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ethambutol

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Description

Ethambutol is a synthetic anti-tuberculosis drug that inhibits the synthesis of arabinogalactan, a key component of the cell wall of Mycobacterium tuberculosis. It works by interfering with the action of the enzyme arabinosyltransferase, which is responsible for adding arabinose to the galactan backbone of the cell wall. This disruption leads to the formation of a weakened and fragile cell wall, making the bacteria more susceptible to attack by the host's immune system. Ethambutol is typically used in combination with other anti-tuberculosis drugs, such as rifampicin, isoniazid, and pyrazinamide, to improve efficacy and reduce the risk of drug resistance. It is an important drug for treating tuberculosis, particularly in cases of multidrug-resistant tuberculosis. Ethambutol is studied to understand its mechanism of action, identify new targets for drug development, and develop more effective and safer treatment regimens for tuberculosis. '

Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone. [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]

Cross-References

ID SourceID
PubMed CID14052
CHEMBL ID44884
CHEBI ID4877
SCHEMBL ID3399
MeSH IDM0007814

Synonyms (92)

Synonym
KBIO1_000561
DIVK1C_000561
(2s,2's)-2,2'-(ethane-1,2-diyldiimino)dibutan-1-ol
etambutolo [dcit]
ethambutolum [inn-latin]
d-2,2'-(ethylenediimino)bis(1-butanol)
d-n,n'-bis(1-hydroxymethylpropyl)ethylenediamine
1-butanol, 2,2'-(1,2-ethanediyldiimino)bis-, (s-(r*,r*))-
(r)-2,2'-(1,2-ethanediyldiimino)bis-1-butanol
einecs 200-810-6
hsdb 3078
1-butanol, 2,2'-(1,2-ethanediyldiimino)bis-, (r)-
d-2,2'-(ethylenediimino)di-1-butanol
ethambutol [inn:ban]
1-butanol, 2,2'-(ethylenediimino)di-, (+)-
d-ethambutol
d,n,n'-bis(1-hydroxymethylpropyl)ethylenediamine
diambutol
etambutol [inn-spanish]
aethambutolum
SPECTRUM_001058
BSPBIO_002012
NCGC00178864-01
(+)-(s,s)-2,2'-(1,2-ethylenediimino)-di-1-butanol
myambutol (dihydrochloride)
(2s)-2-[2-[[(1s)-1-(hydroxymethyl)propyl]amino]ethylamino]butan-1-ol
1-butanol, 2,2'-(1,2-ethanediyldiimino)bis-, (2s,2's)-
cl 40881 (dihydrochloride)
IDI1_000561
SPECTRUM5_000702
C06984
74-55-5
ethambutol
(+)-s,s-ethambutol
(2s,7s)-2,7-diethyl-3,6-diazaoctane-1,8-diol
(+)-ethambutol
(+)-n,n'-bis(1-(hydroxymethyl)propyl)ethylenediamine
DB00330
(s,s)-ethambutol
(+)-2,2'-(ethylenediimino)di-1-butanol
s,s-ethambutol
KBIOSS_001538
KBIO2_006674
KBIO3_001232
KBIO2_001538
KBIOGR_001209
KBIO2_004106
SPECTRUM3_000426
SPECTRUM4_000545
SPECTRUM2_001014
SPBIO_001167
NINDS_000561
CHEMBL44884
CHEBI:4877 ,
ethambutolum
(2r)-2-[2-(1-hydroxybutan-2-ylamino)ethylamino]butan-1-ol
(2s)-2-[2-[[(2s)-1-hydroxybutan-2-yl]amino]ethylamino]butan-1-ol
D07925
ethambutol (inn)
servambutol (tn)
unii-8g167061qz
8g167061qz ,
etambutolo
purderal
(2s,2s)-2,2-(ethane-1,2-diyldiimino)dibutan-1-ol
ethambutol [hsdb]
ethambutol [vandf]
ethambutol [who-dd]
ethambutol [mi]
ethambutol [inn]
bdbm50448407
1-butanol,2,2'-(1,2-ethanediyldiimino)bis-, (2s,2's)-
HY-B0535
SCHEMBL3399
E-3950
ethambutol dihydrochloride, antibiotic for culture media use only
(2s,2's)-2,2'-(ethane-1,2-diylbis(azanediyl))bis(butan-1-ol)
AB00053473_04
AB00053473_05
DTXSID8023006
(2s)-2-[(2-{[(2s)-1-hydroxybutan-2-yl]amino}ethyl)amino]butan-1-ol
SBI-0051375.P003
95E ,
(s,s)-2,2'-(1,2-ethanediyldiimino)bis-1-butanol
Q412318
AEUTYOVWOVBAKS-UWVGGRQHSA-N
BRD-K93231391-300-03-1
D94801
NCGC00178864-04
(2r*,2'r*)-2,2'-(ethane-1,2-diyldiimino)dibutan-1-ol
DTXSID901028179
EN300-150035

Research Excerpts

Overview

Ethambutol (EMB) is an important anti-tuberculosis drug used in the management of multi-drug resistant tuberculosis (MDR-TB) EMB is known to cause optic neuropathy and is an integral part of Antitubercular therapy.

ExcerptReferenceRelevance
"Ethambutol (EMB) is an antimycobacterial drug used extensively for the treatment of tuberculosis caused by Mycobacterium tuberculosis. "( The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
Amin, AG; Chatterjee, D; Goude, R; Parish, T, 2009
)
2.05
"Ethambutol (EMB) is an important anti-tuberculosis drug used in the management of multi-drug resistant tuberculosis (MDR-TB). "( Characterization of embB mutations involved in ethambutol resistance in multi-drug resistant Mycobacterium tuberculosis isolates in Zambia.
Bwalya, P; Chizimu, JY; Mbulo, G; Nakajima, C; Shrestha, D; Solo, ES; Suzuki, Y; Thapa, J, 2022
)
2.42
"Ethambutol (EMB) is a first-line anti-tubercular drug that is known to cause optic neuropathy. "( Exploration of the Plausible Mechanism of Ethambutol Induced Ocular Toxicity by Using Proteomics Informed Physiologically Based Pharmacokinetic (PBPK) Modeling.
Balhara, A; Giri, S; Ladumor, MK; Nankar, RP; Prasad, B; Singh, S; Syed, SD, 2022
)
2.43
"Ethambutol (EMB) is a first-line antituberculosis drug currently being used clinically to treat tuberculosis. "(
Chen, L; Chen, X; Li, H; Liang, H; Liao, Q; Tan, Q; Wang, J; Wei, W; Wu, Z; Xu, L; Yu, M; Zhang, C; Zhao, Y, 2022
)
2.16
"Ethambutol is an antibiotic used as a first line drug in the treatment of tuberculosis and a vision threatening side effect of EMB is ethambutol-induced optic neuropathy (EON). "( Ethambutol induced toxic optic neuropathy - A retrospective study in a tertiary eye care centre in Southern India.
Balakrishnan, HK; Jayasri, KN; Kowsalya, A; Sajja, S; Shanmugam, MK, 2022
)
3.61
"Ethambutol is an integral part of Antitubercular therapy (ATT) and is often associated with optic neuropathy, However, neuroimaging of ethambutol induced optic neuropathy has been sparsely reported in the literature. "( "Neuroimaging in ethambutol induced optic neuropathy: MRI in time can save the vision".
Biswas, S; Murumkar, VS; Prabhuraj, AR; Saini, JS, 2021
)
2.4
"Ethambutol is a bacteriostatic drug that affects cell wall integrity, but the effects of this drug on bacilli are not fully exploited."( New insights on Ethambutol Targets in Mycobacterium tuberculosis.
Baldin, VP; Campanerut-Sá, PAZ; Cardoso, RF; de Lima Scodro, RB; de Souza, EM; Evaristo, GPC; Fiorini, A; Ghiraldi-Lopes, LD; Meneguello, JE; Siqueira, VLD, 2019
)
1.58
"Ethambutol is an antimycobacterial agent associated with toxic optic neuropathies."( Ethambutol toxicity exacerbating the phenotype of CMT2A2.
Arnold, WD; Binkley, EM; Epstein, A; Fonkem, E; Kissel, JT; Lawson, VH; Raymer, DS; Skordilis, MA, 2013
)
2.55
"Ethambutol is an organic cation at physiological pH, and its major metabolite, 2,2'-(ethylenediimino)dibutyric acid (EDA), is zwitterionic."( Interaction of Ethambutol with human organic cation transporters of the SLC22 family indicates potential for drug-drug interactions during antituberculosis therapy.
Gründemann, D; Pan, X; Sweet, DH; Wang, L, 2013
)
1.46
"Ethambutol (EMB) is a first-line antituberculosis drug; however, drug resistance to EMB has been increasing. "( Diagnostic accuracy of a molecular drug susceptibility testing method for the antituberculosis drug ethambutol: a systematic review and meta-analysis.
Cheng, S; Cui, Z; Hu, Z; Li, Y, 2014
)
2.06
"Ethambutol (EMB) is a frontline antituberculosis drug for the treatment of tuberculosis (TB). "( ubiA (Rv3806c) encoding DPPR synthase involved in cell wall synthesis is associated with ethambutol resistance in Mycobacterium tuberculosis.
Chen, J; Cui, P; He, L; Jin, J; Wang, X; Zhang, W; Zhang, Y, 2015
)
2.08
"Ethambutol is a common medicine used for the treatment of tuberculosis, which can have serious side effects, such as retinal and liver dysfunction. "( Ethambutol neutralizes lysosomes and causes lysosomal zinc accumulation.
Fujimura, T; Furuya, N; Hattori, N; Imamichi, Y; Ishikawa, K; Kambe, T; Koike, M; Saiki, S; Sumiyoshi, K; Ueno, T; Yamada, D, 2016
)
3.32
"Ethambutol (EMB) is a first-line anti-TB drug that is effective for preventing treatment failures caused by Mycobacterium tuberculosis strains that are resistant to other drugs."( Frequency of mutational changes in the embB among the ethambutol-resistant strains of Mycobacterium tuberculosis in Iran.
Feizabadi, MM; Haeili, M; Hashemi Shahraki, A; Imani Fooladi, AA; Mohajeri, P; Rezaei, F; Zahednamazi, F, 2016
)
1.4
"Ethambutol (EMB) is a first line drug in tuberculosis treatment inhibiting the biosynthesis of arabinogalactan, which is a component of the mycobacterial cell wall. "( The composition of cell wall skeleton and outermost lipids of Mycobacterium vaccae is modified by ethambutol treatment.
Dziadek, J; Korycka-Machała, M; Lisowska, K; Rumijowska-Galewicz, A, 2008
)
2.01
"Ethambutol (EMB) is an important first line drug, however little information on its molecular mechanism of resistance and pathogenicity of resistant isolates is available. "( Progression of chronic pulmonary tuberculosis in mice intravenously infected with ethambutol resistant Mycobacterium tuberculosis.
Ayyagari, A; Dhole, TN; Dwivedi, SK; Krishnani, N; Nyati, KK; Srivastava, S,
)
1.8
"Ethambutol is an oral anti-tuberculosis agent with chelating effects owing to its chemical structure which is similar to that of penicillamine. "( Serum copper (cu) alterations in pulmonary tuberculosis patients under treatment with ethambutol.
Abbasi Nazari, M; Kobarfard, F; Salamzadeh, J; Tabarsi, P, 2009
)
2.02
"Ethambutol (EMB) is a first-line antitubercular drug that inhibits arabinogalactan and lipoarabinomannan biosynthesis. "( Genetic characterisation of the ethambutol resistance-determining region in Mycobacterium tuberculosis: prevalence and significance of embB306 mutations.
Brum, L; Macedo, R; Perdigão, J; Portugal, I; Ribeiro, A, 2009
)
2.08
"Ethambutol (EMB) is a first-line drug for the treatment of tuberculosis (TB). "( Minor contribution of mutations at iniA codon 501 and embC-embA intergenic region in ethambutol-resistant clinical Mycobacterium tuberculosis isolates in Kuwait.
Ahmad, S; Jaber, AA; Mokaddas, E, 2009
)
2.02
"Ethambutol (EMB) is a major component of the first-line therapy of tuberculosis. "( Mycobacterium tuberculosis embB codon 306 mutations confer moderately increased resistance to ethambutol in vitro and in vivo.
Aly, S; Ehlers, S; Niemann, S; Plinke, C; Walter, K, 2011
)
2.03
"Ethambutol is a commonly used first-line anti-tuberculosis agent, and its most important potential side-effect is ethambutol-induced optic neuropathy (EON). "( [Present status of ethambutol-induced optic neuropathy].
Wang, W; Xhang, XL; Yang, H, 2012
)
2.15
"Ethambutol is an antimicrobial agent used frequently to treat tuberculosis. "( Ocular ethambutol toxicity.
Kosmorsky, GS; Lee, MS; Melamud, A, 2003
)
2.22
"Ethambutol is an antimycobacterial agent often used to treat tuberculosis."( Optical coherence tomography can measure axonal loss in patients with ethambutol-induced optic neuropathy.
Agarwal, M; Sadun, AA; Zoumalan, CI, 2005
)
1.28
"Ethambutol (EMB) is an important component of multidrug treatment regimens for Mycobacterium avium complex lung disease. "( Ethambutol ocular toxicity in treatment regimens for Mycobacterium avium complex lung disease.
Brown-Elliott, BA; Griffith, DE; Griffith, L; McLarty, J; Shepherd, S; Wallace, RJ, 2005
)
3.21
"Ethambutol hydrochloride is a commonly used first-line anti-tuberculous agent. "( Ocular toxicity of ethambutol.
Chan, RY; Kwok, AK, 2006
)
2.1
"Ethambutol is known to be an antituberculotic associated with ocular toxicity."( [Vision impairment in the course of lung tuberculosis treatment].
Czik, T; Sobota, I, 2006
)
1.06
"Ethambutol (EMB) is a first-line drug used for antitubercular therapy in combination with other drugs as recommended by World Health Organization DOTS/DOTS-Plus regimens. "( Nucleotide polymorphism associated with ethambutol resistance in clinical isolates of Mycobacterium tuberculosis.
Ayyagari, A; Dhole, TN; Dwivedi, SK; Garg, A; Nyati, KK; Srivastava, S, 2006
)
2.04
"Ethambutol is a useful first line antituberculous drug, but can cause significant visual impairment. "( Optic neuropathy associated with ethambutol in Koreans.
Choi, SY; Hwang, JM, 1997
)
2.02
"Ethambutol is an essential medication in the management of tuberculosis. "( Ethambutol is toxic to retinal ganglion cells via an excitotoxic pathway.
Dreyer, EB; Heng, JE; Lessell, E; Levin, LA; Vorwerk, CK; Zurakowski, D, 1999
)
3.19
"Ethambutol is an established front-line agent for the treatment of tuberculosis, and is also active against Mycobacterium avium infection. "( Ethambutol-sugar hybrids as potential inhibitors of mycobacterial cell-wall biosynthesis.
Bansal, N; Friedrich, J; Maddry, JA; Reynolds, RC; Rose, J; Suling, WJ, 1999
)
3.19
"Ethambutol is an efficacious antituberculosis agent. "( Ethambutol-induced vacuolar changes and neuronal loss in rat retinal cell culture: mediation by endogenous zinc.
Jung, KH; Koh, JY; Sadun, AA; Shin, HC; Yoon, YH, 2000
)
3.19
"Ethambutol (EMB) is a central component of drug regimens used worldwide for the treatment of tuberculosis. "( Molecular genetic analysis of nucleotide polymorphisms associated with ethambutol resistance in human isolates of Mycobacterium tuberculosis.
Amin, AG; Dou, SJ; El Sahly, H; Göksel, S; Kreiswirth, BN; Moghazeh, SL; Musser, JM; Ramaswamy, SV; Stager, CE, 2000
)
1.98
"Ethambutol is a strong metal-binding drug used for tuberculosis therapy."( Chelating drugs and zinc.
Weismann, K, 1986
)
0.99

