71A harbouring KatG Ser315Thr mutant and wild type InhA assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and anti-Mycobacterium tuberculosis activity of imide-β-carboline and carbomethoxy-β-carboline derivatives. |
| AID1237430 | Antimycobacterial activity against Mycobacterium smegmatis str. MC2 155 incubated for 30 hrs by turbidometric assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Synthesis and evaluation of novel fluorinated pyrazolo-1,2,3-triazole hybrids as antimycobacterial agents. |
| AID325144 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv subculture 1 with wild type katG mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1739763 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition incubated for 3 weeks by Microplate Alamar Blue Assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors. |
| AID1706097 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth by agar plate dilution method | |||
| AID1165081 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by MABA method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and antimycobacterial activity of various 3-(4-(substitutedsulfonyl)piperazin-1-yl)benzo[d]isoxazole derivatives. |
| AID589250 | Mechanism based inhibition of human cytochrome P450 2C19 evaluated using Tolbutamide | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
| AID1381929 | Genotoxicity in Salmonella typhimurium TA98 assessed as increase in revertant colonies at 0.5 uM preincubated for 20 mins followed by addition of top agar and minimal agar and measured after 72 hrs in presence of S9 metabolic activation system by Ames tes | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
| AID574809 | Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 horboring rpoB H526Y, katG D329A/R463L, gyrA D94G/S95T, rrs A1401G by CLSI method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India. |
| AID566906 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth in dormant phase | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection. |
| AID344012 | Antitubercular activity against Mycobacterium smegmatis MC2 155 under hypoxic condition after 96 hrs by MTT method | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Halicyclamine A, a marine spongean alkaloid as a lead for anti-tuberculosis agent. |
| AID1143691 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in spleen at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 1 | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation. |
| AID245536 | In vitro antimycobacterial activity against Mycobacterium tuberculosis Erdman in broth cluture infected with macrophages;nd = not determined | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: part 14. |
| AID244763 | Minimum bactericidal required against isoniazid resistant Mycobacterium tuberculosis was determined in monolayers of mouse bone marrow macrophages | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | In vitro advanced antimycobacterial screening of cobalt(II) and copper(II) complexes of fluorinated isonicotinoylhydrazones. |
| AID1292711 | Drug excretion in human subject rapid inactivator assessed as total isonicotinoyl compound level in urine at 670 mg, iv infused at constant rate 5.2min measured 259 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1743152 | Inhibition of ATP synthase in bedaquiline-resistant Mycobacterium tuberculosis assessed as reduction in bacterial growth incubated for 7 days by microplate alamar blue assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis. |
| AID1246809 | Antimycobacterial activity against Mycobacterium tuberculosis TN1051 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID345805 | Antagonist activity at guinea pig ileum histamine H1 receptor at 0.3 x 10'4 M | 2008 | Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24 | Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives. |
| AID1292630 | Drug metabolism in human slow inactivators assessed as excretion of pyruvic acid isonicotinoylhydrazone in urine at 1 g, iv by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID545243 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 357/2005 after 21 days by micromethod | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | New amino acid esters of salicylanilides active against MDR-TB and other microbes. |
| AID644364 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 7 to 14 days by twofold serial broth dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis and antimalarial and antituberculosis activities of a series of natural and unnatural 4-methoxy-6-styryl-pyran-2-ones, dihydro analogues and photo-dimers. |
| AID594795 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Synthesis, structure-activity relationship of novel substituted 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates as potential anti-mycobacterial and anticancer agents. |
| AID1231579 | Antibacterial activity against Mycobacterium smegmatis MC2 155 under hypoxic condition after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Anti-dormant mycobacterial activity and target analysis of nybomycin produced by a marine-derived Streptomyces sp. |
| AID1646887 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and anti-Mycobacterium tuberculosis activity of imide-β-carboline and carbomethoxy-β-carboline derivatives. |
| AID484740 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv under dormancy-inducing hypoxic condition | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Trichoderins, novel aminolipopeptides from a marine sponge-derived Trichoderma sp., are active against dormant mycobacteria. |
| AID348342 | Antimycobacterial activity against rifampin and isoniazid-susceptible Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by Alamar blue assay | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis and anti-mycobacterial activity of (E)-N'-(monosubstituted-benzylidene)isonicotinohydrazide derivatives. |
| AID619382 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis A8 241 after 28 days by colony forming unit determination | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | New fluorine-containing hydrazones active against MDR-tuberculosis. |
| AID1400020 | Antibacterial activity against Mycobacterium tuberculosis Erdman infected in Balb/c mouse assessed as reduction in bacterial load in lungs at 2.5 mg/kg, po for 3 weeks starting from 10 days post infection measured on day 21 post infection | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | An antimycobacterial pleuromutilin analogue effective against dormant bacilli. |
| AID1381943 | Cytotoxicity against human HepG2 cells after 3 hrs by WST-1 assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
| AID1192651 | Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC100 for Mycobacterium tuberculosis H37Rv | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis. |
| AID576921 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 harboring pYUB1062 plasmid overexpressing Mycobacterium tuberculosis Rv2766 FabG5 gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID576907 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 harboring pYUB1062 plasmid overexpressing Mycobacterium tuberculosis Rv3248c SahH gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID641636 | Antibacterial activity against Salmonella typhi ATCC 6539 at 1 mg/ml after 24 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Electrochemical and spectroscopic investigations of isoniazide and its analogs with ds.DNA at physiological pH: evaluation of biological activities. |
| AID1253866 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis FJ05120 after 3 to 4 weeks by microplate alamar blue assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Discovery of the disubstituted oxazole analogues as a novel class anti-tuberculotic agents against MDR- and XDR-MTB. |
| AID1244806 | Antibacterial activity against Staphylococcus aureus ATCC 6538 after 18 hrs by serial microdilution method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis. |
| AID649717 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv by REMA method | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | Novel N'-benzylidene benzofuran-3-carbohydrazide derivatives as antitubercular and antifungal agents. |
| AID1292670 | Drug excretion in human subject slow inactivator assessed as total isonicotinoyl compound level in urine at 681 mg, iv infused at constant rate 5.4 min measured 208.7 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1292710 | Drug excretion in human subject rapid inactivator assessed as total isonicotinoyl compound level in urine at 670 mg, iv infused at constant rate 5.2min measured 227 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1879690 | Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS). |
| AID650748 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents. |
| AID634614 | Antimycobacterial activity against Mycobacterium tuberculosis TN2524 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1339431 | Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis 9449/2007 after 21 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Novel salicylanilides from 4,5-dihalogenated salicylic acids: Synthesis, antimicrobial activity and cytotoxicity. |
| AID665348 | Bacteriostatic activity against Mycobacterium tuberculosis H37Rv at 0.5 ug/mL assessed as growth index after 7 days by radiometric growth assay (Rvb = 210 growth index) | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives. |
| AID1358587 | Antimycobacterial activity against INH/RIF/OFX resistant Mycobacterium avium 330/88 after 14 days | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action. |
| AID245447 | Minimum inhibitory concentration against sensitive Mycobacterium tuberculosis clinical isolates; N=9; Range = 0.12-0.25 | 2005 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6 | Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents. |
| AID603129 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 24 hrs by tetrazolium microplate assay | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | Dihydro-β-agarofuran sesquiterpenes isolated from Celastrus vulcanicola as potential anti-Mycobacterium tuberculosis multidrug-resistant agents. |
| AID1070197 | Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis UT544 clinical isolate by MTT assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones. |
| AID1292654 | Drug excretion in human subject slow inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 681 mg, iv infused at constant rate 5.4 min measured 466 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID457888 | Antimycobacterial activity against Mycobacterium tuberculosis 331/88 after 14 days by micromethod | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains. |
| AID245333 | In vitro antimycobacterial activity against ethionamide-resistant Mycobacterium tuberculosis strain; nd= not determined | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: part 14. |
| AID768302 | Antibacterial activity against Staphylococcus hominis 1813 assessed as growth inhibition at 1 mg/mL after 24 hrs by agar-disk diffusion technique | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID1365711 | Antitubercular activity against luxABCDE expressing Mycobacterium tuberculosis H37Rv infected in mouse J774 macrophages assessed as log reduction in bacterial colonies at 2.6 uM measured after 4 days under aerobic condition by luminescence assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
| AID1063941 | Antimycobacterial activity against isoniazid, rifamycin, streptomycin, ethambutol and ofloxacin, clofazimine-resistant Mycobacterium tuberculosis Praha 4 after 21 days | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity. |
| AID1326673 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors. |
| AID494995 | Hepatotoxicity in po dosed rat assessed as effect on serum SGOT level (Rvb = 143.71 +/- 1.1 U/mL) | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid. |
| AID1058227 | Antimycobacterial activity against Mycobacterium fortuitum | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis. |
| AID623585 | Antituberculosis activity against 5 x 10'4 inoculum per tube Mycobacterium tuberculosis H37Rv after 24 hrs by Lowenstein-Jensen method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | 1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study. |
| AID685007 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 clinical isolate after 14 days by micromethod | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Synthesis and in vitro antimycobacterial and isocitrate lyase inhibition properties of novel 2-methoxy-2'-hydroxybenzanilides, their thioxo analogues and benzoxazoles. |
| AID535825 | Antibacterial activity against Mycobacterium tuberculosis infected in Hartley guinea pig lung assessed as reduction in bacterial load at 30 mg/kg | 2008 | Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11 | Metronidazole lacks antibacterial activity in guinea pigs infected with Mycobacterium tuberculosis. |
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| AID1072705 | Inhibition of Mycobacterium tuberculosis pantothenate synthetase expressed in Escherichia coli BL21 (DE3) | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Development of novel tetrahydrothieno[2,3-c]pyridine-3-carboxamide based Mycobacterium tuberculosis pantothenate synthetase inhibitors: molecular hybridization from known antimycobacterial leads. |
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| AID779946 | Antimycobacterial activity against Mycobacterium smegmatis ATCC 700084 after 3 days by two-fold serial dilution method | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Antimycobacterial and herbicidal activity of ring-substituted 1-hydroxynaphthalene-2-carboxanilides. |
| AID1624151 | Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 after 7 days | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis. |
| AID1295090 | Tuberculostatic activity against Mycobacterium terrae assessed as induction of penetration size stunting incubated for 10 days by vertical diffusion method | 2016 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10 | A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity. |
| AID1192659 | Bactericidal activity against non-replicating Mycobacterium tuberculosis H37Rv Wayne model under hypoxic/oxygen depleted conditions assessed as log reduction after 4 days by serial dilution assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis. |
| AID1373645 | Antimycobacterial activity against XDR Mycobacterium tuberculosis isolate X_60 by two fold serial dilution based fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis. |
| AID1384045 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by MABA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Recent advances of imidazole-containing derivatives as anti-tubercular agents. |
| AID1443441 | Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 up to 4 times MIC90 after 8 weeks | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Amphiphilic Indole Derivatives as Antimycobacterial Agents: Structure-Activity Relationships and Membrane Targeting Properties. |
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| AID1244827 | Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by serial microdilution method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis. |
| AID1825032 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST media incubated for 8 days by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition. |
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| AID1204432 | Toxicity in ip dosed mouse after 14 days | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds. |
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| AID1879693 | Antimycobacterial activity against PAS resistant Mycobacterium tuberculosis H37Rv harboring S150G mutant assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS). |
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| AID1916536 | Antibacterial activity against Mycobacterium tuberculosis incubated for 1 to 2 weeks in 7H9/DPPC/casitone/Tx medium | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | 6-Fluorophenylbenzohydrazides inhibit Mycobacterium tuberculosis growth through alteration of tryptophan biosynthesis. |
| AID1743154 | Antitubercular activity against Mycobacterium tuberculosis H37Rv | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation. |
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| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
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| AID1301204 | Cytotoxicity against human FEH cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides. |
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| 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). |
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| AID256827 | Maximum concentration in female C57BL/6 mice administered with 300 mg/kg, po | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | Synthesis and evaluation of cyclic secondary amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents. |
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| AID529531 | Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-CTG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. |
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| AID1072704 | Cytotoxicity against mouse RAW264.7 cells at 50 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Development of novel tetrahydrothieno[2,3-c]pyridine-3-carboxamide based Mycobacterium tuberculosis pantothenate synthetase inhibitors: molecular hybridization from known antimycobacterial leads. |
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| AID576914 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 harboring pYUB1062 plasmid overexpressing Mycobacterium tuberculosis Rv2691 CeoB/TrKA gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID721559 | Lipophilicity, log K of the compound in methanol-water mixture by HPLC analysis | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Synthesis and antimycobacterial evaluation of pyrazinamide derivatives with benzylamino substitution. |
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| AID289151 | Antimycobacterial activity against streptomycin, isoniazid, rifampicin, pyrazinamide-resistant Mycobacterium tuberculosis CIBIN 234 isolates | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines. |
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| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1577333 | Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 9449/2007 after 21 days | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase. |
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| AID489574 | Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 14 days by microdilution method | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | A note to the biological activity of benzoxazine derivatives containing the thioxo group. |
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| AID1868119 | Anti-tubercular activity against Mycobacterium tuberculosis CF161 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation. |
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| AID1381952 | Genotoxicity in Salmonella typhimurium TA100 assessed as increase in revertant colonies at 5 uM preincubated for 20 mins followed by addition of top agar and minimal agar and measured after 72 hrs in absence of S9 metabolic activation system by Ames test | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
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| AID1853652 | Antibacterial activity against Mycobacterium avium ATCC 25921 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
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| AID1772329 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as reduction in bacterial burden in mouse lung at 25 mg/kg, po via gavage administered for 20 days starting from day 10 post infection (Rvb = 6.44 +/- 0. | |||
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| AID1174924 | Antitubercular activity against Mycobacterium tuberculosis isolate 439/11 after 7 days by REMA resazurin microtiter assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines. |
| AID1484379 | Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate 303 by broth dilution method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Isoniazid derivatives and their anti-tubercular activity. |
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| AID1891917 | Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy. |
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| AID1278843 | Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 50 uM after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6 | Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors. |
| AID1381939 | Cytotoxicity against mouse J774A.1 cells assessed as decrease in cell viability at 100 nM after 20 hrs by resazurin dye-based fluorimetric method | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
| AID1400034 | Bactericidal activity against replicating Mycobacterium tuberculosis H37Rv incubated for 15 days under aerobic condition by MABA | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | An antimycobacterial pleuromutilin analogue effective against dormant bacilli. |
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| AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
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| AID1290448 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 2 to 4 weeks by Lowensteine-Jensen method | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Novel morpholinoquinoline nucleus clubbed with pyrazoline scaffolds: Synthesis, antibacterial, antitubercular and antimalarial activities. |
| AID566905 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth in log phase by agar dilution method | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection. |
| AID1378014 | Antimycobacterial activity against Mycobacterium tuberculosis MC2 6230 | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Triazole derivatives and their anti-tubercular activity. |
| AID1593910 | Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero cells to MIC for antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis H37Rv | |||
| AID1406780 | Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents. |
| AID1871138 | Antitubercular activity against Multidrug-resistant Mycobacterium tuberculosis qcrB-T313A mutant assessed as bacterial growth inhibition incubated for 7 days by resazurin dye based assay | 2022 | ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8 | Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties. |
| AID1272279 | Cytotoxicity against C57BL/6 mouse peritoneal macrophages assessed as cell viability by lactate dehydrogenase release assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | Synthesis and antituberculosis activity of indole-pyridine derived hydrazides, hydrazide-hydrazones, and thiosemicarbazones. |
| AID685000 | Antimycobacterial activity against Mycobacterium tuberculosis 331/88 after 21 days by micromethod | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Synthesis and in vitro antimycobacterial and isocitrate lyase inhibition properties of novel 2-methoxy-2'-hydroxybenzanilides, their thioxo analogues and benzoxazoles. |
| AID665350 | Bacteriostatic activity against Mycobacterium tuberculosis H37Rv at 0.1 ug/mL assessed as growth index after 3 days by radiometric growth assay (Rvb = 210 growth index) | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives. |
| AID625700 | Cytotoxicity against human PBMC by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | New series of isoniazid hydrazones linked with electron-withdrawing substituents. |
| AID657786 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 164 from Chinese tuberculosis patient measured 24 hrs post dose by microplate alamar blue assay | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives. |
| AID432681 | Antimycobacterial against multidrug resistant Mycobacterium tuberculosis by agar dilution method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | A facile synthesis and antimycobacterial evaluation of novel spiro-pyrido-pyrrolizines and pyrrolidines. |
| AID634616 | Antimycobacterial activity against Mycobacterium tuberculosis TN3979 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID528957 | Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 300 mg/kg, po once daily measured after 6 days | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8 | Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. |
| AID515918 | Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID1416247 | Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis clinical isolate | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant |
| AID1491288 | Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives. |
| AID494997 | Hepatotoxicity in po dosed rat assessed as effect on serum alkaline phosphatase level (Rvb = 12.17 +/- 0.16 U/mL) | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid. |
| AID1477416 | Antibacterial activity against wild type Mycobacterium tuberculosis H37Rv grown in GAST/Fe medium measured on day 14 post inoculation by broth microdilution method | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 | Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies. |
| AID1756892 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC27294 measured after 28 days by two-fold serial dilution method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Antitubercular properties of thiazolidin-4-ones - A review. |
| AID1179480 | Antimycobacterial activity against Mycobacterium marinum ATCC 927 in 7H9 medium after 5 days and 6 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates. |
| AID245485 | Minimum inhibitory concentration tested against Mycobacterium tuberculosis resistant clinical isolates; Range 8->16 ug/mL | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Antitubercular agents. Part 1: synthesis of phthalimido- and naphthalimido-linked phenazines as new prototype antitubercular agents. |
| AID370074 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35812 after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID523294 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as lowest concentration to reduce bacterial burden in lungs to level of reduction achieved with higher doses orally treated in water upto 8 days | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 | Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis. |
| AID1483732 | Selectivity ratio of MIC for Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit a K179N mutant supplemented with 8 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione to MIC for Mycobacterium tuberculosis | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis. |
| AID565229 | Antimicrobial activity against Mycobacterium chelonae ATCC 35752 harboring pZS01 carrying mspA gene by resazurine microtiter assay | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs. |
| AID1697972 | Inhibition of Mycobacterium tuberculosis mc2 6230 InhA assessed as antimycobacterial activity by measuring minimum inhibitory concentration required to inhibit 99% of bacterial growth | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22 | Design and synthesis of 4-Aminoquinoline-isoindoline-dione-isoniazid triads as potential anti-mycobacterials. |
| AID305979 | Antimycobacterial activity against Mycobacterium smegmatis mc2155 after 48 hrs by microdilution resazurin assay | 2007 | Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5 | Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues. |
| AID1204851 | Antitubercular activity against Isoniazid-resistant Mycobacterium tuberculosis assessed as parasite growth inhibition by REMA method | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID1593373 | Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in drug-susceptible Mycobacterium tuberculosis V4207 assessed as reduction in bacterial growth by microplate alamar blue assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II. |
| AID1627188 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by MABA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Preparation, biological evaluation and molecular docking study of imidazolyl dihydropyrimidines as potential Mycobacterium tuberculosis dihydrofolate reductase inhibitors. |
| AID634541 | Antimycobacterial activity against Mycobacterium tuberculosis TN913 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID509628 | Antibacterial activity against Mycobacterium tuberculosis containing phenotypic rpoB513,katG315,inhA-15,ahpC-10,ahpC-6 mutation assessed as microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID382876 | Antitubercular activity against Mycobacterium tuberculosis H37Rv micro-dilution Resazurin assay | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Antifungal and antimycobacterial activity of 1-(3,5-diaryl-4,5-dihydro-1H-pyrazol-4-yl)-1H-imidazole derivatives. |
| AID616700 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in Swiss mouse infected assessed as mouse survival at 25 mg/kg/day, po for 28 days measured on day 40 post infection | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Novel aryloxy azolyl chalcones with potent activity against Mycobacterium tuberculosis H37Rv. |
| AID1289103 | Cmax in healthy Chinese subject (8 subjects) with homozygous mutant of NAT2 genotype assessed as N-acetylisoniazid at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1243392 | Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Synthesis and biological evaluation of phaitanthrin congeners as anti-mycobacterial agents. |
| AID683317 | Antibacterial activity against Bacillus subtilis ATCC 6633 by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776. |
| AID1570241 | Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. |
| AID685008 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 clinical isolate after 21 days by micromethod | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Synthesis and in vitro antimycobacterial and isocitrate lyase inhibition properties of novel 2-methoxy-2'-hydroxybenzanilides, their thioxo analogues and benzoxazoles. |
| AID144150 | In vitro inhibition of Mycobacterium Kansasi (My 6 509/96) growth after 14 days culture. | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Heterocyclic benzazole derivatives with antimycobacterial in vitro activity. |
| AID436697 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by BACTEC radiometric respiratory technique | 2009 | European journal of medicinal chemistry, Oct, Volume: 44, Issue:10 | Synthesis, spectral and biological evaluation of some new thiazolidinones and thiazoles based on t-3-alkyl-r-2,c-6-diarylpiperidin-4-ones. |
| AID1070193 | Antimycobacterial activity against Mycobacterium fortuitum MNT1073 clinical isolate by MTT assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones. |
| AID1285204 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 25177 assessed as growth inhibition at 0.2 ug/ml after 28 days by Lowenstein-Jensen method | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Novel nicotine analogues with potential anti-mycobacterial activity. |
| AID1289105 | Clearance in healthy Chinese subject (8 subjects) with homozygous mutant of NAT2 genotype assessed as N-acetylisoniazid at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID540173 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction of relative light unit at 1 ug/ml after 72 hrs by luciferase reporter phage assay relative to control | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and anti-tubercular and antimicrobial activities of some 2r,4c-diaryl-3-azabicyclo[3.3.1]nonan-9-one N-isonicotinoylhydrazone derivatives. |
| AID641634 | Antibacterial activity against Bordetella bronchiseptica ATCC 10580 at 1 mg/ml after 24 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Electrochemical and spectroscopic investigations of isoniazide and its analogs with ds.DNA at physiological pH: evaluation of biological activities. |
| AID1634341 | Antimycobacterial activity against Pyrazinamide-resistant Mycobacterium tuberculosis ATCC 35828 assessed as inhibition of bacterial cell growth incubated for 7 days by resazurin microtiter assay | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Design, synthesis and antimycobacterial activity of benzoxazinone derivatives and open-ring analogues: Preliminary data and computational analysis. |
| AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID303466 | Antimycobacterial activity against multi-drug-resistant Mycobacterium tuberculosis by agar dilution method | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid. |
| AID363987 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 days by microdilution resazurin assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial. |
| AID1491403 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay | |||
| AID1383983 | Cytotoxicity against human THP1 cells assessed as cell viability at 150 ug/ml after 48 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole. |
| AID1174107 | Antimycobacterial activity against isoniazid, rifampin, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis. |
| AID1181166 | Antimicrobial activity against clinical isolate Rifampin-resistant Mycobacterium tuberculosis assessed as growth inhibition after 7 days by turbidometry | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system. |
| AID1163980 | Antimycobacterial activity against isoniazid, rifampicin, ofloxacin and kanamycin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 clinical isolate after 28 days by two-fold serial dilution assay in presence of 8 mg/mL piperine efflux pump inhibitor | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis. |
| AID1632661 | Antitubercular activity against active Mycobacterium tuberculosis H37Ra ATCC 25177 after 8 days by XTT reduction menadione assay | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8 | Synthesis and Antitubercular Activity of New Benzo[b]thiophenes. |
| AID1250472 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra after 7 days by alamar blue dye assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L. |
| AID1193921 | Inhibition of Mycobacterium smegmatis DNA GyrB domain assessed as inhibition of inorganic phosphate release after 100 mins at room temperature by ATPase assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain. |
| AID1756033 | Antitubercular activity against Mycobacterium tuberculosis H37Ra assessed as bacterial growth inhibition | |||
| AID1292696 | Drug excretion in human subject rapid inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 670 mg, iv infused at constant rate 5.2min measured 296 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1232406 | Antimycobacterial activity against Mycobacterium bovis BCG after 7 days | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides. |
| AID1888137 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD3 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains. |