Effects

Ethambutol hydrochloride has been used in the treatment of tuberculosis for 25 years. It has no significant absorption characteristics beyond 200 nm due to its aliphatic saturated nature.

ExcerptReferenceRelevance
"Ethambutol has a narrow therapeutic index related to ocular toxicity."( Biowaiver monographs for immediate release solid oral dosage forms: ethambutol dihydrochloride.
Amidon, GL; Barends, DM; Becker, C; Dressman, JB; Junginger, HE; Kopp, S; Midha, KK; Shah, VP; Stavchansky, S, 2008
)
1.3
"Ethambutol resistance has mostly been related to mutations in the embB gene. "( Characterization of the embB gene in Mycobacterium tuberculosis isolates from Barcelona and rapid detection of main mutations related to ethambutol resistance using a low-density DNA array.
Alcaide, F; Coll, P; Español, M; Gonzalez-Martin, J; Mick, V; Moure, R; Salvadó, M; Tudó, G; Vicente, E, 2014
)
2.05
"Ethambutol (EMB) has no significant absorption characteristics beyond 200 nm due to its aliphatic saturated nature. "( Ethambutol-Cobalt (II) ions complexation spectral characteristics and applications for quantitative analysis.
Atia, NN; Botros, SM; Ismail-Mohamed, AM; Mohamed, FA, 2015
)
3.3
"Ethambutol has a narrow therapeutic index related to ocular toxicity."( Biowaiver monographs for immediate release solid oral dosage forms: ethambutol dihydrochloride.
Amidon, GL; Barends, DM; Becker, C; Dressman, JB; Junginger, HE; Kopp, S; Midha, KK; Shah, VP; Stavchansky, S, 2008
)
1.3
"Ethambutol hydrochloride has been used in the treatment of tuberculosis for 25 years. "( Toxic ocular effects of ethambutol.
Kahana, LM, 1987
)
2.02

Actions

Ethambutol (EMB) is known to cause optic neuropathy and, more rarely, axonal polyneuropathy. It plays a pivotal role in the chemotherapy of drug-resistant tuberculosis (TB)

ExcerptReferenceRelevance
"Ethambutol is known to cause optic neuropathy and, more rarely, axonal polyneuropathy. "( Optochiasmatic and peripheral neuropathy due to ethambutol overtreatment.
Geyer, HL; Herskovitz, S; Schaumburg, HH; Slamovits, TL, 2014
)
2.1
"Ethambutol (EMB) plays a pivotal role in the chemotherapy of drug-resistant tuberculosis (TB), including multidrug-resistant tuberculosis (MDR-TB). "( Analysis of embCAB mutations associated with ethambutol resistance in multidrug-resistant mycobacterium tuberculosis isolates from China.
Jiang, Y; Li, GL; Liu, HC; Sun, Q; Wan, KL; Wu, XC; Xiao, TY; Zeng, CY; Zhao, LL; Zhao, XQ, 2015
)
2.12
"Ethambutol (EMB) can cause dose-related retrobulbar neuritis."( A rare adverse reaction to ethambutol: drug-induced haemolytic anaemia.
Barlascini, C; Gatto, P; Karamichali, S; Nicolini, A; Perazzo, A; Piroddi, IM; Strada, P, 2016
)
1.45
"Ethambutol can cause optic neuropathy and deficiencies in color-opponent visual processing in patients treated for tuberculosis. "( Ethambutol alters spinule-type synaptic connections and induces morphologic alterations in the cone pedicles of the fish retina.
Kohler, K; Weiler, R; Zrenner, E, 1995
)
3.18

Treatment

Treatment of 31 HIV infected patients with severe immunodeficiency and infection caused by Mycobacterium avium complex (MAC) was evaluated in a retrospective study. Treatment with ethambutol or dendrimers (fourth generation) was demonstrated to increase ON interaction with both species of mycobacteria although not to the same extent.

ExcerptReferenceRelevance
"In ethambutol-treated cases a statistically significant increase in mean serum uric acid levels was observed in the second, third and fourth week of treatment."( Hyperuricaemia induced by ethambutol.
Agarwal, MC; Bihari, K; Narang, RK; Raina, AK; Sharma, SN; Singh, SN, 1983
)
1.08
"Treatment with ethambutol plus rifampin appeared more successful (effective in five [100%] of five cases) than minocycline treatment (effective in 10 [71%] of 14 cases), although not significantly so (P = .28)."( Mycobacterium marinum skin infections. Report of 31 cases and review of the literature.
Edelstein, H, 1994
)
0.63
"Treatment with ethambutol 15 mg/kg, rifabutin 6 mg/kg and amikacin 15 mg/kg (IV for 2-4 weeks) in 31 HIV infected patients with severe immunodeficiency and infection caused by Mycobacterium avium complex (MAC) was evaluated in a retrospective study. "( Efficacy of triple drug regimen of amikacin, ethambutol and rifabutin in AIDS patients with symptomatic Mycobacterium avium complex infection.
Jorup-Rönström, C; Julander, I; Petrini, B, 1993
)
0.9
"Treatment with ethambutol or dendrimers (fourth generation) was demonstrated to increase ON interaction with both species of mycobacteria although not to the same extent."( Interaction of oligodeoxynucleotides with mycobacteria: implications for new therapeutic strategies.
Attia, SA; Davidson, MK; Hughes, JA; Rosenblatt, MN; Shepherd, VE, 1998
)
0.64
"Treatment with ethambutol had different effect in both the strains resulting in decreased total phospholipid and cardiolipin content in EMB-susceptible strain and increased content in EMB-resistant strain, with no effect on fatty acyl group composition."( Effect of ethambutol on the phospholipids of ethambutol susceptible and resistant strains of Mycobacterium smegmatis ATCC 607.
Khuller, GK; Sareen, M, 1990
)
1.02

Toxicity

Ethambutol is safe to use up to a dose of 20 mg/kg/day throughout the entire course of anti-tubercular therapy in children with drug-sensitive tuberculosis. The incidence of eth Ambutol-related toxic optic neuropathy has dramatically decreased since the recommendations for regular follow-up of patients treated with ethambutols.

ExcerptReferenceRelevance
"7%]); had similar rates of adverse drug reactions (7."( USPHS Tuberculosis Short-Course Chemotherapy Trial 21: effectiveness, toxicity, and acceptability. The report of final results.
Combs, DL; Geiter, LJ; O'Brien, RJ, 1990
)
0.28
"An analysis of the adverse effects appearing in 101 patients during at least 4 months of chemotherapy for newly detected pulmonary tuberculosis between September, 1985 and July, 1987 was performed."( Adverse effects of antitubercular drugs and significance of measurement of the drug-stimulating lymphocyte transformation rate.
Umeki, S,
)
0.13
" Secondly an epidemiological survey was attempted based on the 37 ethambutol toxicity cases registered to the Danish Board on Adverse Reactions 1972-81, making up 1% of those receiving antituberculous therapy."( Ocular ethambutol toxicity. A case report with electrophysiological considerations and a review of Danish cases 1972-81.
Fledelius, HC; Petrera, JE; Skjødt, K; Trojaborg, W, 1987
)
0.97
"Optic neuritis, a well known adverse effect of ethambutol, is related to the dose and duration of the therapy."( A case of ocular toxicity to ethambutol--an idiosyncratic reaction?
Al-Shamali, MA; Fenech, FF; Karnik, AM, 1985
)
0.82
" These cases plus similar reports in the literature suggest that isoniazid or rifampin, or both, may potentiate the hepatotoxicity of acetaminophen, perhaps by induction of cytochrome P450 isozymes that oxidize acetaminophen to its toxic metabolites."( Hepatotoxicity associated with acetaminophen usage in patients receiving multiple drug therapy for tuberculosis.
Nelson, SD; Nolan, CM; Sandblom, RE; Slattery, JT; Thummel, KE, 1994
)
0.29
"Because increased hepatotoxicity was observed with first line antituberculous agents using four drug standard induction therapy in orthotopic liver transplant patients, we evaluated the efficacy and adverse effects of a novel continuation regimen for the treatment of tuberculosis in orthotopic liver transplant patients at a University Hospital in New York City."( Tuberculosis in orthotopic liver transplant patients: increased toxicity of recommended agents; cure of disseminated infection with nonconventional regimens.
Emre, S; Meyers, BR; Miller, C; Papanicolaou, GA; Sheiner, P, 2000
)
0.31
"Major adverse reactions to antituberculosis drugs can cause significant morbidity, and compromise treatment regimens for tuberculosis (TB)."( Incidence of serious side effects from first-line antituberculosis drugs among patients treated for active tuberculosis.
Menzies, D; Parisien, I; Pelletier, M; Rocher, I; Valiquette, C; Yee, D, 2003
)
0.32
" Group II also registered; the maximum cost and highest incidence of adverse effects."( Comparative evaluation of efficacy and safety profile of three anti-tuberculous regimens in Mangalore.
Beena, S; Pai, MR; Rao, KN, 2002
)
0.31
" The most commonly recognized toxic effect of ethambutol is optic neuropathy, which generally is considered uncommon and reversible in medical literature."( Ocular ethambutol toxicity.
Kosmorsky, GS; Lee, MS; Melamud, A, 2003
)
1.03
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Measures to ensure a high level of awareness in medical staff and patients of this potential adverse effect appear to be the best current preventive method."( Ocular toxicity of ethambutol.
Chan, RY; Kwok, AK, 2006
)
0.66
"The optic nerve is quite vulnerable to the toxic effect of drugs."( [Toxicity of recent and less recent drugs on the optic nerve. Does Viagra cause blindness?].
Cordonnier, M, 2007
)
0.34
" The occurrence of adverse effects was also monitored."( Clinical evaluation and monitoring of adverse effects for fixed multidose combination against single drug therapy in pulmonary tuberculosis patients.
Chaudhry, A; Jamshaid, M; Zaka-Ur-Rehman, Z, 2008
)
0.35
"Damage of the optic nerve (optic neuropathy) may be caused, apart from other reasons, by an adverse drug effect."( [Adverse effect optic neuropathy].
Martini, BC, 2008
)
0.35
" The major side effect of the antibiotic ethambutol, commonly used in tuberculosis therapy, is a retinopathy, which may lead to selective RGC loss, if not detected in an early stage."( The G11778A LHON mutation does not enhance ethambutol cytotoxicity in a cybrid model.
Kirches, E; Mawrin, C; Pommer, R; Schoeler, S; Szibor, R,
)
0.66
" Noninferiority was dependent on consistent results from a per-protocol and modified intention-to-treat analysis, using 2 different models for the latter, classifying all changes of treatment or refusal to continue treatment (eg, bacteriological failure/relapse, adverse event, default, drug resistance) as unfavorable (model 1) and classifying changes of treatment for reasons other than therapeutic outcomes according to their 18-month bacteriological outcome if available (post hoc model 2)."( Efficacy and safety of a 4-drug fixed-dose combination regimen compared with separate drugs for treatment of pulmonary tuberculosis: the Study C randomized controlled trial.
Anyo, G; Burgos, M; Cook, SV; Enarson, DA; Jindani, A; Kim, SJ; Lienhardt, C; Nunn, AJ; Rigouts, L; Yorke-Edwards, V, 2011
)
0.37
" Adverse events related to trial drugs were similarly distributed among treatment groups."( Efficacy and safety of a 4-drug fixed-dose combination regimen compared with separate drugs for treatment of pulmonary tuberculosis: the Study C randomized controlled trial.
Anyo, G; Burgos, M; Cook, SV; Enarson, DA; Jindani, A; Kim, SJ; Lienhardt, C; Nunn, AJ; Rigouts, L; Yorke-Edwards, V, 2011
)
0.37
" Human RPE cell line RPE50 and ARPE19 cells were pretreated with specific inhibitors or transfected with shRNAs of various PKC isozymes, including PKCα, β, ε, γ, and δ, to examine whether EMB-induced toxic effects were prevented."( PKCδ-dependent signaling mediates ethambutol-induced toxic effects on human retinal pigment cells.
Chen, ZY; He, MS; Tsai, RK; Wu, WC; Wu, WS, 2011
)
0.65
" In contrast, pretreatment of the cells with specific inhibitors of PKCα, β, ε, or γ, or depletion of PKCα or β didn't influence the aforementioned EMB-triggered toxic effects."( PKCδ-dependent signaling mediates ethambutol-induced toxic effects on human retinal pigment cells.
Chen, ZY; He, MS; Tsai, RK; Wu, WC; Wu, WS, 2011
)
0.65
" The cytotoxic effects against mouse fibroblasts (NIH 3T3) in vitro were evaluated for 5c and 5d, which displayed no toxic effects (IC(50) > 1000 μM) against the mouse fibroblast cell line NIH 3T3."( Synthesis of 3-heteroarylthioquinoline derivatives and their in vitro antituberculosis and cytotoxicity studies.
Chitra, S; Manisankar, P; Muthusubramanian, S; Paul, N; Sriram, D; Yogeeswari, P, 2011
)
0.37
" Four patients did not complete the 1-year treatment because of adverse events."( The clinical efficacy and safety of a fluoroquinolone-containing regimen for pulmonary MAC disease.
Fujita, M; Harada, E; Ikegame, S; Kajiki, A; Matsumoto, T; Miyazaki, M; Nakanishi, Y; Ouchi, H; Tao, Y; Uchino, J; Watanabe, K, 2012
)
0.38
" Adverse events were mostly mild and no serious adverse events or drug discontinuations were reported."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
" Ethambutol is an antimycobacterial agent associated with toxic optic neuropathies."( Ethambutol toxicity exacerbating the phenotype of CMT2A2.
Arnold, WD; Binkley, EM; Epstein, A; Fonkem, E; Kissel, JT; Lawson, VH; Raymer, DS; Skordilis, MA, 2013
)
2.74
"The incidence of ethambutol-related toxic optic neuropathy has dramatically decreased since the recommendations for regular follow-up of patients treated with ethambutol."( [Bitemporal hemianopia as presenting sign of severe ethambutol toxicity].
Boulanger Scemama, E; Le Hoang, P; Touitou, V, 2013
)
0.98
" Toxic chiasmal lesions are rare, but in the absence of any tumoral lesion in the sellar area, a detailed history must be obtained in order to rule out drug toxicity, so as to prevent irreversible visual loss."( [Bitemporal hemianopia as presenting sign of severe ethambutol toxicity].
Boulanger Scemama, E; Le Hoang, P; Touitou, V, 2013
)
0.64
" The primary outcome was death and secondary outcome measures were 6 month disability, repeat MRI changes and serious adverse events (SAEs)."( Safety and efficacy of levofloxacin versus rifampicin in tuberculous meningitis: an open-label randomized controlled trial.
Bhoi, SK; Kalita, J; Misra, UK; Prasad, S, 2014
)
0.4
" We also assessed safety and tolerability by monitoring adverse events."( Efficiency and safety of the combination of moxifloxacin, pretomanid (PA-824), and pyrazinamide during the first 8 weeks of antituberculosis treatment: a phase 2b, open-label, partly randomised trial in patients with drug-susceptible or drug-resistant pul
Burger, DA; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Eisenach, K; Everitt, D; Ive, P; Mendel, CM; Ntinginya, NE; Page-Shipp, L; Pym, A; Reither, K; Schall, R; Spigelman, M; van Niekerk, C; Variava, E; Venter, A; von Groote-Bidlingmaier, F, 2015
)
0.42
" Frequencies of adverse events were similar to standard treatment in all groups."( Efficiency and safety of the combination of moxifloxacin, pretomanid (PA-824), and pyrazinamide during the first 8 weeks of antituberculosis treatment: a phase 2b, open-label, partly randomised trial in patients with drug-susceptible or drug-resistant pul
Burger, DA; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Eisenach, K; Everitt, D; Ive, P; Mendel, CM; Ntinginya, NE; Page-Shipp, L; Pym, A; Reither, K; Schall, R; Spigelman, M; van Niekerk, C; Variava, E; Venter, A; von Groote-Bidlingmaier, F, 2015
)
0.42
"Hepatotoxicity is a serious adverse effect of tuberculosis treatment."( Drug-induced hepatotoxicity and tuberculosis in a hospital from the Argentinian northeast: cross-sectional study.
Achinelli, FR; Ferreyra, FG; Golemba, AS; Martearena, RE; Rovai, GB, 2015
)
0.42
" Since we lack a regional registry, this casuistry could be the kickoff for the creation of regional and/or national records of anti-tuberculosis drugs adverse effects and pharmacologic vigilance."( Drug-induced hepatotoxicity and tuberculosis in a hospital from the Argentinian northeast: cross-sectional study.
Achinelli, FR; Ferreyra, FG; Golemba, AS; Martearena, RE; Rovai, GB, 2015
)
0.42
"3%] in the RPT 450 mg, RPT 600 mg and RMP groups), as were ⩾grade 3 adverse events (0/54 [0%], 1/51 [2."( Two-stage activity-safety study of daily rifapentine during intensive phase treatment of pulmonary tuberculosis.
Barnes, GL; Carman, D; Chaisson, RE; Dawson, R; Dorman, SE; Efron, A; Gupte, N; Hoffman, J; McIlleron, H; Narunsky, K; Whitelaw, A, 2015
)
0.42
" Daily RPT was safe and well-tolerated."( Two-stage activity-safety study of daily rifapentine during intensive phase treatment of pulmonary tuberculosis.
Barnes, GL; Carman, D; Chaisson, RE; Dawson, R; Dorman, SE; Efron, A; Gupte, N; Hoffman, J; McIlleron, H; Narunsky, K; Whitelaw, A, 2015
)
0.42
" The combination of anti-TB drugs (4-Tabs)- isoniazid (INH), rifampicin (RIF), pyrazinamide (PZA) and ethambutol (ETB) are effective in the management of the disease, however, their toxic effect is a major concern."( Ameliorative Effects of Kolaviron, a Biflavonoid Fraction from Garcinia Kola Seed, on Hepato-renal Toxicity of Anti-tuberculosis Drugs in Wistar Rats.