| AID1739876 | Antimycobacterial activity against isoniazid/rifampicin/ethambutol/para-aminosalicylic acid extensively drug-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth under GAST medium condition after 7 to 14 days by broth microdilut | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Development of small-molecule inhibitors of fatty acyl-AMP and fatty acyl-CoA ligases in Mycobacterium tuberculosis. |
| AID1365705 | Antitubercular activity against fluoroquinolone-resistant Mycobacterium tuberculosis H37Rv harboring gyrB D94N mutant after 5 days | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
| AID1192646 | Inhibition of Mycobacterium smegmatis TMC 607 ATP synthase incubated for 10 mins prior to NADH addition measured after 1 hr by luminescence assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis. |
| AID1296381 | Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 7 days by microdilution method | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis. |
| AID74655 | Percent of enzyme inhibition by Glutamate decarboxylase assay method | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | Orally active and potent inhibitors of gamma-aminobutyric acid uptake. |
| AID1358613 | Selectivity index, ratio of IC50 for human HepG2 cells to MIC for Mycobacterium kansasii 6509/96 | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action. |
| AID1390094 | Antimycobacterial activity against active form of Mycobacterium tuberculosis H37Rv measured after 7 days by alamar blue assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] analogues against both active and dormant Mycobacterium tuberculosis. |
| AID1179481 | Antimycobacterial activity against Mycobacterium avium ATCC 15769 in 7H9 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates. |
| AID509433 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic ahpC-9 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID532962 | Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 6 | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates. |
| AID1542194 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 12 to 28 days by agar dilution method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Pyridine and nitro-phenyl linked 1,3,4-thiadiazoles as MDR-TB inhibitors. |
| AID1608990 | Antimycobacterial activity against Mycobacterium avium 330/88 after 14 days | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds. |
| AID532969 | Antimicrobial activity against Mycobacterium tuberculosis isolate 13 isolated from Beijing | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates. |
| AID1360448 | Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate CDCT10 harboring rpoB/katG mutant gene after 7 days by resazurin dye based assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | 1H-Benzo[d]imidazoles and 3,4-dihydroquinazolin-4-ones: Design, synthesis and antitubercular activity. |
| AID1868118 | Anti-tubercular activity against Mycobacterium tuberculosis CF152 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation. |
| AID292287 | Antibacterial activity against Escherichia coli ATCC 25922 after 16 to 20 hrs by broth microdilution method | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs. |
| AID625694 | Antimycobacterial activity against Mycobacterium kansasii CNTC My 335/80 after 14 days | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | New series of isoniazid hydrazones linked with electron-withdrawing substituents. |
| AID1576552 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in medium containing 7H9/glucose/BSA/Tyloxapol assessed as reduction in bacterial growth incubated for 7 days by Alamar blue reagent based assay | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Dual-target inhibitors of mycobacterial aminoacyl-tRNA synthetases among |
| AID1557250 | Antitubercular activity against resistant Mycobacterium tuberculosis TDR harboring inhA Promoter (c-15 t)/IIe21Thr mutant | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID1655164 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.1 cells assessed as reduction in bacterial colony at 1 to 10 times MIC incubated for 72 hrs by colony counting method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Improving the Potency of |
| AID1276380 | Selectivity index, ratio of GI50 for human A431 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent. |
| AID774598 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene infected in mouse J774 macrophages assessed as intracellular growth inhibition at 1 uM after 4 days by luminometry relative to untreated control | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine. |
| AID1372625 | Inhibition of recombinant Bacillus subtilis subsp. subtilis 168 N-terminal His-tagged glutamate racemase expressed in Escherichia coli BL21(DE3) using D-glutamate as substrate in presence of NAD+ by spectrophotometric based L-glutamate dehydrogenase enzym | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Lead identification and optimization of bacterial glutamate racemase inhibitors. |
| AID1272620 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by broth microdilution method | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases. |
| AID634611 | Antimycobacterial activity against Mycobacterium tuberculosis TN1051 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1174920 | Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by REMA resazurin microtiter assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines. |
| AID1827077 | Antibacterial activity against Mycobacterium tuberculosis mc2 6230 assessed as reduction in viable cells at 10 times MIC measured for 42 days in solid media by time kill assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A. |
| AID442658 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives. |
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| AID404972 | AUC (0 to 24 hrs)/MIC ratio in Mycobacterium tuberculosis infected mouse model | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Isoniazid bactericidal activity and resistance emergence: integrating pharmacodynamics and pharmacogenomics to predict efficacy in different ethnic populations. |
| AID1194570 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing Lux assessed as reduction in growth measured after 3 weeks by bioluminescence assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Design and synthesis of novel anti-tuberculosis agents from the celecoxib pharmacophore. |
| AID1246814 | Antimycobacterial activity against Mycobacterium tuberculosis TN3979 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1742595 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 to 14 days under 7H9/glucose medium | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Endeavors towards transformation of M. tuberculosis thymidylate kinase (MtbTMPK) inhibitors into potential antimycobacterial agents. |
| AID1854284 | Antitubercular activity against clinical isolate isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant |
| AID1292676 | Drug excretion in human subject slow inactivator assessed as total isonicotinoyl compound level in urine at 681 mg, iv infused at constant rate 5.4 min measured 396 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID144016 | In vitro anti-mycobacterial activity against Mycobacterium fortuitum was determined | 2004 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6 | Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480. |
| AID765104 | Bacteriostatic activity against rifampicin, isoniazid, streptomycin, ethambutol and pyrazinamide-resistant Mycobacterium tuberculosis MS-115 assessed as growth inhibition | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides. |
| AID1891914 | Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy. |
| AID287749 | Antimycobacterial activity against Mycobacterium avium 330/88 after 21 days | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | A new modification of anti-tubercular active molecules. |
| AID1292661 | Drug excretion in human subject slow inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 681 mg, iv infused at constant rate 5.4 min measured 677 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1454449 | Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents. |
| AID1491291 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 treated for 10 days under hypoxic condition followed by 28 hrs of normoxic recovery | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity. |
| AID144144 | Antimycobacterial activity against Mycobacterium kansasii ATCC 12478 | 2003 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17 | Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds. |
| AID1381950 | Genotoxicity in Salmonella typhimurium TA98 assessed as increase in revertant colonies at 5000 uM preincubated for 20 mins followed by addition of top agar and minimal agar and measured after 72 hrs in absence of S9 metabolic activation system by Ames tes | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
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| AID1687477 | Antibacterial activity against Mycobacterium fortuitum assessed as inhibition of microbial growth incubated for 1 week by MABA method | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents. |
| AID619389 | Antimycobacterial activity against Mycobacterium kansasii CNTC My 235/80 after 21 days | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | New fluorine-containing hydrazones active against MDR-tuberculosis. |
| AID620090 | Antimicrobial activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties. |
| AID1738818 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in colony forming unit at 1 to 10 ug/ml incubated for 7 days in nutrient starvation medium by alamar blue based serial dilution method | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors. |
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| AID768304 | Antioxidant activity assessed as DPPH radical scavenging activity at 0.1 mg/mL after 30 mins under dark conditions by spectrophotometric analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis and bioevaluation of some new isoniazid derivatives. |
| AID1484389 | Antimycobacterial activity against Mycobacterium bovis 8 by serial dilution method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Isoniazid derivatives and their anti-tubercular activity. |
| AID1589011 | Anti-mycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis | |||
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| AID1358611 | Selectivity index, ratio of IC50 for human HepG2 cells to MIC for INH/RIF/rifabutine/STM/EMB/OFX/gentamicin/amikacin resistant Mycobacterium tuberculosis Praha 131 | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action. |
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| AID1373646 | Cytotoxicity against CHO cells | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis. |
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| AID1339432 | Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis 242/2015 after 14 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Novel salicylanilides from 4,5-dihalogenated salicylic acids: Synthesis, antimicrobial activity and cytotoxicity. |
| AID1331302 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 45 days | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2 | Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold. |
| AID1609018 | Selectivity index, ratio of IC50 for human HepG2 cells to MIC for antimycobacterial activity against Mycobacterium kansasii 6509/96 | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds. |
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| AID1576555 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in medium containing 7H9/DPPC/ cholesterol/BSA/Tyloxapol assessed as reduction in bacterial growth incubated for 14 days by Alamar blue reagent based assay | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Dual-target inhibitors of mycobacterial aminoacyl-tRNA synthetases among |
| AID1402131 | Antimycobacterial activity against Mycobacterium avium complex CIT19/06 clinical isolate after 5 days by Alamar Blue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Primaquine hybrids as promising antimycobacterial and antimalarial agents. |
| AID1819098 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 3 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay | 2022 | ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1 | Structural Rigidification of |
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| AID1403710 | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 25 uM after 48 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors. |
| AID376995 | Antimicrobial activity against isoniazid-resistant Mycobacterium tuberculosis isolate by alamar blue assay | 2006 | Journal of natural products, May, Volume: 69, Issue:5 | Aegicerin, the first oleanane triterpene with wide-ranging antimycobacterial activity, isolated from Clavija procera. |
| AID1166624 | Antitubercular activity against Mycobacterium tuberculosis ATCC 27294 in high iron condition after 5 days by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21 | Synthesis, characterization, molecular docking and anti-tubercular activity of Plumbagin-Isoniazid Analog and its β-cyclodextrin conjugate. |
| AID634540 | Antimycobacterial activity against clinical isolate of Mycobacterium tuberculosis TN675 assessed as intracellular ATP level after 5 days by luminescence assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis. |
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| AID1063985 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv My 331/88 after 21 days | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity. |
| AID721565 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv CNCTC My 331/88 after 10 to 14 days by microdilution panel method | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Synthesis and antimycobacterial evaluation of pyrazinamide derivatives with benzylamino substitution. |
| AID1329995 | Cytotoxicity against African green monkey Vero cells assessed as reduction cell survival rate after 72 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis. |
| AID1143272 | Antimycobacterial activity against Mycobacterium tuberculosis overexpressing DprE1 assessed as growth inhibition by resazurin assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
| AID1289091 | AUC in healthy Chinese subject (8 subjects) with homozygous wild type NAT2 genotype at 300 mg, po administered after overnight fast by HPLC method | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1483731 | Selectivity ratio of MIC for Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-c D28N mutant supplemented with 8 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione to MIC for Mycobacterium tuberculosis H | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis. |
| AID1143276 | Antimycobacterial activity against 3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one-resistant Mycobacterium tuberculosis clone 8.2 assessed as growth inhibition by resazurin assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
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| AID1639212 | Inhibition of Escherichia coli DNA gyrase assessed as reduction in enzyme-mediated supercoiling of relaxed pBR322 DNA measured after 60 mins by electrophoresis method | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Discovery and development of novel rhodanine derivatives targeting enoyl-acyl carrier protein reductase. |
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| AID326167 | Antimalarial activity against Plasmodium falciparum 3D7 with pLN-hrp3-katG-V5 insertion at attB site | 2007 | The Journal of biological chemistry, Aug-31, Volume: 282, Issue:35 | X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. |
| AID476929 | Human intestinal absorption in po dosed human | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Neural computational prediction of oral drug absorption based on CODES 2D descriptors. |
| AID1381953 | Genotoxicity in Salmonella typhimurium TA100 assessed as increase in revertant colonies at 50 uM preincubated for 20 mins followed by addition of top agar and minimal agar and measured after 72 hrs in absence of S9 metabolic activation system by Ames test | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity. |
| AID571679 | Half life in BALB/c mouse serum at 4 to 5 mg/kg administered as inhalable bolus dose by HPLC | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice. |
| AID1825034 | Selectivity index ratio of MIC90 in Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST-Fe media to Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST media | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition. |
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| AID289152 | Antimycobacterial activity against streptomycin, isoniazid, ethambutol-resistant Mycobacterium tuberculosis CIBIN 112 isolates | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines. |
| AID445285 | Antibacterial activity against Mycobacterium bovis BCG str. Tokyo 172 by broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis. |
| AID1178140 | Cytotoxicity against mouse J774A1 cells after 24 hrs by neutral red dye uptake assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 2,4-Dialkyl-8,9,10,11-tetrahydrobenzo[g]pyrimido[4,5-c]isoquinoline-1,3,7,12(2H,4H)-tetraones as new leads against Mycobacterium tuberculosis. |
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| AID754937 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 14 days by microdilution method | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Synthesis and antimycobacterial evaluation of N-substituted 5-chloropyrazine-2-carboxamides. |