Adaramoye, OA; Adefisan, A; Adeyemi, O; Akanni, OO; Kehinde, AO; Oyinlola, I, 2016
)
0.65
"These findings suggest that anti-TB drugs elicit oxidative damage in liver and kidney of rats while KV protects against the adverse effects via antioxidative mechanism."( Ameliorative Effects of Kolaviron, a Biflavonoid Fraction from Garcinia Kola Seed, on Hepato-renal Toxicity of Anti-tuberculosis Drugs in Wistar Rats.
Adaramoye, OA; Adefisan, A; Adeyemi, O; Akanni, OO; Kehinde, AO; Oyinlola, I, 2016
)
0.43
"To assess whether increasing the dose of rifampicin (RMP) from 10 mg/kg to 15 or 20 mg/kg results in an increase in grade 3 or 4 hepatic adverse events and/or serious adverse events (SAE)."( A randomised Phase II trial to evaluate the toxicity of high-dose rifampicin to treat pulmonary tuberculosis.
Atwine, D; Bonnet, M; Borgulya, G; Burgos, M; Checkley, AM; de Fernandes, RA; de Patiño, IW; Dubash, F; Gonzales, T; Harrison, TS; Jindani, A; Mitchison, D; Patel, N; Shrestha, B, 2016
)
0.43
"No significant increase in adverse events occurred when the RMP dose was increased from 10 mg/kg to 15 mg/kg or 20 mg/kg."( A randomised Phase II trial to evaluate the toxicity of high-dose rifampicin to treat pulmonary tuberculosis.
Atwine, D; Bonnet, M; Borgulya, G; Burgos, M; Checkley, AM; de Fernandes, RA; de Patiño, IW; Dubash, F; Gonzales, T; Harrison, TS; Jindani, A; Mitchison, D; Patel, N; Shrestha, B, 2016
)
0.43
" Primary outcome was death and secondary outcomes were disability as assess by Barthel Index score and adverse events."( Safety and efficacy of additional levofloxacin in tuberculous meningitis: A randomized controlled pilot study.
Betai, S; Bhoi, SK; Kalita, J; Misra, UK, 2016
)
0.43
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
" Adverse events associated with second-line drugs (SLDs) can have severe impact on efficient management."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"To know the frequency of adverse events due to SLDs in patients of MDR-TB."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
" Adverse events associated with treatment were recognized primarily by clinical evidence and/or laboratory investigations that were advised at baseline and whenever clinically indicated during course of treatment."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"119 adverse events were reported in 46 (46."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"MDR-TB can be cured successfully with appropriate combination of drugs if adverse events associated with them can be managed aggressively and timely."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"Anti-tuberculosis drug-induced hepatotoxicity (ATDH) is a serious adverse reaction to anti-tuberculosis (TB) treatment."( Association between TXNRD1 polymorphisms and anti-tuberculosis drug-induced hepatotoxicity in a prospective study.
He, JQ; Ji, GY; Liu, QQ; Sandford, AJ; Wang, Y; Wu, JC; Wu, SQ; Zhang, MM, 2016
)
0.43
" The characteristics of RMR-TB were compared with those with adverse events to rifampin (RAE-TB)."( Treatment outcomes of rifampin-sparing treatment in patients with pulmonary tuberculosis with rifampin-mono-resistance or rifampin adverse events: A retrospective cohort analysis.
Jo, KW; Kim, WS; Lee, SD; Park, S; Shim, TS, 2017
)
0.46
" The anti-TB drugs of first choice were developed more than 4 decades ago and present several adverse effects, making the treatment of TB even more complicated and the development of new chemotherapeutics for this disease imperative."( New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity.
Aiub, CAF; Araujo-Lima, CF; Boechat, N; Castelo-Branco, FS; Costa, TEMM; Costa-Lima, MM; de Lima, EC; Domingos, JLO; Felzenszwalb, I; Gomes, KM; Henriques, MG; Lourenço, MCS; Penido, C; Pinto, AC, 2018
)
0.48
" However, their neurotoxicity could cause adverse effect and the patients with end-stage renal disease are especially vulnerable due to the reduction in renal drug clearance."( Ethambutol and isoniazid induced severe neurotoxicity in a patient undergoing continuous ambulatory peritoneal dialysis.
Chen, Y; Li, H; Peng, H; Si, M, 2018
)
1.92
"All grade 3 & 4 adverse events (AEs) and their relationship to treatment for patients who had taken at least one dose of therapy in the REMoxTB clinical trial were recorded."( Toxicity associated with tuberculosis chemotherapy in the REMoxTB study.
Amukoye, EI; Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; Hanekom, M; McHugh, TD; Mendel, CM; Meredith, SK; Murphy, ME; Murthy, SE; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD; Wills, GH, 2018
)
0.48
" The most common adverse events on standard therapy related to hepatobiliary, musculoskeletal and metabolic disorders."( Toxicity associated with tuberculosis chemotherapy in the REMoxTB study.
Amukoye, EI; Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; Hanekom, M; McHugh, TD; Mendel, CM; Meredith, SK; Murphy, ME; Murthy, SE; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD; Wills, GH, 2018
)
0.48
" Therefore, this side effect is thought to be unrecognized by most physicians."( Acute tubulointerstitial nephritis caused by rifampicin: An increasing and often overlooked side effect in elderly patients
.
Iwata, K; Nagata, M; Ohji, G, 2019
)
0.51
" Incidence rate of adverse effects was 19."( Efficacy and safety of cholecalciferol-augmented anti-tuberculosis therapy for treatment of naïve patients with pulmonary tuberculosis: A randomized, controlled, clinical study.
Abd-Ellatief, RB; Hasanain, AFA; Nafee, AMA; Zayed, AAH, 2019
)
0.51
" In addition, adding vitamin D3 to ATT provides extra protection against the hepatic and muscular adverse effects of ATT."( Efficacy and safety of cholecalciferol-augmented anti-tuberculosis therapy for treatment of naïve patients with pulmonary tuberculosis: A randomized, controlled, clinical study.
Abd-Ellatief, RB; Hasanain, AFA; Nafee, AMA; Zayed, AAH, 2019
)
0.51
" In conclusion, regimen including PZA seems to be safe for late elderly patients with pulmonary TB."( Safety of pyrazinamide-including regimen in late elderly patients with pulmonary tuberculosis: A prospective randomized open-label study.
Asaoka, M; Baba, T; Hagiwara, E; Katano, T; Kitamura, H; Komatsu, S; Ogura, T; Okuda, R; Sekine, A; Suido, Y, 2019
)
0.51
" We investigated the incidence of adverse events and cure rates according to HIV status for patients receiving standard TB therapy in the trial."( Toxicity related to standard TB therapy for pulmonary tuberculosis and treatment outcomes in the REMoxTB study according to HIV status.
Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; McHugh, TD; Mendel, CM; Meredith, SK; Mohapi, L; Murphy, ME; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD, 2019
)
0.51
" Grade 3 and 4 adverse events (AEs) were summarised by MedDRA System Organ Class."( Toxicity related to standard TB therapy for pulmonary tuberculosis and treatment outcomes in the REMoxTB study according to HIV status.
Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; McHugh, TD; Mendel, CM; Meredith, SK; Mohapi, L; Murphy, ME; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD, 2019
)
0.51
"HIV-positive patients receiving standard TB therapy in the REMoxTB study were at greater risk of adverse events during treatment but cure rates were similar when compared to a matched sample of HIV-negative patients."( Toxicity related to standard TB therapy for pulmonary tuberculosis and treatment outcomes in the REMoxTB study according to HIV status.
Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; McHugh, TD; Mendel, CM; Meredith, SK; Mohapi, L; Murphy, ME; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD, 2019
)
0.51
"8%) discontinued EMB due to various adverse effects."( Treatment Outcomes after Discontinuation of Ethambutol due to Adverse Events in
Chong, YP; Jo, KW; Kim, OH; Kwon, BS; Kwon, YS; Park, YE; Shim, TS, 2020
)
0.82
"These findings suggest that treatment outcomes are unsatisfactory in patients with MAC-LD who discontinue EMB owing to adverse events."( Treatment Outcomes after Discontinuation of Ethambutol due to Adverse Events in
Chong, YP; Jo, KW; Kim, OH; Kwon, BS; Kwon, YS; Park, YE; Shim, TS, 2020
)
0.82
" The main toxic effect of the substances was related to inhibition of mitochondrial dehydrogenases (succinate dehydrogenase and α-glycerol phosphate dehydrogenase) usually followed by suppression of activity of hydrolytic enzymes (acid phosphatase and non-specific esterase)."( Cytochemical Evaluation of the Toxic Effects of Combined Antituberculosis Substances on Metabolic State of Blood Lymphocytes.
Dolgushin, MV, 2020
)
0.56
"Completion of tuberculosis (TB) preventive treatment is important to optimize efficacy; treatment-related adverse events (AEs) sometimes result in discontinuation."( Risk Factors for Adverse Events in Household Contacts Prescribed Preventive Treatment for Drug-resistant Tuberculosis Exposure.
Amanullah, F; Becerra, MC; Cranmer, LM; Fuad, J; Gandhi, NR; Hussain, H; Jaswal, M; Keshavjee, S; Lash, TL; Malik, AA; Omer, SB; Salahuddin, N; Siddiqui, S, 2021
)
0.62
" Adverse events were categorized using the AE grading tables of the National Institutes of Health."( Risk Factors for Adverse Events in Household Contacts Prescribed Preventive Treatment for Drug-resistant Tuberculosis Exposure.
Amanullah, F; Becerra, MC; Cranmer, LM; Fuad, J; Gandhi, NR; Hussain, H; Jaswal, M; Keshavjee, S; Lash, TL; Malik, AA; Omer, SB; Salahuddin, N; Siddiqui, S, 2021
)
0.62
"To evaluate incidence of toxic optic neuropathy in patients receiving ethambutol (EMB) for 6 months and to identify its early indicators."( Prospective study to evaluate incidence and indicators for early detection of ethambutol toxicity.
Dhiman, R; Guleria, R; Mandal, S; Mohan, A; Padhy, SK; Phuljhele, S; Saxena, R; Sharma, P, 2021
)
1.08
" Adverse reaction to anti-TB chemotherapy is frequent and affects the course of the therapy, leading sometimes to discontinuation of drugs."( Isolated testicular tuberculosis with ethambutol cutaneous toxicity: A combination of two rare entities.
Cavadas, S; Ladeira, I; Leal, MDS; Pereira, FG,
)
0.4
" Recently, the guidelines of the Revised National Tuberculosis Control Programme of India have been revised to allow for fixed dose and longer duration of ethambutol use; this is likely to result in an increase in vision-threatening adverse effects."( Ethambutol toxicity: Expert panel consensus for the primary prevention, diagnosis and management of ethambutol-induced optic neuropathy.
Gandhi, R; Garg, R; Kalaiselvan, V; Karna, S; Lodha, R; Menon, V; Mohan, A; Phuljhele, S; Prakash, A; Saxena, R; Singh, D, 2021
)
2.26
"We used the Korea Adverse Event Reporting System (KAERS) database (2009-2018)."( Analysis of Adverse Drug Reactions to First-Line Anti-Tuberculosis Drugs Using the Korea Adverse Event Reporting System.
Byeon, SJ; Choi, JH; Chung, SJ, 2022
)
0.72
"Ethambutol is safe to use up to a dose of 20 mg/kg/day throughout the entire course of anti-tubercular therapy in children with drug-sensitive tuberculosis."( Ocular Toxicity of Ethambutol During Both Intensive and Continuation Phases of Anti-Tubercular Therapy in Children.
Ali, MK; Mandal, A; Mane, SS; Pustake, M; Yadav, N, 2022
)
2.49