| AID144574 | The compound was tested for its ability to inhibit the growth of Mycobacterium tuberculosis strain H6/99; Resistant | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10 | Antimycobacterial activity of ionic fullerene derivatives. |
| AID494207 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 24 hrs after 4 weeks | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv. |
| AID765270 | AUC/MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID574810 | Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 horboring rpoB D516V, katG S315T/R463L, gyrA D94G/S95T/R128S/Y129C, rrs A1401G by CLSI method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID1333153 | Induction of membrane damage in CI/DOPG/DOPI large unilamellar vesicles assessed as calcein leakage at compound to lipid ratio of 1:2 to 1:8 by fluorescence based total phosphorous determination assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties. |
| AID1488485 | Selectivity index, ratio of CC50 for Swiss mouse BMDM to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents. |
| AID325111 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 0.1 ug/ml after 4 weeks by BACTED460 method | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1287438 | Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis H37Rv clinical isolate 6 harboring InhA promoter C-15T mutant | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold. |
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| AID545252 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 14 days by micromethod | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | New amino acid esters of salicylanilides active against MDR-TB and other microbes. |
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| AID1743942 | Antitubercular activity against Mycobacterium tuberculosis resistant mutants generated by plating on 7H11/0ADC agar plates in presence of 3.75 to 15 uM 2-((3,5-Dinitrobenzyl)thio)quinazolin-4(3H)-one followed by sensitivity testing | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | 2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F |
| AID733456 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Hybrid furoxanyl N-acylhydrazone derivatives as hits for the development of neglected diseases drug candidates. |
| AID1058225 | Antimycobacterial activity against Mycobacterium chelonae | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis. |
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| AID569259 | Antimycobacterial activity against Mycobacterium avium subsp. avium ATCC 2529I | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3 | Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives. |
| AID1296376 | Antimycobacterial activity against Mycobacterium kansasii CNCTC My 6509/96 after 14 days by microdilution method | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis. |
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| AID775978 | Inhibition of Mycobacterium tuberculosis pantothenate synthetase cloned in Escherichia coli BL21 (DE3) using ATP, beta-alanine, pantoic acid as substrate assessed as NAD+ production at 100 uM measured every 12 secs for 120 secs by spectrophotometric analy | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors. |
| AID1338198 | Antimycobacterial activity against GFP-fused Mycobacterium tuberculosis H37Rv infected in macrophages | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and structure-activity studies of side chain analogues of the anti-tubercular agent, Q203. |
| AID1484381 | Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate 35829 by broth dilution method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Isoniazid derivatives and their anti-tubercular activity. |
| AID1292672 | Drug excretion in human subject slow inactivator assessed as total isonicotinoyl compound level in urine at 681 mg, iv infused at constant rate 5.4 min measured 276.3 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
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| 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). |
| AID725312 | Inhibition of human Flag-tagged LEDGF interaction to His6-tagged HIV1 integrase expressed in Escherichia coli BL21 (DE3) at 1000 uM preincubated for 20 mins measured after 1 hr by AlphaScreen proximity luminescent assay | 2013 | Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4 | Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions. |
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| AID1194330 | Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors. |
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| AID1767895 | Toxicity in BALB/c mouse infected with Mycobacterium tuberculosis H37Rv assessed as body weight at 25 mg/kg, po via gavage administered for 3 weeks starting from day 10 post infection and administered 5 times a week (Rvb = 24.59 +/- 0.61 g) | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis. |
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| AID1609013 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after overnight incubation by MTT assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds. |
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| AID344013 | Antitubercular activity against Mycobacterium bovis BCG under aerobic condition after 7 days by MTT method | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Halicyclamine A, a marine spongean alkaloid as a lead for anti-tuberculosis agent. |
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| AID1491511 | Genotoxicity in Salmonella typhimurium TA104 harboring Pr1 lux operon fusion at 1.28 to 128 uM measured every 5 mins for 4 hrs in absence of S9 liver fraction by vitotox assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones. |
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| AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3 | Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
| AID529521 | Antimycobacterial activity against ethambutol-susceptible and rifampin-resistant Mycobacterium tuberculosis isolate NJT30167 expressing embB codon 306 ATG assessed as bacterial growth rate at sub MIC compound concentration by radiometric Bactec 460TB meth | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. |
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| AID1402130 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 after 7 days by Alamar Blue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Primaquine hybrids as promising antimycobacterial and antimalarial agents. |
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| AID1732051 | Antibacterial activity against Mycobacterium smegmatis mc2155 | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Discovery of novel N |
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| AID683325 | Antifungal activity against Candida albicans ATCC 10231 by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776. |
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| AID1246807 | Antimycobacterial activity against Mycobacterium tuberculosis TN1037 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1772572 | Antimycobacterial activity against drug resistant Mycobacterium avium 330/88 assessed as minimal inhibitory concentration required for complete inhibition of mycobacterial growth incubated for 14 days | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Design and synthesis of 2-(2-isonicotinoylhydrazineylidene)propanamides as InhA inhibitors with high antitubercular activity. |
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| AID1143485 | Antitubercular activity against katG-deficient isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 by BACTEC 960 assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity. |
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
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| AID1058223 | Antimycobacterial activity against Mycobacterium avium | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis. |
| AID780668 | Cytotoxicity against African green monkey Vero C1008 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Rational drug design based synthesis of novel arylquinolines as anti-tuberculosis agents. |
| AID1061100 | Antimicrobial activity against Candida albicans | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | A novel indigoid anti-tuberculosis agent. |
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| AID404975 | Antimicrobial activity against Mycobacterium tuberculosis H37Ra assessed as early bactericidal activity | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Isoniazid bactericidal activity and resistance emergence: integrating pharmacodynamics and pharmacogenomics to predict efficacy in different ethnic populations. |
| AID1323727 | Inhibition of Mycobacterium tuberculosis H37Ra infected in human THP1 cells assessed as reduction in surviving bacteria at 1 ug/ml after 7 days by serial dilution method | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents. |
| AID445331 | Cytotoxicity against human MRC5 cells | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis. |
| AID465572 | Cytotoxicity against african green monkey Vero C1008 cells assessed as cell viability at 2000 ug/ml after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Novel molecular hybrids of cinnamic acids and guanylhydrazones as potential antitubercular agents. |
| AID625338 | Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis by two fold serial dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues. |
| AID1603255 | Antibacterial activity against Mycobacterium tuberculosis H37Rv harboring LuxAB incubated for 10 days under anaerobic conditions followed by incubation under aerobic conditions for 28 hrs by LORA method | |||
| AID495474 | Antimicrobial activity against Mycobacterium tuberculosis NJT210TCC harboring embB406 GGC-TCC(Gly-Ser) mutation in embB gene after 4 weeks | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 | Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis. |
| AID576926 | Antimicrobial activity against Mycobacterium smegmatis MC2 5072 overexpressing dhfr gene assessed as growth inhibition at 120 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID1154327 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by standard microdilution method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | 4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity. |
| AID625696 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 isolate after 7 days | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | New series of isoniazid hydrazones linked with electron-withdrawing substituents. |
| AID623581 | Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 22 hrs by microbroth dilution antibiotic susceptibility assay | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | One-pot syntheses of pseudopteroxazoles from pseudopterosins: a rapid route to non-natural congeners with improved antimicrobial activity. |
| AID1173784 | Inhibition of Mycobacterium tuberculosis DNA gyrase using relaxed pBR322 as substrate after 30 mins by supercoiling assay | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 | An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition. |
| AID1193495 | Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID1246819 | Antimycobacterial activity against Mycobacterium tuberculosis W4 after 5 days by spectrophotometry | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1292713 | Drug excretion in human subject rapid inactivator assessed as total isonicotinoyl compound level in urine at 670 mg, iv infused at constant rate 5.2min measured 335 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID571670 | Elimination rate constant in human THP1 cells at 3 ug/ml after 10 mins by HPLC | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice. |
| AID1242345 | Antimycobacterial activity against 1-(2-(4-((5-chloro-6-methylpyridin-3-yl)methylamino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA D89N mutant incubated for 7 days by microdilu | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding. |
| AID1585522 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as reduction in bacterial load in lungs at 10 mg/kg, po administered once daily via gavage for 5 consecutive days per week for 2 weeks | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Benzofuran derivatives and their anti-tubercular, anti-bacterial activities. |
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| AID373113 | Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 7 days by micromethod | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Preparation and in vitro evaluation of benzylsulfanyl benzoxazole derivatives as potential antituberculosis agents. |
| AID1129650 | Cytotoxicity against mouse J774A1 cells assessed as cell viability after 24 hrs by Trypan blue exclusion assay | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | 1,2,3,4,8,9,10,11-octahydrobenzo[j]phenanthridine-7,12-diones as new leads against Mycobacterium tuberculosis. |
| AID316444 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation. |
| AID303471 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected CD1 mouse assessed as spleen bacterial count at 25 mg/kg, ip after 35 days post infection | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid. |
| AID408343 | Antibacterial activity against Mycobacterium smegmatis ATCC 14468 assessed as inhibition zone diameter at 500 mg/mL after 24 hrs by Kirby-Bauer disk diffusion assay | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis of methyl 5-S-alkyl-5-thio-D-arabinofuranosides and evaluation of their antimycobacterial activity. |
| AID1491401 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 7 days by rapid direct susceptibility test | |||
| AID1193920 | Inhibition of Mycobacterium tuberculosis DNA GyrA/B heterotetramer assessed as inhibition of pBR322 supercoiling after 30 mins by gel electrophoresis | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain. |
| AID609619 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues. |
| AID1129654 | Antimycobacterial activity against Mycobacterium tuberculosis Beijing 17919 expressing luciferase assessed as growth inhibition after 6 days by luminometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | 1,2,3,4,8,9,10,11-octahydrobenzo[j]phenanthridine-7,12-diones as new leads against Mycobacterium tuberculosis. |
| AID566040 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assat | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Synthesis and in vitro antimycobacterial activity of 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives. |
| AID1196885 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors. |
| AID1287508 | Selectivity index, ratio of GI50 for human HeLa cells to MIC for dormant state Mycobacterium bovis BCG ATCC 35734 | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents. |
| AID775853 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition by micro plate alamar blue assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21 | Studies on substituted benzo[h]quinazolines, benzo[g]indazoles, pyrazoles, 2,6-diarylpyridines as anti-tubercular agents. |
| AID1292616 | Drug excretion in human rapid inactivators urine assessed as total isonicotinoyl compounds at 1 g, iv by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1154547 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 Rv1937/F426C mutant assessed as growth inhibition after 5 days by microdilution method | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Lead optimization of 1,4-azaindoles as antimycobacterial agents. |
| AID1180392 | Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 50 uM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Identification and development of 2-methylimidazo[1,2-a]pyridine-3-carboxamides as Mycobacterium tuberculosis pantothenate synthetase inhibitors. |
| AID1756862 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC27294 incubated for 7 days by microplate alamar blue assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Antitubercular properties of thiazolidin-4-ones - A review. |
| AID1174122 | Antimicrobial activity against Mycobacterium tuberculosis Spec. 210 by two-fold serial dilution method | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Synthesis and evaluation of in vitro antimycobacterial activity of novel 1H-benzo[d]imidazole derivatives and analogues. |
| AID1183263 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of colony formation at 250 ug/ml after 4 weeks of incubation | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening. |
| AID325143 | Antimicrobial activity against Mycobacterium tuberculosis TB20 isolate at 0.4 ug/ml after 4 weeks | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis. |
| AID1608996 | Antimycobacterial activity against Mycobacterium kansasii 235/80 after 21 days | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds. |
| AID285162 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID1337096 | Irreversible inhibition of MPO (unknown origin) | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | From Dynamic Combinatorial Chemistry to |
| AID1854286 | Antitubercular activity against clinical isolate streptomycin-resistant Mycobacterium tuberculosis ATCC 35820 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant |
| AID494996 | Hepatotoxicity in po dosed rat assessed as effect on serum SGPT level (Rvb = 32.46 +/- 0.76 U/mL) | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid. |
| AID649898 | Antimycobacterial activity against Mycobacterium kansasii 235/80 after 7 days | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold. |