Pharmacokinetics

The pharmacokinetic parameters of rifampin, isoniazid, ethambutol, and pyrazinamide were determined for each patient. No statistically significant difference was found in plasma pharmacokinetics. A significant decrease in the amount of unchanged ethambUTol excreted in urine was observed.

ExcerptReferenceRelevance
" A pharmacokinetic study in the mouse and rat indicated that the complex is eliminated by the kidney faster than DTPA, slower than [131I]hippuran and without significant renal retention."( Labeling of ethambutol with 99mTc using a new reduction procedure. Pharmacokinetic study in the mouse and rat.
Bally, P; Benbarek, M; Causse, JE; Couret, I; Cypriani, B; Descomps, B; Dupuy, A; Pasqualini, R; van der Valk, R; Weil, R, 1990
)
0.66
" Pharmacokinetic parameters were interpreted by using an one-part model with absorption."( [Ethambutol pharmacokinetics in pulmonary tuberculosis patients].
Abramovich, AG; Bessarabova, TN; Ivleva, AIa; Sokolova, GB; Ziia, AV,
)
1.04
" By an iteration process, based on non-linear regression analysis, the following pharmacokinetic parameters were calculated: Vd, Ka, Ke, T0."( Pharmacokinetics of antituberculosis drugs after oral isolated and simultaneous administration in triple combination.
Janků, I; Papezová, E; Stastná, J; Tousek, J; Zítková, L, 1983
)
0.27
" The beta phase exhibited a mean half-life of approximately 2 hr on dialysis in comparison to off dialysis half-lives of 7 hr or longer in renal failure."( Clearance calculations in hemodialysis: application to blood, plasma, and dialysate measurements for ethambutol.
Benet, LZ; Lee, CS; Marbury, TC, 1980
)
0.48
" Data were analyzed by noncompartmental methods and by a two-compartment pharmacokinetic model with zero-order absorption and first-order elimination."( Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids.
Bulpitt, AE; Childs, JM; Jaresko, GS; Jelliffe, RW; Nix, DE; Peloquin, CA, 1999
)
0.63
" No statistically significant difference was found in plasma pharmacokinetics (C(max), t(max), AUC, half-life and MRT) and in the renal clearance, whereas a significant decrease in the amount of unchanged ethambutol excreted in urine was observed."( Effect of rifabutin on ethambutol pharmacokinetics in healthy volunteers.
Bani, M; Benedetti, MS; Breda, M; Brianceschi, G; Dolfi, L; Pellizzoni, C; Poggesi, I; Rimoldi, R; Rocchetti, M; Sassella, D, 1999
)
0.8
" Pharmacokinetic studies in the rat show a very rapid elimination from the body after intravenous administration and a poor absorption after oral administration."( Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
Fraschini, F; Gascón, AR; Pagani, G; Pedraz Muñoz, JL; Piersimoni, C; Pregnolato, M; Scaglione, F; Terreni, M; Ubiali, D, 2000
)
0.31
" Introduction of a hydroxyl or a tertiary amino group in the N-alkyl chain resulted in an improved pharmacokinetic profile without affecting sensitively the antituberculous potency."( New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
Pagani, G; Pedraz Muñoz, JL; Piersimoni, C; Pregnolato, M; Rodríguez Gascón, A; Terreni, M; Ubiali, D, 2002
)
0.31
" We present detailed pharmacokinetic (PK) data for amikacin (AMK), ethambutol (EMB), INH, pyrazinamide (PZA), RIF, and levofloxacin in four female bongos."( Population pharmacokinetics of antituberculous drugs and treatment of Mycobacterium bovis infection in bongo antelope (Tragelaphus eurycerus isaaci).
Aguilar, R; Auclair, B; Maslow, JN; Mikota, SK; Peloquin, CA, 2002
)
0.55
"The concentration and half-life of theophylline was decreased and its clearance was increased significantly at days 5-7 after administration of antituberculosis agents compared to before the therapy was started."( The clearance of theophylline is increased during the initial period of tuberculosis treatment.
Ahn, HC; Lee, YC, 2003
)
0.32
" Concentration data were analyzed using non-compartmental and population pharmacokinetic methods."( Pharmacokinetics of ethambutol in children and adults with tuberculosis.
Ashkin, D; Auclair, B; Berning, SE; Bulpitt, AE; Burman, WJ; Jaresko, GS; Jelliffe, RW; Peloquin, CA; Stambaugh, JJ; Starke, JR; Steiner, P; Zhu, M, 2004
)
0.65
" Pharmacokinetic profiles of SQ109 in mice following a single administration showed its C(max) as 1038 (intravenous (i."( Pharmacodynamics and pharmacokinetics of SQ109, a new diamine-based antitubercular drug.
Coward, L; Gorman, G; Hanrahan, C; Jia, L; Nikonenko, B; Noker, P; Protopopova, M; Tomaszewski, JE, 2005
)
0.33
"Integrating combinatorial lead optimization of [1,2]-diamine core structure based on ethambutol with high-throughput screening has led us to focus on three promising analogs (SQ37, SQ59 and SQ109) as potential anti-tubercular drug candidates from thousands of synthesized diamine analogs for further characterization of their biopharmaceutical and pharmacokinetic properties by using liquid chromatography/tandem mass spectrometry (LC/MS/MS) and cassette dosing for pharmacokinetic screening."( Simultaneous estimation of pharmacokinetic properties in mice of three anti-tubercular ethambutol analogs obtained from combinatorial lead optimization.
Glaze, E; Gorman, GS; Jia, L; Noker, PE; Protopopova, M; Tomaszewski, JE, 2005
)
0.78
"Evaluation of sources of pharmacokinetic variation can facilitate optimization of tuberculosis treatment regimens by identification of avoidable sources of variation and of risk factors for low or high drug concentrations in patients."( Determinants of rifampin, isoniazid, pyrazinamide, and ethambutol pharmacokinetics in a cohort of tuberculosis patients.
Burger, A; Folb, PI; McIlleron, H; Norman, J; Smith, P; Wash, P, 2006
)
0.58
" A full pharmacokinetic curve for rifampin, pyrazinamide, and ethambutol was recorded after 6 weeks of daily TB treatment."( Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
Aarnoutse, RE; Alisjahbana, B; Nijland, HM; Parwati, I; Ruslami, R; van Crevel, R, 2007
)
0.58
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Intensive pharmacokinetic sampling was performed for rifampin, pyrazinamide, and ethambutol at steady state."( Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
Aarnoutse, RE; Adhiarta, IG; Alisjahbana, B; Kariadi, SH; Nijland, HM; Ruslami, R; van Crevel, R, 2010
)
0.59
" Population pharmacokinetic parameters and their variability encountered in tuberculosis patients were utilized in Monte Carlo simulations to determine the probability that particular daily doses of the drugs would achieve or exceed the EC(90) in the epithelial lining fluid of 10,000 tuberculosis patients."( New susceptibility breakpoints for first-line antituberculosis drugs based on antimicrobial pharmacokinetic/pharmacodynamic science and population pharmacokinetic variability.
Gumbo, T, 2010
)
0.36
" Ratio of peak concentration to MIC (C(max)/MIC) was linked to microbial kill rate."( Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
Deshpande, D; Gumbo, T; Leff, R; Meek, C; Srivastava, S, 2010
)
1.8
"We retrospectively collected pharmacokinetic data of all patients treated for MAC lung disease in the Adult Care Unit at National Jewish Health, Denver, Colorado, in the January 2006 to January 2010 period; we retrospectively calculated areas under the time-concentration curve (AUC)."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
0.38
"We included 531 pharmacokinetic analyses, performed for 481 patients (84% females; mean age, 63 yr; mean body mass index, 21."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
0.38
" Pharmacodynamic indices for rifampicin, clarithromycin, amikacin, and moxifloxacin are seldom met."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
0.38
"This was a Phase II open-label multiple dose pharmacokinetic and safety study."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"A total of 25 patients (56% male) completed the study; 21 had evaluable pharmacokinetic profiles."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"Coadministration of efavirenz, tenofovir and emtricitabine with a standard first-line TB treatment regimen did not significantly alter the pharmacokinetic parameters of these drugs and was tolerated well by Tanzanian TB patients who are coinfected with HIV."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
" No pharmacokinetic data are available from South American children."( Pharmacokinetics of anti-tuberculosis drugs in Venezuelan children younger than 16 years of age: supportive evidence for the implementation of revised WHO dosing recommendations.
Aarnoutse, RE; de Groot, R; de Waard, JH; García, JF; Hermans, PW; López, D; Verhagen, LM; Warris, A, 2012
)
0.38
"25 patients (83%) had an isoniazid Cmax below 3 mg/l and 23 patients (77%) had a rifampicin Cmax below 8 mg/l."( Pharmacokinetics of anti-tuberculosis drugs in Venezuelan children younger than 16 years of age: supportive evidence for the implementation of revised WHO dosing recommendations.
Aarnoutse, RE; de Groot, R; de Waard, JH; García, JF; Hermans, PW; López, D; Verhagen, LM; Warris, A, 2012
)
0.38
" We therefore determined the pharmacokinetic characteristics of first-line TB drugs in Tanzanian patients using intensive pharmacokinetic sampling."( Pharmacokinetics of first-line tuberculosis drugs in Tanzanian patients.
Aarnoutse, RE; Boeree, MJ; Kibiki, GS; Mtabho, CM; Semvua, HH; Tostmann, A; van den Boogaard, J, 2013
)
0.39
" Serum concentration-time profiles, maximum serum concentrations, time to achieve maximum serum concentrations, the half-life and the areas under the serum concentration-time curve for each of the four drugs were determined."( Pharmacokinetics and serum concentrations of antimycobacterial drugs in adult Turkish patients.
Arpag, H; Babalık, A; Bakirci, N; Çarpaner, E; Dagyildiz, L; Kuyucu, T; Ulus, IH, 2013
)
0.39
"Wide variations in pharmacokinetic parameters were observed among patients."( Pharmacokinetics and serum concentrations of antimycobacterial drugs in adult Turkish patients.
Arpag, H; Babalık, A; Bakirci, N; Çarpaner, E; Dagyildiz, L; Kuyucu, T; Ulus, IH, 2013
)
0.39
"This review will introduce pharmacokinetic parameters for key anti-TB drugs, as well as the indications and limitations of measuring these parameters in clinical practice."( Understanding pharmacokinetics to improve tuberculosis treatment outcome.
Heysell, SK; Reynolds, J, 2014
)
0.4
"Individual pharmacokinetic variability is commonplace, underappreciated and difficult to predict without therapeutic drug monitoring (TDM)."( Understanding pharmacokinetics to improve tuberculosis treatment outcome.
Heysell, SK; Reynolds, J, 2014
)
0.4
" Rectal isoniazid produced an earlier Tmax compared with oral administration."( The pharmacokinetics of a single oral or rectal dose of concurrently administered isoniazid, rifampin, pyrazinamide, and ethambutol in Asian elephants (Elephas maximus).
Egelund, EF; Hunter, RP; Isaza, R; P Brock, A; Peloquin, CA, 2014
)
0.61
" The pharmacokinetic parameters of rifampin, isoniazid, ethambutol, and pyrazinamide were determined for each patient."( Impact of nonlinear interactions of pharmacokinetics and MICs on sputum bacillary kill rates as a marker of sterilizing effect in tuberculosis.
Chigutsa, E; Gumbo, T; McIlleron, H; Pasipanodya, JG; Sirgel, FA; Smith, PJ; van Helden, PD; Visser, ME, 2015
)
0.66
"Thirty children aged 6 months to 15 years underwent intensive pharmacokinetic sampling for first-line anti-TB drugs at Queen Elizabeth Central Hospital, Blantyre, Malawi."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
0.64
"These data support recently revised WHO recommendations for dosing of anti-TB drugs in children, but dosing of ethambutol in children also appears inadequate by comparison with adult pharmacokinetic data."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
0.85
"The available pharmacokinetic data on anti-tubercular drugs in children raises the concern of suboptimal plasma concentrations attained when doses extrapolated from adult studies are used."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
0.66
" Data was analysed using population pharmacokinetic modelling."( Pharmacokinetics of Isoniazid, Pyrazinamide, and Ethambutol in Newly Diagnosed Pulmonary TB Patients in Tanzania.
Andersen, AB; Castel, S; Changalucha, J; Chigutsa, E; Christiansen, M; Denti, P; Faurholt-Jepsen, D; Friis, H; Hagen, CM; Jeremiah, K; McIlleron, H; PrayGod, G; Range, N; Wiesner, L, 2015
)
0.67
"We evaluated ethambutol plasma and intracellular pharmacokinetic according to single nucleotide polymorphisms in ABCB1, OATP1B1, PXR, VDR, CYP24A1 and CYP27B1 genes."( Ethambutol plasma and intracellular pharmacokinetics: A pharmacogenetic study.
Allegra, S; Baietto, L; Bonora, S; Calcagno, A; Cusato, J; D'Avolio, A; Fatiguso, G; Favata, F; Motta, I; Perri, GD, 2016
)
2.25
"There are limited pharmacokinetic data for use of the first-line antituberculosis drugs during infancy (<12 months of age), when drug disposition may differ."( Pharmacokinetics of Rifampin, Isoniazid, Pyrazinamide, and Ethambutol in Infants Dosed According to Revised WHO-Recommended Treatment Guidelines.
Bekker, A; Donald, PR; Draper, HR; Hesseling, AC; McIlleron, HM; Murray, S; Schaaf, HS; van der Laan, L; Wiesner, L, 2016
)
0.68
" The relative bias and relative imprecision of each pharmacokinetic parameter for each drug were derived and assessed to choose the final designs."( Population pharmacokinetics, optimised design and sample size determination for rifampicin, isoniazid, ethambutol and pyrazinamide in the mouse.
Alameda, L; Chen, C; Ferrer, S; Ortega, F; Simonsson, US, 2016
)
0.65
" The AZM Cmax was measured in patients receiving daily therapy (250 mg of AZM daily, n = 77) or intermittent therapy (500 mg of AZM three times weekly, n = 89) for MAC-LD and daily therapy for Mycobacterium abscessus complex LD (MABC-LD) (250 mg of AZM daily, n = 55)."( Peak Plasma Concentration of Azithromycin and Treatment Responses in Mycobacterium avium Complex Lung Disease.
Daley, CL; Jeon, K; Jeong, BH; Kim, SY; Koh, WJ; Lee, SY; Moon, SM; Park, HY; Shin, SJ, 2016
)
0.43
" Pyrazinamide pharmacokinetic (PK) data from 61 HIV/TB-coinfected patients in South Africa were used in the analysis."( Pharmacokinetics of Pyrazinamide and Optimal Dosing Regimens for Drug-Sensitive and -Resistant Tuberculosis.
Chirehwa, MT; Denti, P; McIlleron, H; Mthiyane, T; Onyebujoh, P; Rustomjee, R; Smith, P, 2017
)
0.46
" Intensive pharmacokinetic sampling occurred in 63 patients after 6 weeks of treatment, and safety/tolerability was assessed."( Pharmacokinetics, Tolerability, and Bacteriological Response of Rifampin Administered at 600, 900, and 1,200 Milligrams Daily in Patients with Pulmonary Tuberculosis.
Aarnoutse, RE; Boeree, MJ; Colbers, A; Gillespie, SH; Haraka, F; Hoelscher, M; Kibiki, GS; Logger, JGM; Magis-Escurra, C; Mpagama, SG; Mtabho, CM; Phillips, PPJ; Plemper van Balen, G; Reither, K; Semvua, HH; Sumari-de Boer, IM; Te Brake, LHM; van den Boogaard, J; Wattenberg, M, 2017
)
0.46
" A combined population pharmacokinetic model was developed to jointly describe the pharmacokinetics of lopinavir and ritonavir in 32 HIV-infected children (16 with MDR-TB receiving treatment with combinations of high-dose isoniazid, pyrazinamide, ethambutol, ethionamide, terizidone, a fluoroquinolone, and amikacin and 16 without TB) who were established on a lopinavir-ritonavir-containing antiretroviral regimen."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
0.66
"Dried blood spot (DBS) sampling for pharmacokinetic (PK) studies and therapeutic drug monitoring have unique advantages over venous sampling."( Evaluation of dried blood spot sampling for pharmacokinetic research and therapeutic drug monitoring of anti-tuberculosis drugs in children.
Aarnoutse, RE; Aguirre, S; Alffenaar, JW; Chaparro, G; Coronel, R; Gomez, R; Gonzalez, F; Huisman, J; Jongedijk, E; Kerkhoff, J; Magis-Escurra, C; Martial, LC; Martinez, N; Molinas, G; Pérez, D; Rodríguez, M; Roman, M; Touw, DJ, 2018
)
0.48
"Dosing recommendations for treating childhood tuberculosis (TB) were revised by the World Health Organization, yet so far, pharmacokinetic studies that have evaluated these changes are relatively limited."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
0.56
" Inter-individual pharmacokinetic variability and the effect of age, nutritional status, Human immunodeficiency virus (HIV) infection, acetylator genotype may need to be accounted for in striving for the dosages best suited for an individual."( Pharmacokinetics of First-Line Anti-Tubercular Drugs.
Kabra, SK; Lodha, R; Mukherjee, A, 2019
)
0.51
"To perform a population pharmacokinetic study of ethambutol in HIV/TB patients, and to evaluate an intensified ethambutol weight-based dosing strategy to support pharmacokinetic target attainment."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.16
" Clinical and disease status markers, including HIV-associated systemic immune activation and gut dysfunction biomarkers, were evaluated as covariates of ethambutol pharmacokinetic parameters in non-linear mixed effects analysis."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.1
" In Monte Carlo simulations, a supplementary ethambutol dose of 400 mg daily led to >2-fold improvements in pharmacokinetic target attainment probabilities in lung tissue, both before and after ART initiation."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.16
"Whole-body physiologically based pharmacokinetic (WB-PBPK) models have become an important tool in drug development, as they enable characterization of pharmacokinetic profiles across different organs based on physiological (systems-specific) and physicochemical (drug-specific) properties."( Ethambutol disposition in humans: Challenges and limitations of whole-body physiologically-based pharmacokinetic modelling in early drug development.
Carrara, L; Della Pasqua, O; Kloprogge, F; Magni, P; Pasotti, L; Teutonico, D, 2020
)
2
" Population pharmacokinetic modeling generated estimates of drug exposure (Cmax and AUC) from individual-level post hoc Bayesian estimates of plasma and intrapulmonary pharmacokinetics."( Intrapulmonary Pharmacokinetics of First-line Anti-tuberculosis Drugs in Malawian Patients With Tuberculosis.
Chasweka, M; Chirambo, AP; Chitani, A; Davies, GR; Dilly-Penchala, S; Else, LJ; Gordon, SB; Khoo, SH; Malamba, RD; McCallum, AD; Meghji, JZ; Mwandumba, HC; Pertinez, HE; Sheha, I; Sloan, DJ, 2021
)
0.62
" Nonlinear mixed-effects modeling was used to evaluate the pharmacokinetic properties of the four drugs and to simulate different dosing strategies."( Population Pharmacokinetic Properties of Antituberculosis Drugs in Vietnamese Children with Tuberculous Meningitis.
Bang, ND; Day, JN; Hoglund, RM; Ngo, VN; Nosoongnoen, W; Panjasawatwong, N; Pouplin, T; Tarning, J; Wattanakul, T, 2020
)
0.56
" We report the first pharmacokinetic data for these FDC tablets in Zambian and South African children in the treatment-shortening SHINE trial."( Pharmacokinetics of First-Line Drugs in Children With Tuberculosis, Using World Health Organization-Recommended Weight Band Doses and Formulations.
Aarnoutse, R; Chabala, C; Chirehwa, M; Choo, L; Gibb, D; Hesseling, AC; Hissar, S; Kapasa, M; Kinikar, A; LeBeau, K; Mave, V; McIlleron, H; Mulenga, V; Palmer, M; Turkova, A; van der Zalm, M; Wiesner, L; Wobudeya, E; Zimba, KM, 2022
)
0.72
"Children with drug-susceptible tuberculosis in Malawi and South Africa underwent pharmacokinetic sampling while receiving first-line tuberculosis drugs as single formulations according the 2010 WHO recommended doses."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
0.72
" Serum CAM, 14-OH CAM, EB, and RFP concentrations were measured before and at 2, 4, 6, and 12 or 24 h after administration on days 14, 28, and 42, and pharmacokinetic parameters were calculated."( Impact of rifampicin on the pharmacokinetics of clarithromycin and 14-hydroxy clarithromycin in patients with multidrug combination therapy for pulmonary Mycobacterium avium complex infection.
Enoki, Y; Hasegawa, N; Iketani, O; Kizu, J; Komeya, A; Matsumoto, K; Taguchi, K; Uno, S; Uwamino, Y, 2022
)
0.72
" Often antitubercular human dose selection is derived from pharmacokinetic data in plasma."( Prediction of lung exposure to anti-tubercular drugs using plasma pharmacokinetic data: Implications for dose selection.
Della Pasqua, O; Ferrer, S; Muliaditan, M; Ortega-Muro, F; Teutonico, D, 2022
)
0.72
" The purpose of this study was to predict the levels of drug and EDBA in the eye using physiologically based pharmacokinetic (PBPK) modeling."( Exploration of the Plausible Mechanism of Ethambutol Induced Ocular Toxicity by Using Proteomics Informed Physiologically Based Pharmacokinetic (PBPK) Modeling.
Balhara, A; Giri, S; Ladumor, MK; Nankar, RP; Prasad, B; Singh, S; Syed, SD, 2022
)
0.99
" Population pharmacokinetic models used plasma and intrapulmonary drug levels at 8 and 16 weeks."( High Intrapulmonary Rifampicin and Isoniazid Concentrations Are Associated With Rapid Sputum Bacillary Clearance in Patients With Pulmonary Tuberculosis.
Chasweka, M; Chirambo, AP; Chitani, A; Corbett, EL; Davies, GR; Ghany, JF; Gordon, SB; Khoo, SH; Malamba, R; Mallewa, JE; McCallum, AD; Meghji, JZ; Mwandumba, HC; Pertinez, HE; Shani, D; Sheha, I; Sloan, DJ, 2022
)
0.72
"58 children were assessed for eligibilty and enrolled between June 25, 2016, and Feb 6, 2018; 44 had complete stool testing and serum pharmacokinetic data, and they were included in the analyses."( Enteropathogen spectrum and effect on antimycobacterial pharmacokinetics among children with tuberculosis in rural Tanzania: a prospective cohort study.
Alshaer, MH; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kosek, M; Liu, J; Maro, A; Mduma, E; Mpagama, SG; Mujaga, B; Peloquin, CA; Rogawski McQuade, ET; Thomas, TA; Van Aartsen, D, 2022
)
0.72
"Tanzanian children undergoing tuberculosis treatment rarely attained pharmacokinetic targets; enteropathogen carriage was common and enteropathogen burden was associated with significant reductions in the concentrations of some antimycobacterial drugs."( Enteropathogen spectrum and effect on antimycobacterial pharmacokinetics among children with tuberculosis in rural Tanzania: a prospective cohort study.
Alshaer, MH; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kosek, M; Liu, J; Maro, A; Mduma, E; Mpagama, SG; Mujaga, B; Peloquin, CA; Rogawski McQuade, ET; Thomas, TA; Van Aartsen, D, 2022
)
0.72
"We systematically searched MEDLINE, Embase and Web of Science (1990-2021) for pharmacokinetic studies of first-line anti-TB drugs in children and adolescents."( Global estimates and determinants of antituberculosis drug pharmacokinetics in children and adolescents: a systematic review and individual patient data meta-analysis.
Aarnoutse, RE; Agarwal, D; Alffenaar, JC; Antwi, S; Bang, ND; Bekker, A; Bell, DJ; Chabala, C; Choo, L; Davies, GR; Day, JN; Dayal, R; Denti, P; Donald, PR; Engidawork, E; Gafar, F; Garcia-Prats, AJ; Gibb, D; Graham, SM; Hesseling, AC; Heysell, SK; Idris, MI; Kabra, SK; Kinikar, A; Kumar, AKH; Kwara, A; Lodha, R; Magis-Escurra, C; Marais, BJ; Martinez, N; Mathew, BS; Mave, V; McIlleron, HM; Mduma, E; Mlotha-Mitole, R; Mpagama, SG; Mukherjee, A; Nataprawira, HM; Peloquin, CA; Pouplin, T; Ramachandran, G; Ranjalkar, J; Roy, V; Ruslami, R; Schaaf, HS; Shah, I; Singh, Y; Stevens, J; Sturkenboom, MGG; Svensson, EM; Swaminathan, S; Taxis, K; Thatte, U; Thee, S; Thomas, TA; Tikiso, T; Touw, DJ; Turkova, A; Velpandian, T; Verhagen, LM; Wasmann, RE; Winckler, JL; Yang, H; Yunivita, V, 2023
)
0.91
" We aimed to determine whether children treated using World Health Organization-recommended or higher doses of first-line drugs achieve successful outcomes and sufficient pharmacokinetic (PK) exposures."( Effectiveness and Pharmacokinetic Exposures of First-Line Drugs Used to Treat Drug-Susceptible Tuberculosis in Children: A Systematic Review and Meta-Analysis.
Béranger, A; Gegia, M; Linh, NN; Mirzayev, F; Mohamed, A; Nahid, P; Radtke, K; Savic, RM; Schumacher, SG; Solans, BP, 2023
)
0.91
" To address this gap, we formulate a whole-body physiologically-based pharmacokinetic (PBPK) model for EPTB that for the first time includes the ability to simulate drug concentrations in the pleura and lymph node, the most commonly affected sites of EPTB."( A physiologically-based pharmacokinetic model for tuberculosis drug disposition at extrapulmonary sites.
Gadgil, CJ; Ramachandran, A, 2023
)
0.91