| AID325852 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids. |
| AID1627191 | Selectivity ratio of IC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 27294 | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Preparation, biological evaluation and molecular docking study of imidazolyl dihydropyrimidines as potential Mycobacterium tuberculosis dihydrofolate reductase inhibitors. |
| AID1570245 | Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 1 incubated for 7 days by rapid direct susceptibility test | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. |
| AID1692252 | Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16883 clinical isolate assessed as inhibition of bacterial growth incubated for 7 days by MABA assay | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Identification of benzothiazinones containing 2-benzyl-2,7-diazaspiro[3.5]nonane moieties as new antitubercular agents. |
| AID457889 | Antimycobacterial activity against Mycobacterium tuberculosis 331/88 after 21 days by micromethod | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains. |
| AID1174112 | Antimycobacterial activity against isoniazid, rifampin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis. |
| AID509438 | Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic katG299 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China. |
| AID1582588 | Resistance factor, ratio of MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv over expressing InhA to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv transfected with pMV261 empty vector | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Synthesis and Structure-Activity Relationship Studies of C2-Modified Analogs of the Antimycobacterial Natural Product Pyridomycin. |
| AID717304 | Antitubercular activity against streptomycin, isoniazid, rifampicin,ethambutol-resistant Mycobacterium tuberculosis clinical isolate assessed as reduction in RLU at 0.5 ug/mL after 72 hrs by luciferase reporter phage assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Microwave-assisted synthesis, molecular docking and antitubercular activity of 1,2,3,4-tetrahydropyrimidine-5-carbonitrile derivatives. |
| AID1401977 | Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv RIF-R1 harboring rpoB S522L mutant | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes. |
| AID458160 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 7357/98 after 14 days by micromethod | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains. |
| AID1246802 | Cytotoxicity against hamster BHK21 cells after 3 days | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Linked pyridinyl-thiadiazoles: Design and synthesis as potential candidate for treatment of XDR and MDR tuberculosis. |
| AID1289088 | Drug metabolism in plasma of healthy Chinese subject (8 subjects) with heterozygous mutant of NAT2 genotype assessed as N-acetylisoniazid formation by measuring ratio of N-acetylisoniazid to isoniazid at 300 mg, po administered after overnight fast measur | 2011 | Drug metabolism and drug interactions, , Volume: 26, Issue:3 | Gene dose effect of NAT2 variants on the pharmacokinetics of isoniazid and acetylisoniazid in healthy Chinese subjects. |
| AID1687559 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 assessed as inhibition of microbial growth by classical test tube method | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents. |
| AID326164 | Antimalarial activity against Plasmodium falciparum Dd2 with pLN-hrp3-katG-V5 insertion at attB site | 2007 | The Journal of biological chemistry, Aug-31, Volume: 282, Issue:35 | X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. |
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| AID1400064 | Bactericidal activity against non-replicating Mycobacterium tuberculosis CDC1551 expressing tdTomato infected in mouse J774A.1 cells at 2 times MIC up to 72 hrs by UV-Visible spectroscopic method | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | An antimycobacterial pleuromutilin analogue effective against dormant bacilli. |
| AID183969 | Brain mitochondrial activity measured at 120 min of incubation at 1 uM concentration | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids. |
| AID644431 | Antibacterial activity against Mycobacterium tuberculosis H37Rv harboring pSMT1 encoding Vibrio harveyi luxAB gene at 10 uM after 7 days by luminometric analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | 1,4-diarylpiperazines and analogs as anti-tubercular agents: synthesis and biological evaluation. |
| AID1585121 | Antimicrobial activity against multi drug-resistant Mycobacterium tuberculosis 14231 after 7 days by MABA | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones. |
| AID1183298 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives. |
| AID1463962 | Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 8666/2010 incubated for 14 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents. |
| AID609928 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 30 days by agar microdilution method | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis, molecular modeling and bio-evaluation of cycloalkyl fused 2-aminopyrimidines as antitubercular and antidiabetic agents. |
| AID1577337 | Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 7357/1998 after 21 days | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase. |
| AID373112 | Antimycobacterial activity against Mycobacterium tuberculosis CNCTC My 331/88 after 21 days by micromethod | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Preparation and in vitro evaluation of benzylsulfanyl benzoxazole derivatives as potential antituberculosis agents. |
| AID1401980 | Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis H37Rv FQ-R1 harboring unidentified mutation | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes. |
| AID353151 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth index at 6.25 ug/mL after 7 days by radiometric method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Design, synthesis, biological evaluation and molecular modelling studies of novel quinoline derivatives against Mycobacterium tuberculosis. |
| AID373116 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 7 days by micromethod | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Preparation and in vitro evaluation of benzylsulfanyl benzoxazole derivatives as potential antituberculosis agents. |
| AID1158121 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as lung bacterial load at 15 mg/kg administered 3 weeks after infection via oral gavage for 28 days, five times per week measured per lung (Rvb = 7.24 +/ | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1224511 | Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 7 days by micromethod | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | 1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria. |
| AID1224745 | Antitubercular activity against Mycobacterium tuberculosis H37Rv | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Ultrasound-assisted one-pot four-component synthesis of novel 2-amino-3-cyanopyridine derivatives bearing 5-imidazopyrazole scaffold and their biological broadcast. |
| AID1602080 | Antibacterial activity against Escherichia coli ATCC 25922 measured after overnight incubation | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Design, synthesis and anti-bacterial studies of piperazine derivatives against drug resistant bacteria. |
| AID774293 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS-PMS assay | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID1721019 | Antitubercular activity against Mycobacterium tuberculosis isolate 12525 incubated for 7 days by microplate alamar blue assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1736312 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis. |
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| AID1292705 | Drug excretion in human subject rapid inactivator assessed as total isonicotinoyl compound level in urine at 670 mg, iv infused at constant rate 5.2min measured 62 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID353150 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth index at 6.25 ug/mL after 6 days by radiometric method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Design, synthesis, biological evaluation and molecular modelling studies of novel quinoline derivatives against Mycobacterium tuberculosis. |
| AID344014 | Antitubercular activity against Mycobacterium bovis BCG under hypoxic condition after 14 days by MTT method | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Halicyclamine A, a marine spongean alkaloid as a lead for anti-tuberculosis agent. |
| AID1463958 | Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 131 incubated for 14 days by micromethod | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents. |
| AID1632662 | Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra ATCC 25177 after 12 days by XTT reduction menadione assay | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8 | Synthesis and Antitubercular Activity of New Benzo[b]thiophenes. |
| AID1055954 | Antimycobacterial activity against capreomycin-resistant Mycobacterium tuberculosis under normoxic condition after 7 days by MABA assay | 2013 | Journal of natural products, Nov-22, Volume: 76, Issue:11 | Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain. |
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| AID1191521 | Cytostatic activity against human HepG2 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Synthesis and in vitro biological evaluation of 2-(phenylcarbamoyl)phenyl 4-substituted benzoates. |
| AID143115 | In vitro anti-mycobacterial activity against pirazynamide resistant Mycobacterium tuberculosis ATCC 35828 determined by the MTT method | 2004 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6 | Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480. |
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| AID1292665 | Drug excretion in human subject slow inactivator assessed as total isonicotinoyl compound level in urine at 681 mg, iv infused at constant rate 5.4 min measured 59.1 mins after start of drug injection by colorimetry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID292293 | Antibacterial activity against Staphylococcus aureus ATCC 25923 after 16 to 20 hrs by broth microdilution method | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs. |
| AID445332 | Selectivity for Mycobacterium tuberculosis H37Rv over human THP1 cells | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis. |
| AID1292697 | Drug excretion in human subject rapid inactivator assessed as sum of isoniazid plus hydrazones, acetylisoniazid, isonicotinic acid and isonicotinuric acid level in urine at 670 mg, iv infused at constant rate 5.2min measured 335 mins after start of drug i | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID1585120 | Antimicrobial activity against multi drug-resistant Mycobacterium tuberculosis 12611 after 7 days by MABA | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones. |
| AID1760640 | Antibacterial activity against Mycobacterium tuberculosis H37Ra ATCC2517 assessed as inhibition of bacterial growth measured after 17 hrs by resazurin based flourimetric assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synthesis and structure-activity studies of novel anhydrohexitol-based Leucyl-tRNA synthetase inhibitors. |
| AID1546639 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial population at 10 ug/ml under starvation condition after 7 days by MPN assay | 2020 | Journal of natural products, 01-24, Volume: 83, Issue:1 | Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents. |
| AID1126674 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of colony formation at 250 ug/mL after 2 to 4 weeks by Lowensteine-Jensen method relative to control | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis, characterization and pharmacological screening of some novel 5-imidazopyrazole incorporated polyhydroquinoline derivatives. |
| AID1296082 | Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis isolate MDR1 assessed as inhibition of mycobacterial growth incubated for 9 days | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul |
| AID609620 | Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis by agar dilution method | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues. |
| AID774606 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene assessed as growth inhibition at 10 uM after 6 days by luminometry relative to control | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine. |
| AID1372628 | Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week in presence of efflux pump inhibitor verapamil by MABA | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Lead identification and optimization of bacterial glutamate racemase inhibitors. |
| AID1484380 | Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate 1889 by broth dilution method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Isoniazid derivatives and their anti-tubercular activity. |
| AID1296092 | Inhibition of multidrug resistance efflux pump in Mycobacterium aurum ATCC 23366 assessed as inhibition of ethidium bromide efflux by measuring relative fluorescence units for ethidium bromide accumulation at 1/4 times MIC incubated for 60 mins by fluorim | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul |
| AID1143277 | Antimycobacterial activity against 3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one-resistant Mycobacterium tuberculosis clone 8.3 assessed as growth inhibition by resazurin assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity. |
| AID1125149 | Cytotoxicity against mouse J774A1 cells after 24 hrs by neutral red dye uptake assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Anti-mycobacterial activity of 1,3-diaryltriazenes. |
| AID538838 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 30 days by agar microdilution method | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Synthesis and bio-evaluation of alkylaminoaryl phenyl cyclopropyl methanones as antitubercular and antimalarial agents. |
| AID319147 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections. |
| AID616791 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in Swiss mouse assessed as inhibition of viable bacterial counts in lungs at 25 mg/kg, po for 28 days measured on day 30 post infection | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Novel aryloxy azolyl chalcones with potent activity against Mycobacterium tuberculosis H37Rv. |
| AID1654158 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth after 7 days by alamar blue assay | 2020 | Journal of natural products, 03-27, Volume: 83, Issue:3 | Antimycobacterial Rufomycin Analogues from |
| AID1491507 | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 24 hrs by neutral red uptake assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones. |
| AID1514448 | Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety. |
| AID369302 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN1040 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID576904 | Antimicrobial activity against Mycobacterium smegmatis MC2 4517 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid. |
| AID1296090 | Selectivity index, ratio of GIC50 for cytotoxicity against mouse RAW264.7 cells to MIC for Mycobacterium tuberculosis H37Rv ATTC 27294 | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul |
| AID427284 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by microdilution resazurin assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Antimycobacterial activity of new 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-one derivatives. Molecular modeling investigations. |
| AID1739877 | Antimycobacterial activity against isoniazid/rifampicin/ethambutol/streptomycin/ofloxacin/para-aminosalicylic acid/prothionamide multidrug-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth under 7H9 medium condition after 7 t | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Development of small-molecule inhibitors of fatty acyl-AMP and fatty acyl-CoA ligases in Mycobacterium tuberculosis. |
| AID325871 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in spleen at 25 mg/kg, ip after 10 days | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids. |
| AID1460597 | Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv | 2017 | Bioorganic & medicinal chemistry, 11-15, Volume: 25, Issue:22 | Anti-tuberculosis activity and structure-activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives. |
| AID529539 | Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 CTG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. |
| AID1292636 | Half life in human subject slow inactivator at 681 mg, iv infused at constant rate over 5.4 mins by spectrophotometry | 1974 | Journal of pharmaceutical sciences, Aug, Volume: 63, Issue:8 | Determination of isoniazid and metabolites in biological fluids. |
| AID487838 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 48 hrs by green fluorescent protein-based assay | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives. |
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| AID1819097 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 4 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay | 2022 | ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1 | Structural Rigidification of |
| AID1395195 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC27395 after 7 days by Alamar blue assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety. |