Compound-Compound Interactions

The activity of TLC G-65 (a liposomal gentamicin preparation), alone and in combination with rifapentine, clarithromycin, clofazimine and ethambutol, was evaluated in the beige mouse (C57BL/6J--bgj/bgj) model of disseminated Mycobacterium avium infection.

ExcerptReferenceRelevance
"14C-Isoniazid (20 mg/kg po or iv) was administered alone or in combination with aspirin (100 mg/kg po), rifampin (30 mg/kg po), ethambutol (100 mg/kg po), or ethanol (3 g/kg po) to rats."( Drug interactions with isoniazid metabolism in rats.
Solomonraj, G; Thomas, BH, 1977
)
0.46
"The activity of TLC G-65 (a liposomal gentamicin preparation), alone and in combination with rifapentine, clarithromycin, clofazimine and ethambutol, was evaluated in the beige mouse (C57BL/6J--bgj/bgj) model of disseminated Mycobacterium avium infection."( TLC G-65 in combination with other agents in the therapy of Mycobacterium avium infection in beige mice.
Cynamon, MH; Klemens, SP; Swenson, CE, 1992
)
0.49
" However, pronounced antibacterial effects were seen when ethambutol was tested in combination with ciprofloxacin, rifampicin or rifabutin, which corresponded to significantly decreased resistance to these drugs in combination."( Susceptibility of Mycobacterium kansasii to ethambutol and its combination with rifamycins, ciprofloxacin and isoniazid.
Hjelm, U; Hoffner, SE; Kaustová, J; Kubín, M, 1992
)
0.79
"The activity of clarithromycin in combination with ethambutol and rifampicin was tested at concentrations achievable in serum against 20 strains of Mycobacterium avium complex."( In vitro testing of clarithromycin in combination with ethambutol and rifampicin against Mycobacterium avium complex.
Dörtbudak, O; Lahonik, E; Stauffer, F,
)
0.63
" If chemotherapy is initiated 3 wk after challenge (established infections), the activity of this double drug combination is less effective."( Activity of rifabutin alone or in combination with clofazimine or ethambutol or both against acute and chronic experimental Mycobacterium intracellulare infections.
Farhi, DC; Gangadharam, PR; Iseman, MD; Jairam, BT; Nguyen, AK; Perumal, VK; Rao, PN, 1987
)
0.51
" tuberculosis were treated in the initial phase as inpatients for 2-3 months at random with either pyrazinamide (Z) or ethambutol (E) in combination with isoniazid (H) and rifampicin (R)."( [Which is the best drug combination for the short-term therapy of tuberculosis? A prospective randomized study with 190 patients].
Bezel, R; Brändli, O; Häcki, M; Karrer, W; Röthlisberger, K; Rubin, S, 1985
)
0.48
" We investigated the activity of three doses of the semisynthetic benzoxazinorifamycin KRM 1648, alone or in combination with ethambutol or clarithromycin, in beige mice challenged with the MAC strain 101."( Activity of KRM 1648 alone or in combination with ethambutol or clarithromycin against Mycobacterium avium in beige mouse model of disseminated infection.
Bermudez, LE; Inderlied, CB; Kolonoski, P; Young, LS, 1994
)
0.75
"5 micrograms/ml dapsone significantly inhibited growth of MAC bacteria when used in combination with other drugs specifically acting at the mycobacterial cell-wall level."( Activity of subinhibitory concentrations of dapsone alone and in combination with cell-wall inhibitors against Mycobacterium avium complex organisms.
Goh, KS; Labrousse, V; Rastogi, N, 1993
)
0.29
" malmoense isolates to a number of antibacterial drugs as well as their possible synergistic interactions when each of them was combined with ethambutol."( Susceptibility of Mycobacterium malmoense to antibacterial drugs and drug combinations.
Hjelm, U; Hoffner, SE; Källenius, G, 1993
)
0.49
"The postantibiotic effect (PAE) of clarithromycin alone and in combination with ethambutol was determined for two clinical blood isolates of Mycobacterium avium complex."( Postantibiotic effect of clarithromycin alone and combined with ethambutol against Mycobacterium avium complex.
Benson, CA; Ellis, LC; Koenig, GI; Trenholme, GM, 1995
)
0.76
"The in vivo activities of KRM-1648 alone or in combination with both ethambutol (EB) and kanamycin (KM) or clarithromycin (CAM) were tested against Mycobacterium intracellulare infections in beige mice."( Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infections in beige mice.
Amitani, R; Kuze, F; Murayama, T; Suzuki, K; Tanaka, E; Yamamoto, T, 1996
)
0.78
" The potential therapeutic activities of these agents both alone and combined with ethambutol were evaluated in a human macrophage test system and in the beige mouse animal test system with MAC strain 101."( Activities of bay Y 3118, levofloxacin, and ofloxacin alone or in combination with ethambutol against Mycobacterium avium complex in vitro, in human macrophages, and in beige mice.
Barbara-Burnham, L; Bermudez, LE; Inderlied, CB; Kolonoski, P; Wu, M; Young, LS, 1996
)
0.74
" The MIC of amoxycillin in combination with clavulanic acid was > or =2 mg/L for 27/30 (90%) isolates."( Susceptibility of multidrug-resistant strains of Mycobacterium tuberculosis to amoxycillin in combination with clavulanic acid and ethambutol.
Abate, G; Miörner, H, 1998
)
0.5
" Moxifloxacin at both concentrations in combination with ethambutol was significantly more active than each drug alone."( Activity of moxifloxacin by itself and in combination with ethambutol, rifabutin, and azithromycin in vitro and in vivo against Mycobacterium avium.
Aralar, P; Bermudez, LE; Inderlied, CB; Kolonoski, P; Petrofsky, M; Wu, M; Young, LS, 2001
)
0.8
"The activities of clarithromycin or roxithromicin used in combination with other antimicrobial drugs were tested in human macrophages experimentally infected with 23 strains of Mycobacterium avium."( Efficacy of macrolides used in combination with ethambutol, with or without other drugs, against Mycobacterium avium within human macrophages.
Brandi, G; Celeste, AG; Salvaggio, L; Schiavano, GF; Sisti, M, 2001
)
0.57
"The purpose of this study was to carry out drug-drug compatibility studies on pure first line anti-tuberculosis drugs, viz."( Drug-drug interaction studies on first-line anti-tuberculosis drugs.
Bhutani, H; Jindal, KC; Singh, S, 2005
)
0.33
" For TB drugs, equivalence was suggested for peak plasma concentrations when administered with and without efavirenz/tenofovir/emtricitabine."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"Comprehensive information on the effects of cytochrome P450 2B6 (CYP2B6) polymorphisms, clinical factors, and drug-drug interactions on efavirenz concentrations in HIV/tuberculosis-coinfected (HIV/TB) patients is unavailable."( Impact of pharmacogenetic markers of CYP2B6, clinical factors, and drug-drug interaction on efavirenz concentrations in HIV/tuberculosis-coinfected patients.
Lueangniyomkul, A; Mankatitham, W; Manosuthi, S; Manosuthi, W; Nilkamhang, S; Sukasem, C; Sungkanuparph, S; Thongyen, S, 2013
)
0.39
" Moreover, the frequency of comorbidity with human immunodeficiency virus (HIV) and with diabetes is on the rise, increasing the risk of these patients for experiencing drug-drug interactions (DDIs) due to polypharmacy."( Interaction of Ethambutol with human organic cation transporters of the SLC22 family indicates potential for drug-drug interactions during antituberculosis therapy.
Gründemann, D; Pan, X; Sweet, DH; Wang, L, 2013
)
0.74
"New compounds with antituberculosis activity and their combination with classic drugs have been evaluated to determine possible interactions and antagonism."( Potential of Casiopeínas® Copper Complexes and Antituberculosis Drug Combination against Mycobacterium tuberculosis.
Barbosa, AR; Caleffi-Ferracioli, KR; Cardoso, RF; García-Ramos, JC; Leite, CQ; Pavan, FR; Ruiz-Azuara, L; Siqueira, VL; Toledano-Magaña, Y, 2016
)
0.43
" Three studies were conducted to evaluate the potential drug-drug interactions between delamanid and antiretroviral drugs, including ritonavir, a strong inhibitor of CYP3A4, and selected anti-TB drugs, including rifampin, a strong inducer of cytochrome P450 (CYP) isozymes."( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects.
Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016
)
0.43
" Ultimately, the good permeability, moderate rates of metabolism and low risk of drug-drug interactions displayed by some of the synthesized compounds indicate that 2-(quinolin-4-yloxy)acetamides may yield candidates to use in the development of novel alternative therapeutics for tuberculosis treatment."( New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
Abbadi, BL; Back, DF; Basso, LA; Campos, MM; Giacobbo, BC; Grams, ES; Machado, P; Pissinate, K; Rodrigues-Junior, V; Santos, DS; Sperotto, N; Subtil, FT; Trindade, RV; Villela, AD, 2017
)
0.46
" We describe the pharmacokinetics of and potential drug-drug interactions between lopinavir-ritonavir and drugs routinely used for MDR-TB treatment in HIV-infected children."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
0.48
"When RFP is combined with CAM in the treatment of pulmonary MAC infection, the blood concentration of CAM significantly decreased and that of the active metabolite 14-OH CAM increased, but not significantly."( Impact of rifampicin on the pharmacokinetics of clarithromycin and 14-hydroxy clarithromycin in patients with multidrug combination therapy for pulmonary Mycobacterium avium complex infection.
Enoki, Y; Hasegawa, N; Iketani, O; Kizu, J; Komeya, A; Matsumoto, K; Taguchi, K; Uno, S; Uwamino, Y, 2022
)
0.72
" Clofazimine (CFZ) has showed benefit in shortening DS-TB treatment in vivo from six to four months when used in combination with this regimen in murine models of experimental infection."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
0.72
"In the current in vitro study, the inhibitory and bactericidal activities of CFZ in combination with the primary anti-TB drugs, RMP, INH and EMB against the AR and SR organisms in planktonic and biofilm-forming cultures, respectively, were evaluated by fractional inhibitory concentration index (FICI) and fractional bactericidal concentration index (FBCI) determinations, using the Loewe Additivity Model."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
0.72
"In planktonic cultures, CFZ demonstrated synergistic growth inhibitory activity in combination with RMP and INH individually and collectively."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
0.72
"Clofazimine exhibited synergistic effects in combination with primary anti-TB drugs against both planktonic and biofilm-forming cultures, showing potential benefit in augmenting treatment outcome when used during standard TB chemotherapy."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
0.72