| AID1585771 | Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv after 5 days under hypoxic condition by resazurin dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
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| AID1706090 | Antimycobacterial activity against non-replicating Mycobacterium tuberculosis H37Rv expressing pFCA-LuxAB assessed as bacterial growth inhibition incubated for 10 days under anerobic condition by low oxygen recovery assay | |||
| AID487843 | Antimycobacterial activity against Mycobacterium intracellular after 48 hrs by microtiter plate method | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives. |
| AID1393800 | Antitubercular activity against Mycobacterium tuberculosis H37Rv after 21 days by broth dilution assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Fluoroquinolone derivatives and their anti-tubercular activities. |
| AID1224516 | Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 21 days by micromethod | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | 1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria. |
| AID1333143 | Induction of membrane disruption in Mycobacterium bovis BCG ATCC 35734 at 60 uM up to 3 hrs by Sytox green uptake assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties. |
| AID1149233 | Antibacterial activity against Mycobacterium tuberculosis assessed as growth inhibition in presence of 16 uM nicotinic acid hydrazide | 1976 | Journal of medicinal chemistry, Apr, Volume: 19, Issue:4 | Mode of action and quantitative structure-activity correlations of tuberculostatic drugs of the isonicotinic acid hydrazide type. |
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| AID1360449 | Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate CDCT16 harboring rpoB/katG/inhA mutant gene after 7 days by resazurin dye based assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | 1H-Benzo[d]imidazoles and 3,4-dihydroquinazolin-4-ones: Design, synthesis and antitubercular activity. |
| AID1476353 | Antitubercular activity against dormant stage Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days in anaerobic condition followed by incubation for 28 hrs in ambient gaseous condition measured after day 11 by two fold serial dilution assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity. |
| AID364834 | Antibacterial activity against Mycobacterium smegmatis ATCC 14468 assessed as zone of inhibition diameter at 1 mg/mL after 48 hrs by Kirby-Bauer disk diffusion assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | Synthesis of triazole-oxazolidinones via a one-pot reaction and evaluation of their antimicrobial activity. |
| AID1499663 | Antimycobacterial activity against Mycobacterium tuberculosis RCMB 010126 clinical isolate after 7 days by MABA | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and 2D QSAR study of novel pyridine and quinolone hydrazone derivatives as potential antimicrobial and antitubercular agents. |
| AID529537 | Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 ATC-ATG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. |
| AID1326671 | Inhibition of Mycobacterium tuberculosis DNA gyrase subunit A2B2 supercoiling activity using relaxed pBR322 as substrate after 30 mins in presence of ATP by agarose gel electrophoresis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors. |
| AID617280 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by Microplate Alamar blue assay | 2011 | Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17 | Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain. |
| AID642349 | Binding affinity to chicken blood dsDNA at pH 7.4 by UV-spectroscopy | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Electrochemical and spectroscopic investigations of isoniazide and its analogs with ds.DNA at physiological pH: evaluation of biological activities. |
| AID1736314 | Antitubercular activity against INH, SM, RFP, EMB, PAS, Prothionamide 1321, Capreomycin-resistant Mycobacterium tuberculosis 14862 assessed as inhibition of bacterial growth | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis. |
| AID1593908 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as complete inhibition of bacterial growth incubated for 7 days by rapid direct susceptibility test | |||
| AID1064525 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv CNCTC My 331/88 after 5 days by microplate alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Alkylamino derivatives of pyrazinamide: synthesis and antimycobacterial evaluation. |
| AID499895 | Antitubercular activity against Mycobacterium bovis BCG at 1 ug/ml after 6 days by microplate alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Inhibition of mycobacterial replication by pyrimidines possessing various C-5 functionalities and related 2'-deoxynucleoside analogues using in vitro and in vivo models. |
| AID1392551 | Antimycobacterial activity against Mycobacterium bovis BCG harboring pATB45::inhA after 48 hrs by resazurin microtiter assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis, antimycobacterial activity and influence on mycobacterial InhA and PknB of 12-membered cyclodepsipeptides. |
| AID1191526 | Selectivity index, ratio of IC50 for human HepG2 cells to MIC for Mycobacterium kansasii 6509/96 | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Synthesis and in vitro biological evaluation of 2-(phenylcarbamoyl)phenyl 4-substituted benzoates. |
| AID644435 | Cytotoxicity against human HepG2/C3A cells after 24 hrs by neutral red assay | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | 1,4-diarylpiperazines and analogs as anti-tubercular agents: synthesis and biological evaluation. |
| AID1879692 | Antimycobacterial activity against PAS resistant Mycobacterium tuberculosis H37Rv harboring E153A mutant assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS). |
| AID1736704 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | 4-Substituted picolinohydrazonamides as a new class of potential antitubercular agents. |
| AID1646902 | Antimycobacterial activity against Mycobacterium tuberculosis BRF57 harbouring KatG Ser315Thr mutant and wild type InhA assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and anti-Mycobacterium tuberculosis activity of imide-β-carboline and carbomethoxy-β-carboline derivatives. |
| AID1287511 | Selectivity index, ratio of GI50 for human PANC1 cells to MIC for active state Mycobacterium bovis BCG ATCC 35734 | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents. |
| AID1365704 | Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv RIF-R1 harboring rpoB S522L mutant after 5 days | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
| AID1224510 | Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 21 days by micromethod | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | 1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria. |
| AID569261 | Antimicrobial activity against methicillin-resistant Staphylococcus aureus 873 | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3 | Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| 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. |
| AID1802950 | ICL Enzyme Assay from Article 10.3109/14756360903425221: \\5-Nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides: synthesis, in vitro antimycobacterial activity, cytotoxicity, and isocitrate lyase inhibition studies.\\ | 2010 | Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 25, Issue:6 | 5-Nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides: synthesis, in vitro antimycobacterial activity, cytotoxicity, and isocitrate lyase inhibition studies. |
| AID1801344 | Fluorescence-based Assay from Article 10.1021/acschembio.5b00452: \\Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).\\ | 2015 | ACS chemical biology, Oct-16, Volume: 10, Issue:10 | Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1). |
| AID1802256 | MymA Inhibition Assay from Article 10.1111/cbdd.12840: \\Characterization of MymA protein as a flavin-containing monooxygenase and as a target of isoniazid.\\ | 2017 | Chemical biology & drug design, Jan, Volume: 89, Issue:1 | Characterization of MymA protein as a flavin-containing monooxygenase and as a target of isoniazid. |
| AID1801343 | Gel-based Cleavage Assay from Article 10.1021/acschembio.5b00452: \\Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).\\ | 2015 | ACS chemical biology, Oct-16, Volume: 10, Issue:10 | Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1). |
| 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. |
| AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 10988 (54.83) | 18.7374 |
| 1990's | 1878 (9.37) | 18.2507 |
| 2000's | 2337 (11.66) | 29.6817 |
| 2010's | 3625 (18.09) | 24.3611 |
| 2020's | 1211 (6.04) | 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 (92.75) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 960 (4.40%) | 5.53% |
| Reviews | 1,083 (4.96%) | 6.00% |
| Case Studies | 1,742 (7.99%) | 4.05% |
| Observational | 77 (0.35%) | 0.25% |
| Other | 17,953 (82.30%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Comparison of Two Strategies for Therapeutic Decision-making in Tuberculosis Contact Tracing: a Standard Strategy Based on Tuberculin Skin Test (TST) Alone vs TST Combined With QuantiFERON®-TB Gold In-Tube (QFT-IT) [NCT01223534] | Phase 4 | 871 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| Optimizing Antituberculosis Therapy in Adults With Tuberculous Meningitis Based on N-Acetyltransferase Type 2 Genotyping [NCT03787940] | 676 participants (Anticipated) | Interventional | 2019-03-04 | Recruiting | |||
| Efficacy of Risk-Targeted Video Based Directly on Observed Therapy for Latent TB [NCT03783728] | 0 participants (Actual) | Observational | 2019-06-30 | Withdrawn(stopped due to Investigator is leaving the University) | |||
| Short Course Rifapentine and Isoniazid for the Preventive Treatment of Tuberculosis(SCRIPT-TB) [NCT03900858] | 566 participants (Anticipated) | Interventional | 2018-12-01 | Recruiting | |||
| Six Weeks of Daily Rifapentine vs. a Comparator Arm of 12-16 Week Rifamycin-based Treatment of Latent M. Tuberculosis Infection: Assessment of Safety, Tolerability and Effectiveness [NCT03474029] | Phase 2/Phase 3 | 3,400 participants (Anticipated) | Interventional | 2019-08-01 | Recruiting | ||
| Preventing Mycobacterium Tuberculosis Infection in HIV-Exposed Infants [NCT02613169] | Phase 2 | 300 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
| Studying the Blood Levels of First-line Anti-tuberculosis Drugs in Relation to Treatment Outcomes Among Newly Diagnosed Adults With Pulmonary Tuberculosis on the Thai-Myanmar Border [NCT02457208] | Phase 1 | 61 participants (Actual) | Interventional | 2015-07-07 | Completed | ||
| Clinical Trial to Investigate the Appropriate Dose of Isoniazid According to NAT2 Polymorphism Status in Korean Subjects [NCT03665402] | 16 participants (Actual) | Interventional | 2018-05-13 | Completed | |||
| Open Label, Single Center, Phase 1 Dose Escalation and Extension Trial to Evaluate Safety and Tolerability of Chlorquine as Adjuvant Drug to Standard 4-drug Anti-tuberculosis Therapy in Healthy Volunteers [NCT05443178] | Phase 1 | 16 participants (Anticipated) | Interventional | 2022-01-04 | Recruiting | ||
| A Randomized, Double-Blind, Active Drug Controlled Study to Assess the Efficacy of HUEXC030 as Add-on Excipient to Eradicate Anti-Tuberculosis Drugs Induced Liver Injury in Subjects With Pulmonary Tuberculosis [NCT02467608] | Phase 2/Phase 3 | 557 participants (Actual) | Interventional | 2012-12-06 | Completed | ||
| A Phase II Trial to Describe the Pharmacokinetics, Safety and Efficacy of Pharmacogenetics-guided Dosing of Isoniazid in Patients With HIV-associated TB [NCT05124678] | Phase 2 | 40 participants (Anticipated) | Interventional | 2021-12-07 | Recruiting | ||
| The Prophylaxis of Tuberculosis According to TSPOT Results After Kidney Transplantation (PTTKT):Protocol for an Open-label, Prospective, Randomized, 3-arm, Controlled Trial [NCT05249699] | 303 participants (Anticipated) | Interventional | 2022-04-01 | Not yet recruiting | |||
| Addiction, HIV and Tuberculosis in Malaysian Criminal Justice Settings [NCT03089983] | 1,129 participants (Actual) | Interventional | 2017-08-21 | Active, not recruiting | |||
| A Prospective Study of Shortening the Duration of Standard Short Course Chemotherapy From 6 Months to 4 Months in HIV-non-infected Patients With Fully Drug-Susceptible, Non-cavitary Pulmonary Tuberculosis With Negative Sputum Cultures After 2 Months of An [NCT00130247] | Phase 3 | 394 participants (Actual) | Interventional | 2002-04-08 | Completed | ||
| Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240] | Early Phase 1 | 11 participants (Actual) | Interventional | 2014-03-06 | Terminated(stopped due to Not enough patient enrollment and lack of staffing) | ||
| STREAM: The Evaluation of a Standard Treatment Regimen of Anti-tuberculosis Drugs for Patients With MDR-TB [NCT02409290] | Phase 3 | 588 participants (Actual) | Interventional | 2016-03-31 | Completed | ||
| A Prospective, Randomized, Open Labeled Trial of Isoniazid Treatment Based on ELISPOT Assay to Prevent Tuberculosis in a Kidney Transplant Recipient [NCT01087190] | 831 participants (Actual) | Interventional | 2010-06-30 | Completed | |||
| Adjuvant Isonicotinic Acid Hydrazide (INH) Pretreatment With Misoprostol for Induction of Abortion in First-trimester Missed Miscarriage: A Randomized Controlled Trial [NCT04500002] | 240 participants (Anticipated) | Interventional | 2020-09-01 | Not yet recruiting | |||
| The Study of Standardized Preoperative Anti-tuberculosis Treatment of Surgical Treatment of Spinal Tuberculosis Patients [NCT02477852] | Phase 4 | 400 participants (Anticipated) | Interventional | 2015-04-30 | Recruiting | ||
| Randomized, Open Label, Multiple Dose Phase 2a Study of the Early Bactericidal Activity of AZD5847 in Adults With Pulmonary Tuberculosis [NCT01516203] | Phase 2 | 75 participants (Actual) | Interventional | 2012-12-05 | Completed | ||
| The Effect of Fermented Soybean Supplementation on the Body Weight and Physical Function of Tuberculosis Patients With Standard Therapy in Indonesia [NCT02554318] | 147 participants (Actual) | Interventional | 2013-11-30 | Completed | |||
| Population Pharmacokinetics of Anti-tuberculosis Drugs in Children With Tuberculosis [NCT03625739] | 800 participants (Anticipated) | Observational [Patient Registry] | 2018-07-01 | Recruiting | |||
| Systematic Empirical vs. Test-guided Anti-tuberculosis Treatment Impact in Severely Immunosuppressed HIV-infected Adults Initiating Antiretroviral Therapy With CD4 Cell Counts <100/mm3: the STATIS Randomized Controlled Trial [NCT02057796] | Phase 4 | 1,050 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| URBAN ARCH (3/5) Uganda Cohort TB Preventive Therapy for HIV-infected Alcohol Users in Uganda: an Evaluation of Safety Tolerability and Adherence [NCT03302299] | Phase 4 | 302 participants (Actual) | Interventional | 2017-04-07 | Completed | ||
| Pharmacokinetics of Anti-tuberculosis and Antiretroviral Drugs in Children [NCT03800381] | 92 participants (Anticipated) | Observational | 2019-01-28 | Recruiting | |||
| Primary Prophylaxis for Prevention of TB in Prison's Populations [NCT03028129] | Phase 4 | 467 participants (Actual) | Interventional | 2017-09-04 | Terminated(stopped due to Interim analysis showed efficacy less than 2.5%.) | ||
| A Seamless Phase 2B/C Platform Trial to Evaluate Multiple Regimens and Durations of Treatment in Pulmonary Tuberculosis [NCT06114628] | Phase 2 | 2,500 participants (Anticipated) | Interventional | 2023-12-08 | Not yet recruiting | ||
| Evaluation of the Impact of Diabetes Control on Transmission and Development of Tuberculosis in the General Population [NCT03498534] | Phase 4 | 0 participants (Actual) | Interventional | 2012-09-30 | Withdrawn(stopped due to Due to administrative procedures) | ||
| Brief Bactericidal Activity of Anti-Tuberculosis Drugs in Drug-Resistant Tuberculosis [NCT02236078] | Phase 1 | 18 participants (Actual) | Interventional | 2015-11-30 | Completed | ||
| Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289] | 1,578 participants (Actual) | Observational | 2003-06-09 | Completed | |||
| TB YOUTH - TB sYstemic Management Using One-month, Ultra-short TPT Regimen for scHool Contacts [NCT06022146] | Phase 3 | 3,520 participants (Anticipated) | Interventional | 2023-09-01 | Recruiting | ||
| A Randomized Double Blind Placebo Controlled Trial of Rifapentine and Isoniazid for Prevention of Tuberculosis in People With Diabetes [NCT04600167] | Phase 3 | 3,000 participants (Anticipated) | Interventional | 2022-06-17 | Recruiting | ||
| Characterization of Immune Responses in Treatment-induced Latency in Pulmonary Tuberculosis [NCT01154959] | Phase 3 | 120 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| Integral Research of the Managing and Treatment of the Infection With Human Immunodeficiency (VIH) /Human Immunodeficiency Syndrome(SIDA) Co-infection With Latent Tuberculosis Infection. A Multidisciplinary and Interinstitucional Approach [NCT01875952] | Phase 4 | 100 participants (Anticipated) | Interventional | 2010-05-31 | Active, not recruiting | ||
| Phase I Study of Whether Preclearance of Latent M. Tuberculosis (MTB) Infection With Isoniazid (INH) Enhances Specific Immune Responses to MTB Following Subsequent BCG Revaccination in Healthy, HIV-Uninfected, Tuberculin Skin Test Positive Adults [NCT01119521] | Phase 1 | 82 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| Vaginal Dinoprostone Versus Vaginal Isonicotinic Acid Hydrazide Prior to Diagnostic Office Hysteroscopy in Postmenopausal Patients: a Randomized Controlled Trial [NCT04500496] | 200 participants (Anticipated) | Interventional | 2020-09-01 | Recruiting | |||
| TBTC Study 31 PK/PD: Population Pharmacokinetic and Pharmacodynamic Study of Efficacy and Safety of High-Dose Rifapentine and Moxifloxacin for Treatment of Tuberculosis in the Study 31 Treatment Trial: Intensive PK Sampling [NCT02563327] | Phase 3 | 60 participants (Anticipated) | Interventional | 2016-05-30 | Recruiting | ||
| One-month Latent Tuberculosis Treatment for Renal Transplant Candidates [NCT05411744] | Phase 4 | 25 participants (Anticipated) | Interventional | 2022-07-01 | Recruiting | ||
| An International Multicentre Controlled Clinical Trial to Evaluate 1200mg and 1800mg Rifampicin Daily for Four Months in the Reduction of the Duration of Standard Treatment of Pulmonary Tuberculosis [NCT02581527] | Phase 3 | 672 participants (Actual) | Interventional | 2017-02-01 | Completed | ||
| Toward a Safe and Reachable Preventive Therapy for LTBI: a Multicenter Randomized Controlled Study in Taiwan [NCT02208427] | Phase 3 | 283 participants (Actual) | Interventional | 2014-08-31 | Active, not recruiting | ||
| Comparison of Vaginal Misoprostol and Dinoprostone and Isonicotinic Acid Hydrazide Prior to Copper Intrauterine Device Insertion in Nulliparous Women : a Randomized Controlled Study [NCT04505943] | 200 participants (Anticipated) | Interventional | 2020-09-01 | Not yet recruiting | |||
| Rosuvastatin Evaluation as a Tuberculosis Treatment Adjunct [NCT04504851] | Phase 2 | 154 participants (Anticipated) | Interventional | 2020-08-12 | Not yet recruiting | ||
| The Application of the N-acetyltransferase 2 (NAT2) Genotyping in Re-challenge Protocol of Isoniazid (INH) Titration in Patients With Anti-TB Medications-induced Hepatitis [NCT02076685] | 60 participants (Anticipated) | Interventional | 2007-11-30 | Recruiting | |||
| Impact of Weekly Administration of Rifapentine and Isoniazid on Steady State Pharmacokinetics of Tenofovir Alafenamide in Healthy Volunteers [NCT03510468] | Phase 1 | 51 participants (Actual) | Interventional | 2018-06-12 | Completed | ||
| A Randomized Clinical Trial of 4 Months of Rifampin vs. 9 Months of Isoniazid for Latent Tuberculosis Infection. Part 3 - Effectiveness [NCT00931736] | Phase 3 | 6,031 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| A Randomized, Double Blind, Placebo Controlled Trial to Determine the Efficacy of Isoniazid (INH) in Preventing Tuberculosis Disease and Latent Tuberculosis Infection Among Infants With Perinatal Exposure to HIV [NCT00080119] | Phase 2/Phase 3 | 1,354 participants (Actual) | Interventional | 2004-02-29 | Terminated(stopped due to Data Safety Monitoring Board (DSMB) recommended stopping study due to futility) | ||
| Active Screening of Latent TB Infection, Treatment and Long Term Follow-up in Prison [NCT00767975] | Phase 3 | 2,384 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| The Effect of Rifampicin on the Pharmacokinetics of Intracellular Tenofovir-diphosphate and Tenofovir When Coadministered With Tenofovir Alafenamide Fumarate During the Maintenance Phase of Tuberculosis Treatment in TB/HIV-1 Coinfected Participants [NCT04424264] | Phase 1 | 18 participants (Actual) | Interventional | 2019-12-05 | Completed | ||
| TBTC Study 26: Effectiveness and Tolerability of Weekly Rifapentine/Isoniazid for 3 Months Versus Daily Isoniazid for 9 Months for the Treatment of Latent Tuberculosis Infection [NCT00023452] | Phase 3 | 8,053 participants (Actual) | Interventional | 2001-06-30 | Completed | ||
| A Prospective, Randomized Open-Label Phase II Study of the Safety and Tolerability of Metformin in Combination With Standard Antimicrobial Treatment of Pulmonary Tuberculosis in People With TB and Co-infected With HIV [NCT04930744] | Phase 2 | 112 participants (Anticipated) | Interventional | 2021-08-03 | Recruiting | ||
| Impact of Once-Weekly Rifapentine and Isoniazid on the Steady State Pharmacokinetics of Dolutegravir and Darunavir Boosted With Cobicistat in Healthy Volunteers [NCT02771249] | Phase 1 | 37 participants (Actual) | Interventional | 2016-06-03 | Completed | ||
| IMPACT-TB (Imatinib Mesylate Per Oral as a Clinical Therapeutic for TB): A Phase II Clinical Trial of the Safety, Pharmacokinetics and Hematologic Effects of Imatinib on Myelopoiesis in Adults When Given With and Without Isoniazid and Rifabutin [NCT03891901] | Phase 2 | 24 participants (Actual) | Interventional | 2020-10-27 | Completed | ||
| Open-label, Randomized, Multicenter, Controlled, Parallel, Comparative Study of Efficacy and Safety of Treatment of Tuberculosis With Isoniazid, Rifampicin, Ethambutol for Intravenous Infusion in Comparison With Oral Forms While the Intensive Phase of Tre [NCT04150367] | 166 participants (Actual) | Observational | 2017-03-03 | Terminated(stopped due to According to Sponsor decision.) | |||
| The Application of the N-acetyltransferase 2 (NAT2) Genotyping in Re-challenge Protocol of Isoniazid (INH) Titration in Patients With Anti-TB Medications-induced Hepatitis [NCT00728546] | Phase 4 | 100 participants (Anticipated) | Interventional | 2008-06-30 | Recruiting | ||
| Efficacy of Simultaneous Versus Sequential Antiretroviral Therapy and Antituberculosis Treatment in Patients With AIDS and Active Tuberculosis. Open, Randomized and Controlled, Multisite Clinical Trial. [NCT00737724] | 63 participants (Actual) | Interventional | 2008-03-31 | Terminated(stopped due to Other published trials showed definitive expected superiority of Group 1) | |||
| Steady-state Pharmacokinetics of Efavirenz (Sustiva/Stocrin) 400 mg Once Daily in the Presence of Rifampicin and Isoniazid (Rifinah or the Local Generics) [NCT02832778] | Phase 1 | 35 participants (Anticipated) | Interventional | 2016-11-21 | Recruiting | ||
| A Randomized, Partially-blinded, Clinical Trial of Isoniazid and Rifapentine (3HP) Therapy to Prevent Pulmonary Tuberculosis in High-risk Individuals Identified by a Transcriptomic Correlate of Risk [NCT02735590] | Phase 2/Phase 3 | 2,927 participants (Actual) | Interventional | 2016-09-20 | Active, not recruiting | ||
| Comparing the Efficacy of Two Preventive Regimens for Adult Household Contacts With Latent Tuberculosis Infection [NCT01398618] | Phase 3 | 300 participants (Anticipated) | Interventional | 2011-05-31 | Active, not recruiting | ||
| Phase III Clinical Trial of Ultra-Short-Course Rifapentine/Isoniazid for the Prevention of Active Tuberculosis in HIV-Infected Individuals With Latent Tuberculosis Infection [NCT01404312] | Phase 3 | 3,000 participants (Actual) | Interventional | 2012-05-23 | Completed | ||
| Comparative Evaluation of Intensified Short Course Regimen and Standard Regimen for Adults TB Meningitis : an Open-label Randomized Controlled Trial [NCT05917340] | Phase 3 | 372 participants (Anticipated) | Interventional | 2024-03-31 | Not yet recruiting | ||
| Pharmacokinetics of Standard First and Second Line Anti-TB Drugs in the Lung and Lesions of Subjects Elected for Resection Surgery [NCT00816426] | Phase 1 | 19 participants (Actual) | Interventional | 2008-12-29 | Completed | ||
| New Strategy for Treating Latent Tuberculosis Infection in Brazil: A Bioequivalence Study of Two Different Dosages of Isoniazid Tablet Formulations in Human Healthy Volunteers [NCT02043314] | Phase 1 | 28 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| A Phase IV Randomized Double-Blind Placebo-Controlled Trial to Evaluate the Safety of Immediate (Antepartum-Initiated) Versus Deferred (Postpartum-Initiated) Isoniazid Preventive Therapy Among HIV-Infected Women in High Tuberculosis (TB) Incidence Setting [NCT01494038] | Phase 4 | 956 participants (Actual) | Interventional | 2014-08-19 | Completed | ||
| Randomized, Open Label, Multiple Dose Phase I Study of the Early Bactericidal Activity of Linezolid, Gatifloxacin, Levofloxacin, and Moxifloxacin in HIV-non-infected Adults With Initial Episodes of Sputum Smear-Positive Pulmonary Tuberculosis [NCT00396084] | Phase 1/Phase 2 | 70 participants (Actual) | Interventional | 2004-02-10 | Completed | ||
| Clinical Trial of Short Course Rifampin Versus INH for LTBI in Jail [NCT00128206] | Phase 3 | 364 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
| The Treatment of Pulmonary Mycobacterium Tuberculosis in HIV Infection [NCT00001033] | Phase 3 | 650 participants | Interventional | Completed | |||
| A Randomised Controlled Trial of a 12-dose Rifapentine and Isoniazid (RPT+INH) Regimen Using Direct Observed Therapy (DOT) Versus 6 Months of Daily Isoniazid for Latent Tuberculosis Infection (LTBI) in Socially Marginalised People [NCT03266991] | Phase 4 | 22 participants (Actual) | Interventional | 2017-10-27 | Terminated(stopped due to Recruitment issues) | ||
| A Phase IIc Trial of Clofazimine- and Rifapentine-Containing Treatment Shortening Regimens in Drug-Susceptible Tuberculosis: The CLO-FAST Study [NCT04311502] | Phase 2 | 104 participants (Actual) | Interventional | 2021-06-16 | Active, not recruiting | ||
| Role of Short Course Rifapentine and Isoniazid for the Preventive Treatment for Latent Genital Tuberculosis in Women With Recurrent Implantation Failure: A Prospective Interventional Cohort Study [NCT04528277] | Phase 3 | 1,050 participants (Anticipated) | Interventional | 2020-09-01 | Not yet recruiting | ||
| Reducing Early Mortality and Early Morbidity by Empiric Tuberculosis Treatment Regimens (REMEMBER) [NCT01380080] | Phase 4 | 851 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| The Early Bactericidal Activity of High-Dose or Standard-Dose Isoniazid Among Adult Participants With Isoniazid-Resistant or Drug-Sensitive Tuberculosis [NCT01936831] | Phase 2 | 282 participants (Actual) | Interventional | 2014-08-13 | Completed | ||
| A Prospective, Randomized Controlled Study for the Efficacy and Safety of the Substitution of Pyrazinamide and Ethambutol With Moxifloxacin During the Intensive Phase of Treatment of Pulmonary Tuberculosis [NCT04187469] | 286 participants (Anticipated) | Interventional | 2020-03-01 | Not yet recruiting | |||
| Different Reintroduction Regimens of Antituberculosis Drugs After Development of Hepatitis During Anti-tuberculosis Treatment [NCT01395654] | Phase 4 | 100 participants (Anticipated) | Interventional | 2011-07-31 | Recruiting | ||
| TBTC Study 26 PK: Rifapentine Pharmacokinetics in Children Receiving Once Weekly Rifapentine and Isoniazid for the Treatment of Latent Tuberculosis Infection [NCT00164450] | 230 participants (Anticipated) | Interventional | 2005-09-30 | Completed | |||
| Co-SAM: An Adaptive Multi-arm Trial to Improve Clinical Outcomes Among Children Recovering From Complicated Severe Acute Malnutrition [NCT05994742] | Phase 3 | 1,266 participants (Anticipated) | Interventional | 2024-03-01 | Not yet recruiting | ||
| Impact of LTBI Treatment on Glucose Tolerance and Chronic Inflammation [NCT04830462] | Phase 4 | 32 participants (Actual) | Interventional | 2021-04-15 | Completed | ||
| Shortened Regimens for First Diagnosed Smear Positive Drug Susceptible Pulmonary Tuberculosis: a Randomised Controlled Non-inferiority Trial [NCT02901288] | Phase 4 | 3,900 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | ||
| Prophylaxis Against Tuberculosis (TB) in Patients With Human Immunodeficiency Virus (HIV) Infection and Confirmed Latent Tuberculous Infection [NCT00000636] | 2,000 participants | Interventional | Completed | ||||
| [NCT00004740] | 300 participants | Interventional | 1995-02-28 | Active, not recruiting | |||
| A Randomized-controlled Trial of Isoniazid Plus Highly Active Antiretroviral Therapy Against Placebo to Prevent Tuberculosis in HIV-infected Persons [NCT00463086] | 1,368 participants (Actual) | Interventional | 2007-11-30 | Completed | |||
| Randomized Non-inferiority Trial Comparing the Nevirapine-based Antiretroviral Therapy Versus the Standard Efavirenz-based ART for the Treatment of HIV-TB Co-infected Patients on Rifampicin-based Therapy (ANRS 12146 CARINEMO) [NCT00495326] | Phase 2/Phase 3 | 570 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
| A Randomized Control Trial Of High-Dose Isoniazid Adjuvant Therapy For Multidrug Resistant Tuberculosis [NCT00513396] | Phase 2/Phase 3 | 134 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
| Phase I/II Dose Finding and Safety Study of Rifapentine and Isoniazid in HIV-Infected and HIV-Uninfected Children With Latent Tuberculosis Infection [NCT03730181] | Phase 1/Phase 2 | 72 participants (Anticipated) | Interventional | 2019-10-12 | Recruiting | ||
| Protecting Households On Exposure to Newly Diagnosed Index Multidrug-Resistant Tuberculosis Patients (PHOENIx MDR-TB) [NCT03568383] | Phase 3 | 5,610 participants (Anticipated) | Interventional | 2019-06-03 | Recruiting | ||
| Testing New Strategies for Patients Hospitalised With HIV-associated Disseminated Tuberculosis [NCT04951986] | Phase 3 | 732 participants (Anticipated) | Interventional | 2021-08-11 | Recruiting | ||
| Multicenter, Open, Randomized Study With Active Control to Evaluate the Early Bactericidal Activity, Safety and Pharmacokinetics of the Drug PBTZ169 When Used in Patients With First-diagnosed Tuberculosis of the Respiratory System With Bacterial Excretion [NCT03334734] | Phase 2 | 16 participants (Actual) | Interventional | 2016-12-16 | Terminated(stopped due to Very slow enrollment) | ||
| [NCT00298870] | Phase 4 | 172 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
| Long Term Study of 2 Isoniazid (INH) Prophylactic Regimens With Concomitant Cotrimoxazole (CTX) in HIV-infected Children - Impact on Morbidity, Mortality, Bacterial Resistance and Incidence of Tuberculosis [NCT00330304] | Phase 3 | 450 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
| TBTC Study 28: Evaluation of a Moxifloxacin-based, Isoniazid-sparing Regimen for Tuberculosis Treatment [NCT00144417] | Phase 2 | 433 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| TBTC Study 27: An Evaluation of the Activity and Tolerability of Moxifloxacin During the First Two Months of Treatment for Pulmonary Tuberculosis--A Double-Blind, Randomized, Multicenter Study by the Tuberculosis Trials Consortium [NCT00140309] | Phase 2 | 350 participants | Interventional | 2003-07-31 | Completed | ||
| Comparing Incidence Rate of Systemic Drug Reactions Under 3HP and 1HP Regimen for Latent Tuberculosis Infection Treatment: a Pragmatic Multicenter Randomized Control Trial [NCT04094012] | Phase 3 | 490 participants (Actual) | Interventional | 2019-09-24 | Completed | ||
| Phase 2C Clinical Trial of Novel, Short-course Regimens for the Treatment of Pulmonary Tuberculosis: CRUSH-TB (Combination Regimens for Shortening TB Treatment) [NCT05766267] | Phase 2/Phase 3 | 288 participants (Anticipated) | Interventional | 2023-03-01 | Not yet recruiting | ||
| TBTC Study 27/28 PK: Pharmacokinetic Issues in the Use of Moxifloxacin for Treatment of Tuberculosis [NCT00164463] | Phase 2 | 72 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
| A Double-blind, Multicentre, Parallel Group, Randomised, Controlled Trial to Evaluate the Possible Benefit of Isoniazid Dose Adjustment According to the Genotype for NAT2 (Arylamine N-acetyltransferase Type 2) in Patients With Pulmonary Tuberculosis [NCT00571753] | Phase 3 | 900 participants (Anticipated) | Interventional | 2008-06-30 | Terminated(stopped due to Enrolling participants has halted prematurely due to a low recruitment rate.) | ||
| Benefits and Risks of Early Antiretroviral Therapy in HIV-infected Adults in Abidjan, Côte d'Ivoire: Randomized Controlled Trial (ANRS 12136 TEMPRANO) [NCT00495651] | Phase 3 | 2,073 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
| An Open Label, Single Dose, Randomized, Two-Way Cross-Over Bioequivalence Study Comparing Rifampicin In A Fixed-Dose Combination Rifampicin + Isoniazid (Myrin© 2, Pfizer Inc) Tablet With The Reference Drug (Rimactane®, Novartis Sandoz) Capsule In Healthy [NCT01311505] | Phase 1 | 21 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| The Bioavailability of Rifampicin in Fixed Dose Combinations (FDCs) Widely Used in South Africa to Treat Drug-susceptible Tuberculosis (TB) [NCT02953847] | Phase 1 | 21 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
| Pharmacokinetics of Antituberculosis Agents in HIV-Infected Persons With Tuberculosis [NCT00000950] | 50 participants | Interventional | Completed | ||||
| Vaginal Isonicotinic Acid Hydrazide (INH) Prior to Diagnostic Office Hysteroscopy in Primarily Infertile Patients: a Randomized Controlled Trial [NCT04500522] | Phase 4 | 150 participants (Actual) | Interventional | 2020-09-01 | Completed | ||
| TBTC Study 22: Efficacy and Safety of Once-Weekly Rifapentine and Isoniazid Compared to Efficacy and Safety of Once-Weekly Rifapentine and Isoniazid Compared to Twice-Weekly Rifampin and Isoniazid in the Continuation Phase of Therapy for Pulmonary Tubercu [NCT00023335] | Phase 3 | 1,000 participants | Interventional | 1995-04-30 | Completed | ||
| Prophylaxis Against Tuberculosis (TB) in Patients With Human Immunodeficiency Virus (HIV) Infection and Suspected Latent Tuberculous Infection [NCT00000959] | 600 participants | Interventional | Completed | ||||
| Intensive Pharmacokinetics of the Nelfinavir-Rifabutin Interaction in Patients With HIV-Related Tuberculosis Treated With a Rifabutin-Based Regimen [NCT00018083] | 0 participants | Interventional | Recruiting | ||||
| A Double Blind Placebo-controlled Randomized Trial of Isoniazid for the Reversion of a Positive IFNg ELISPOT in TB Case Contacts [NCT00130325] | 214 participants (Actual) | Interventional | 2004-10-31 | Completed | |||
| TBTC Study 23A: Pharmacokinetics of Intermittent Isoniazid and Rifabutin in USPHS Study 23: Treatment of HIV-Related Tuberculosis Using a Rifabutin-Based Regimen [NCT00023348] | Phase 2/Phase 3 | 150 participants | Interventional | 1999-07-31 | Completed | ||
| Intensive Pharmacokinetic Study of Three Doses of Rifapentine (600, 900 and 1200mg) During Continuation Phase Therapy of Tuberculosis in HIV-Negative Adults [NCT00023387] | 36 participants | Interventional | 2000-03-31 | Completed | |||
| Evaluation of Three Regimens of Chemoprophylaxis for Tuberculosis in Patients co-Infected by HIV and Mycobacterium Tuberculosis [NCT00402454] | Phase 4 | 300 participants | Interventional | 1994-01-31 | Completed | ||
| A Randomized Trial of Three Regimens to Prevent Tuberculosis in HIV-Infected Patients With Anergy [NCT00402610] | Phase 4 | 332 participants | Interventional | 1994-01-31 | Completed | ||
| Short-Course Isoniazid and Rifampin Compared With Isoniazid for Latent Tuberculosis Infection: A Randomized Clinical Trial. [NCT00397709] | Phase 4 | 228 participants | Interventional | 1996-03-31 | Terminated | ||
| A Randomized, Placebo-Controlled Study of Limited vs. Continuous Isoniazid Tuberculosis Preventive Therapy in HIV-infected Persons in Botswana [NCT00164281] | Phase 4 | 2,000 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
| A Randomized Trial to Compare Effectiveness of 4 Months Rifampin (4 RIF) With 9 Months Isoniazid (9 INH) in the Prevention of Active TB in Children: The P4v9 Trial [NCT00170209] | Phase 3 | 844 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| Novel TB Prevention Regimens for HIV-Infected Adults [NCT00057122] | Phase 3 | 1,148 participants (Actual) | Interventional | 2002-09-30 | Completed | ||
| Effectiveness and Tolerability of Weekly Rifapentine/Isoniazid for 3 Months for Tuberculosis Preventive Treatment: A Randomized Controlled Study in China [NCT02430259] | Phase 3 | 566 participants (Anticipated) | Interventional | 2015-03-31 | Completed | ||
| A Randomised Placebo - Controlled Double Blind Trial Comparing 1) a Two Month Intensive Phase of Ethambutol, Moxifloxacin, Rifampicin, Pyrazinamide Versus the Standard Regimen (Ethambutol, Isoniazid, Rifampicin, Pyrazinamide) and 2) a Treatment Shortening [NCT00864383] | Phase 3 | 1,931 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| A Multiple Arm, Multiple Stage, Phase 2, OL, Randomized, Controlled Trial to Evaluate 4 Treatment Regimens of SQ109, Increased Doses of Rifampicin, and Moxifloxacin in Adults With Newly Diagnosed, Smear-positive Pulmonary Tuberculosis [NCT01785186] | Phase 2 | 365 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
| A Phase 2 Dose-ranging Trial to Evaluate the Bactericidal Activity, Safety, Tolerability and Pharmacokinetics of Linezolid in Adult Subjects With Newly Diagnosed Drug-Sensitive, Smear-Positive Pulmonary Tuberculosis. [NCT02279875] | Phase 2 | 113 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
| A Phase II Randomized, Open-label Trial of a Rifapentine Plus Moxifloxacin-Based Regimen for Intensive Phase Treatment of Smear-Positive Pulmonary Tuberculosis [NCT00728507] | Phase 2 | 121 participants (Actual) | Interventional | 2009-11-30 | Terminated(stopped due to Funding withdrawn) | ||
| Drugs for Treatment of Latent Tuberculosis Infection Objective 4: Identify Biomarkers for Clinical Trials of Drugs Active Against Latent TB [NCT00293228] | Phase 4 | 200 participants (Anticipated) | Interventional | 2007-02-28 | Completed | ||
| Point-of-care Pharmacogenomic Testing to Optimize Isoniazid Dosing for Tuberculosis Prevention [NCT05413551] | Phase 1 | 72 participants (Anticipated) | Interventional | 2023-03-23 | Recruiting | ||
| Implementation for Tuberculosis Preventive Therapy Among Latent Tuberculosis Infection in HIV-infected Individuals Using Novel Regimen of Isoniazid/Rifapentine Daily (4 Weeks) Compared to Isoniazid/Rifapentine Weekly (12 Weeks) [NCT03785106] | Phase 3 | 2,500 participants (Anticipated) | Interventional | 2019-08-15 | Recruiting | ||
| Essentiality of Isoniazid in Tuberculosis Therapy [NCT01589497] | Phase 2 | 69 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
| "A Prospective, Randomized, Comparative Clinical Trial of the Efficacy and Safety of Levofloxacin Versus Isoniazid in the Treatment of Latent Tuberculosis Infection in Liver Transplant Patients." [NCT01761201] | Phase 3 | 68 participants (Actual) | Interventional | 2012-01-31 | Terminated(stopped due to Recruitment rythm not sufficent to reach the simple size needed.) | ||
| Evaluation of the Pharmacokinetics of Antituberculosis Drugs and Tuberculosis Treatment Outcomes in HIV-tuberculosis Co-infected Ugandan Adults [NCT01782950] | Phase 4 | 400 participants (Anticipated) | Interventional | 2013-02-28 | Recruiting | ||
| Reduction of Early mortALITY in HIV-infected African Adults and Children Starting Antiretroviral Therapy: a Randomised Controlled Trial [NCT01825031] | Phase 3 | 1,805 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
| A Phase I/II Trial of the Pharmacokinetics, Tolerability, and Safety of Once-Weekly Rifapentine and Isoniazid in HIV-1-infected and HIV-1-uninfected Pregnant and Postpartum Women With Latent Tuberculosis Infection [NCT02651259] | Phase 1/Phase 2 | 50 participants (Actual) | Interventional | 2017-03-13 | Completed | ||
| A Randomised, Pragmatic, Open-Label Trial To Evaluate The Effect Of Three Months Of High Dose Rifapentine Plus Isoniazid Administered As A Single Round Or Given Annually In HIV-Positive Individuals [NCT02980016] | Phase 3 | 4,027 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
| A Randomized Controlled Non-Inferiority Study for Shortening Tuberculosis Treatment With Sitafloxacin-Containing Regimens [NCT05454345] | Phase 3 | 620 participants (Anticipated) | Interventional | 2022-10-01 | Not yet recruiting | ||
| A Phase 3 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of the Combination of Moxifloxacin Plus PA-824 Plus Pyrazinamide After 4 and 6 Months of Treatment in Adult Subjects With Drug-Sensitive Smear-Positive Pulmo [NCT02342886] | Phase 3 | 284 participants (Actual) | Interventional | 2015-02-28 | Completed | ||
| A Phase 1, Open-Label, Fixed-Sequence, Drug Interaction Study to Investigate the Effect of Once-Weekly Rifapentine and Isoniazid on the Pharmacokinetics of Steady-State Doravirine [NCT03886701] | Phase 1 | 11 participants (Actual) | Interventional | 2019-04-22 | Completed | ||
| Using Biomarkers to Predict TB Treatment Duration [NCT02821832] | Phase 2 | 946 participants (Actual) | Interventional | 2017-06-21 | Active, not recruiting | ||
| Randomized Clinical Trial to Assess the Efficacy of Short Course Intermittent Regimens for the Treatment of HIV-Associated Tuberculosis [NCT00376012] | Phase 3 | 300 participants (Actual) | Interventional | 2001-02-28 | Active, not recruiting | ||
| A Prospective Multicenter Phase II-study: Pharmacokinetics and Safety of High-Dose Rifampicin and Pyrazinamide in a Shorter Tuberculosis Treatment Compared With Standardized Treatment in Patients With Mild to Moderate Pulmonary TB [NCT04694586] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-11-30 | Recruiting | ||
| A Pilot Study of Methodology to Rapidly Evaluate Drugs for Bactericidal Activity, Tolerance, and Pharmacokinetics in the Treatment of Pulmonary Tuberculosis Using Isoniazid and Levofloxacin [NCT00000778] | Phase 1 | 44 participants | Interventional | Completed | |||
| A Prospective Study of Multidrug Resistance and a Pilot Study of the Safety of and Clinical and Microbiologic Response to Levofloxacin in Combination With Other Antimycobacterial Drugs for Treatment of Multidrug-Resistant Pulmonary Tuberculosis (MDRTB) in [NCT00000796] | 525 participants | Interventional | Completed | ||||
| A Prospective Phase Ib/IIa, Active-controlled, Randomized, Open-label Study to Evaluate the Safety, Tolerability, Extended Early Bactericidal Activity and Pharmacokinetics of Multiple Oral Doses of BTZ-043 Tablets in Subjects With Newly Diagnosed, Uncompl [NCT04044001] | Phase 1/Phase 2 | 77 participants (Actual) | Interventional | 2019-11-15 | Completed | ||
| A Combination Intervention Package for Isoniazid Preventive Therapy in Ethiopia [NCT01926379] | 338 participants (Actual) | Interventional | 2013-07-31 | Completed | |||
| Healing of Ischemic Leg Ulcers: A Pilot Trial [NCT04802928] | Phase 2 | 0 participants (Actual) | Interventional | 2008-04-30 | Withdrawn(stopped due to Patients fulfilling the criteria could not be found.) | ||
| Study to Evaluate the Safety of the Use of doTBal (Rifampicin, Isoniazid, Pyrazinamide and Ethambutol) in Patients With Tuberculosis: Conduction of an Intensive Pharmacovigilance Program [NCT04916899] | 47 participants (Actual) | Observational | 2014-11-30 | Completed | |||
| TBTC Study 33. An Evaluation of Adherence to Latent Tuberculosis Infection (LTBI) Treatment With 12 Doses of Once Weekly Rifapentine (RPT) and Isoniazid (INH) Given as Self-administered (SAT) Versus Directly-observed Therapy (DOT): iAdhere. [NCT01582711] | Phase 3 | 1,002 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| A Phase 2 Trial to Evaluate the EBA, Safety and Tolerability of Ethionamide Alone and in Combination With BVL-GSK098 Administered Orally to Adults With Newly Diagnosed, Rifampicin- and Isoniazid-Susceptible Pulmonary Tuberculosis [NCT05473195] | Phase 2 | 105 participants (Anticipated) | Interventional | 2022-12-06 | Recruiting | ||
| A Randomized Trial of DOTS Versus Enhanced DOTS for Community Control of Tuberculosis [NCT00317330] | Phase 3 | 6,400 participants | Interventional | 2004-12-31 | Completed | ||
| Evaluation of Two Different Preventive Therapy Regimens for Tuberculosis in HIV Infected Persons [NCT00351702] | Phase 3 | 650 participants (Actual) | Interventional | 2001-02-28 | Completed | ||
| Prophylaxis Against Tuberculosis (TB) in Patients With Human Immunodeficiency Virus (HIV) Infection and Confirmed Latent Tuberculous Infection [NCT00000638] | 2,000 participants | Interventional | Completed | ||||
| Viral and Immune Dynamics in HIV-Infected Patients With Tuberculosis [NCT00004736] | Phase 1 | 44 participants | Interventional | Completed | |||
| A Multiple Arm, Multiple Stage (MAMS), Phase 2B/C, Open Label, Randomized, Controlled Platform Trial to Evaluate Experimental Arms Including an Increased Dose of Rifampicin, an Optimized Dose of Pyrazinamide, Moxifloxacin and Sutezolid, in Adult Subjects [NCT05807399] | Phase 2 | 360 participants (Anticipated) | Interventional | 2023-04-14 | Recruiting | ||
| "A Randomized Trial Comparing Treatment Completion of Daily Rifapentine & Isoniazid for One Month (1HP) To Weekly Rifapentine & Isoniazid For 3 Months (3HP) In Persons Living With HIV and in HIV-negative Household Contacts of Recently Diagnosed Tuberculos [NCT05118490] | Phase 4 | 1,000 participants (Anticipated) | Interventional | 2023-04-01 | Not yet recruiting | ||
| Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis [NCT03474198] | Phase 2/Phase 3 | 675 participants (Actual) | Interventional | 2018-03-21 | Completed | ||
| Safety and Tolerability of 1 Month Daily (1HP) and 3 Months Weekly (3HP) Isoniazid and Rifapentine With Pharmacokinetics of Dolutegravir (DTG) in Pregnant People With HIV [NCT05122026] | Phase 1/Phase 2 | 252 participants (Anticipated) | Interventional | 2023-01-30 | Not yet recruiting | ||
| Efficacy, Security, Adherence, Tolerability and Cost Effectiveness of Latent TB Treatment in Patients With TB/DM2 [NCT03278483] | Phase 4 | 396 participants (Actual) | Interventional | 2019-02-28 | Completed | ||
| An Open Label, Randomized Controlled Trial to Establish the Efficacy and Safety of a Study Strategy Consisting of 6 Months of Bedaquiline (BDQ), Delamanid (DLM), and Linezolid (LNZ), With Levofloxacin (LVX) and Clofazimine (CFZ) Compared to the Current So [NCT04062201] | Phase 3 | 402 participants (Actual) | Interventional | 2019-08-22 | Active, not recruiting | ||
| Multi-centric Prospective Cohort Study of TB Recurrence Free Cure Among Microbiologically Confirmed New Pulmonary Tuberculosis Patients Treated Under NTEP With the 4-month Moxifloxacin Containing Daily Regimen [NCT05047055] | 550 participants (Anticipated) | Observational | 2021-10-01 | Not yet recruiting | |||
| New Super-short Course Regimen for Retreatment Pulmonary Tuberculosis [NCT02331823] | Phase 4 | 864 participants (Anticipated) | Interventional | 2013-06-30 | Recruiting | ||
| Quantification of the Effects of Isoniazid Treatment on Erythrocyte and Plasma Protoporphyrin IX Concentration and Plasma Aminolevulinic Acid in Patients With Erythropoietic Protoporphyria [NCT01550705] | 11 participants (Actual) | Interventional | 2012-03-31 | Terminated(stopped due to Interim analysis demonstrated the treatment was not effective) | |||
| A Phase I Single Site Open Label Clinical Trial for the Development of a Human BCG Challenge Model to Assess TB Drugs and Vaccines. [NCT05592223] | Phase 1 | 20 participants (Actual) | Interventional | 2022-12-06 | Active, not recruiting | ||
| The Effect of Cycloserine on Smoking Behavior in Nicotine Dependent Smokers. [NCT00633256] | 20 participants (Actual) | Interventional | 2006-12-31 | Completed | |||
| A Phase I Study of Intralesional Bacillus Calmette-Guerin (BCG) and Followed by Ipilimumab Therapy in Patients With Advanced Metastatic Melanoma [NCT01838200] | Phase 1 | 5 participants (Actual) | Interventional | 2014-03-31 | Terminated(stopped due to Slow recruitment due to changes in standard of care) | ||
| Comparison of 3-month Once-weekly Isoniazid Plus Rifapentine, 4-month Daily Rifampicin, and 3-month Daily Isoniazid Plus Rifampicin for the Treatment Latent Tuberculosis in Patients With End-stage Kidney Disease: A Randomised Clinical Trial [NCT05021731] | Phase 4 | 225 participants (Anticipated) | Interventional | 2022-04-01 | Not yet recruiting | ||
| A Phase 2b/c, Multi-Arm, 2-Stage, Duration Randomized Trial of the Efficacy and Safety of Two to Four Months Treatment With Regimens Containing Bedaquiline, OPC-167832, and Sutezolid, Plus Either Pretomanid or Delamanid, in Adults With Pulmonary Tuberculo [NCT05971602] | Phase 2 | 514 participants (Anticipated) | Interventional | 2023-07-26 | Recruiting | ||
| A Phase 2 Randomized, Open-Label Trial of PA-824-Containing Regimens Versus Standard Treatment for Drug-Sensitive Sputum Smear-Positive Pulmonary Tuberculosis [NCT02256696] | Phase 2 | 157 participants (Actual) | Interventional | 2015-04-29 | Completed | ||
| Drug-Drug Interactions Between Rifapentine and Dolutegravir in HIV/LTBI Co-Infected Individuals [NCT04272242] | Phase 2 | 72 participants (Anticipated) | Interventional | 2020-08-01 | Suspended(stopped due to Following completion of Arm 1, A5372 is currently Temporarily Closed. Timeline for opening of Arm 2 is not available.) | ||
| A Randomized, Phase 2b Study of a Double-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifampin-Based Tuberculosis Treatment Versus a Standard-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifabutin-Based Tuberculosis Treatment W [NCT01601626] | Phase 2 | 71 participants (Actual) | Interventional | 2013-07-13 | Terminated(stopped due to The study was stopped early due to feasibility concerns.) | ||
| Novel Triple-dose Tuberculosis Retreatment Regimen: How to Overcome Resistance Without Creating More in Niger [NCT04260477] | Phase 3 | 370 participants (Anticipated) | Interventional | 2021-03-01 | Recruiting | ||
| A Phase II, Randomized, Open-Label Trial of a Six-Month Regimen of High-Dose Rifampicin, High-Dose Isoniazid, Linezolid, and Pyrazinamide Versus a Standard Nine-Month Regimen for the Treatment of Adults and Adolescents With Tuberculous Meningitis: Improve [NCT05383742] | Phase 2 | 330 participants (Anticipated) | Interventional | 2024-01-02 | Not yet recruiting | ||
| An Open-Label, Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of a 4-month Treatment of Bedaquiline Plus Pretomanid Plus Moxifloxacin Plus Pyrazinamide (BPaMZ) Compared to a 6-month Treatment of HRZE/HR (Control) in Adult Par [NCT03338621] | Phase 2/Phase 3 | 455 participants (Actual) | Interventional | 2018-07-30 | Completed | ||
| Clinical Outcomes of Vaginal Isonicotinic Acid Hydrazide (INH) Administration Prior to T380A Intrauterine Device Insertion in Women Delivered Only by Cesarean Delivery: a Randomized Double Blinded Clinical Trial [NCT04499989] | Phase 4 | 220 participants (Actual) | Interventional | 2020-09-01 | Completed | ||
| Evaluating a New Treatment Regimen for Patients With Multidrug-resistant TB (MDR-TB) - a Prospective Open-label Randomised Controlled Trial [NCT02454205] | Phase 2/Phase 3 | 154 participants (Actual) | Interventional | 2015-11-12 | Completed | ||
| A Phase IIc, Open-Label, Randomized Controlled Trial of Ultra-Short Course Bedaquiline, Clofazimine, Pyrazinamide and Delamanid Versus Standard Therapy for Drug-Susceptible Tuberculosis (PRESCIENT) [NCT05556746] | Phase 2 | 156 participants (Anticipated) | Interventional | 2023-10-31 | Not yet recruiting | ||
| Treatment Shortening of Drug-Sensitive Pulmonary Tuberculosis Using High Dose Rifampicin to 3 Months After Culture Conversion (Hi-DoRi-3): A Phase 3, Multicenter, Randomized, Open-label, Clinical Trial [NCT04485156] | Phase 3 | 926 participants (Anticipated) | Interventional | 2020-09-30 | Not yet recruiting | ||
| A Phase 2 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of Combinations of Bedaquiline, Moxifloxacin, PA-824 and Pyrazinamide During 8 Weeks of Treatment in Adult Subjects With Newly Diagnosed Drug-Sensitive or Mu [NCT02193776] | Phase 2 | 240 participants (Actual) | Interventional | 2014-10-23 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||