Bioavailability

Poor bioavailability of rifampicin (R) in combination with other anti-tuberculosis drugs such as isoniazid (H), pyrazinamide (Z), and ethambutol (E) is a subject of much concern for the last few decades. This study was conducted in healthy Chinese subjects to compare the bioavailability from a 4-drug FDC formulation versus that of separate formulations.

ExcerptReferenceRelevance
"In a pilot study involving 62 patients with open pulmonary tuberculosis, we established that slow acetyators and patients receiving intravenous rifampicin treatment showed a tendency towards a more rapid negativisation of the sputum culture than did fast acetyators (lower levels of isoniazid) or patients receiving oral rifampicin therapy (decreasing bioavailability of the rifampicin during treatment)."( [Significance of the acetylator phenotype and initial oral/intravenous rifampicin administration in the treatment of tuberculosis].
Loos, U; Musch, E; Schwabe, HK, 1990
)
0.28
" The bioavailability of the active, orally administered rifampicin decreased from 93% after the first single oral dose to 68% after 3 weeks of oral and intravenous rifampicin therapy."( Pharmacokinetics of oral and intravenous rifampicin during chronic administration.
Eichelbaum, M; Jensen, JC; Loos, U; Mikus, G; Musch, E; Schwabe, HK, 1985
)
0.27
" Mean bioavailability of ethambutol was approximately 28% and was not affected by the presence of aluminum hydroxide."( Absorption and disposition of ethambutol in rabbits.
Chen, MM; Lee, CS; Perrin, JH, 1984
)
0.86
" The method was utilized for studying the bioavailability and pharmacokinetics of the drug."( Determination of ethambutol in plasma using selected ion monitoring.
Ohya, K; Sano, M; Shintani, S, 1980
)
0.6
"Twenty male volunteers who were slow metabolisers of isoniazid, completed this single-blind, single-dose, randomised, cross-over study to compare the bioavailability of rifampicin (CAS 13292-46-1), isoniazid (CAS 54-85-3) and ethambutol (CAS 1070-11-7) from Myrin tablets (test preparation) with the bioavailability of these drugs from a combination of capsules containing rifampicin and tablets containing isoniazid and ethambutol (reference)."( Relative bioavailability of rifampicin, isoniazid and ethambutol from a combination tablet vs. concomitant administration of a capsule containing rifampicin and a tablet containing isoniazid and ethambutol.
Duursema, L; Groenewoud, G; Hundt, HK; Middle, MV; Mogilnicka, EM; Müller, FO; Schall, R; Swart, KJ, 1995
)
0.72
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"The perceived need for simple, non-invasive methods of assessing the relative bioavailability of rifampicin in fixed-dose combination (FDC) anti-tuberculosis formulations."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
0.31
"To compare the performance of methods based on urinary excretion data with those utilising plasma concentration-time profiles to assess the relative bioavailability of rifampicin in combined and single-drug formulations."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
0.31
"There was good agreement between the relative bioavailability of the formulations using plasma and urinary excretion data, although the precision of the urinary-based estimates was slightly less than those derived from the plasma findings."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
0.31
" The pharmacokinetics and relative bioavailability after intravenous administration of three derivatives have been investigated."( New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
Pagani, G; Pedraz Muñoz, JL; Piersimoni, C; Pregnolato, M; Rodríguez Gascón, A; Terreni, M; Ubiali, D, 2002
)
0.31
" In this study, the relative bioavailability of rifampicin, isoniazid and pyrazinamide was assessed in a group of 14 healthy male subjects using the FDC tablet containing 4 drugs versus separate formulations at the same dose levels."( Bioequivalence assessment of rifampicin, isoniazid and pyrazinamide in a fixed dose combination of rifampicin, isoniazid, pyrazinamide and ethambutol vs. separate formulations.
Agrawal, S; Bhade, SR; Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 2002
)
0.52
" The objective of this investigation was to evaluate whether the World Health Organization (WHO) simplified screening protocol for the bioequivalence assessment of rifampicin can be used for the evaluation of other components of FDC so as to ensure the bioavailability of all drugs at tissue site."( Evaluation of bioequivalence of isoniazid and pyrazinamide in three and four drugs fixed dose combinations using WHO simplified protocol.
Agrawal, S; Kaul, CL; Panchagnula, R; Rungta, S; Sancheti, P, 2003
)
0.32
"Poor bioavailability of rifampicin (R) in combination with other anti-tuberculosis drugs such as isoniazid (H), pyrazinamide (Z), and ethambutol (E) is a subject of much concern for the last few decades."( Bioavailability of rifampicin following concomitant administration of ethambutol or isoniazid or pyrazinamide or a combination of the three drugs.
Chandrasekaran, V; Gurumurthy, P; Immanuel, C; Prabhakar, R; Ramachandran, G; Venkatesan, P, 2003
)
0.76
" Bioavailability was expressed as an index (BI) of area under time concentration curve (AUC) calculated from the plasma concentrations or proportion of dose of R excreted as R plus DR in urine with the combinations to that with R alone."( Bioavailability of rifampicin following concomitant administration of ethambutol or isoniazid or pyrazinamide or a combination of the three drugs.
Chandrasekaran, V; Gurumurthy, P; Immanuel, C; Prabhakar, R; Ramachandran, G; Venkatesan, P, 2003
)
0.55
" HIV and HIV-tuberculosis patients who have diarrhea and cryptosporidial infection exhibit decreased bioavailability of antituberculosis drugs."( Decreased bioavailability of rifampin and other antituberculosis drugs in patients with advanced human immunodeficiency virus disease.
Bhagavathy, S; Gurumurthy, P; Hemanth Kumar, AK; Mahilmaran, A; Padmapriyadarsini, C; Paramesh, P; Rajasekaran, S; Ramachandran, G; Ravichandran, N; Sekar, L; Swaminathan, S; Venkatesan, P, 2004
)
0.32
" The oral bioavailability was 4%."( Pharmacodynamics and pharmacokinetics of SQ109, a new diamine-based antitubercular drug.
Coward, L; Gorman, G; Hanrahan, C; Jia, L; Nikonenko, B; Noker, P; Protopopova, M; Tomaszewski, JE, 2005
)
0.33
" The relative/absolute bioavailability of the 4 antituberculosis drugs was enhanced several fold."( Chemotherapeutic efficacy of nanoparticle encapsulated antitubercular drugs.
Khuller, GK; Pandey, R; Sharma, S,
)
0.13
" The studies determined the bioavailability and bioequivalence of RMP-containing FDCs, and conformed with the requirements of the South African national drug regulatory authority for each of the active constituents."( Modification to improve efficiency of sampling schedules for BA/BE testing of FDC anti-tuberculosis drugs.
Folb, PI; Fourie, PB; Gabriels, GA; McIlleron, H; Smith, PJ, 2007
)
0.34
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" In comparison to free drugs (which were cleared from plasma/organs within 12-24 h), there was a significant enhancement in the relative bioavailability of encapsulated drugs."( Alginate nanoparticles as antituberculosis drug carriers: formulation development, pharmacokinetics and therapeutic potential.
Ahmad, Z; Khuller, GK; Pandey, R; Sharma, S,
)
0.13
" The bioavailability of rifampin was determined by comparing rifampin exposure after oral versus intravenous administration."( Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
Aarnoutse, RE; Adhiarta, IG; Alisjahbana, B; Kariadi, SH; Nijland, HM; Ruslami, R; van Crevel, R, 2010
)
0.36
" However, the quality of FDCs with respect to variable bioavailability is a major issue."( Oral bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide in a 4-drug fixed-dose combination compared with the separate formulations in healthy Chinese male volunteers.
Chen, M; Fu, L; Jin, H; Liu, C; Lu, Y; Wang, B; Xu, J; Zhao, W; Zheng, M; Zhou, L; Zhu, H, 2013
)
0.65
"This study was conducted in healthy Chinese subjects to compare the bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide from a 4-drug FDC formulation versus that of the separate formulations."( Oral bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide in a 4-drug fixed-dose combination compared with the separate formulations in healthy Chinese male volunteers.
Chen, M; Fu, L; Jin, H; Liu, C; Lu, Y; Wang, B; Xu, J; Zhao, W; Zheng, M; Zhou, L; Zhu, H, 2013
)
0.86
" Oral rifampin and oral ethambutol were well absorbed while rectal rifampin was not."( The pharmacokinetics of a single oral or rectal dose of concurrently administered isoniazid, rifampin, pyrazinamide, and ethambutol in Asian elephants (Elephas maximus).
Egelund, EF; Hunter, RP; Isaza, R; P Brock, A; Peloquin, CA, 2014
)
0.92
"2h) and low absolute bioavailability (1."( Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis.
Chaturvedi, V; Dasgupta, A; Gupta, AD; Jaiswal, S; Kashyap, VK; Khan, SR; Krishnan, MY; Lal, J; Roy, KK; Saxena, AK; Sharma, A; Sharma, SK; Singh, S; Sinha, S; Srivastava, R, 2015
)
0.42
" Nonlinear mixed-effects modeling found that influential covariates for the pharmacokinetics were weight, sex, and a 30% increased bioavailability among heterozygous carriers of SLCO1B1 rs1104581 (previously associated with low rifampin concentrations)."( Effect of SLCO1B1 Polymorphisms on Rifabutin Pharmacokinetics in African HIV-Infected Patients with Tuberculosis.
Egan, D; Hennig, S; Kellerman, T; McIlleron, H; Naiker, S; Owen, A; Pym, A; Reddy, T; Wiesner, L, 2016
)
0.43
" Its bioavailability at an oral dose of 2 mg/kg was 15%."( Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
Beuerman, RW; Cao, D; Corkran, HM; Dick, T; Koh, JJ; Lakshminarayanan, R; Lim, F; Lin, S; Liu, S; Mukherjee, D; Stocker, BL; Tan, DTH; Tan, DZ; Tan, JK; Timmer, MSM; Zou, H, 2016
)
0.43
" MDR-TB treatment did not have a significant effect on the bioavailability, clearance, or absorption rate constants of lopinavir or ritonavir."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
0.48
" Pharmacokinetic studies indicate that 1 has an oral bioavailability with an average F-value of 27."( An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
Eslamimehr, S; Franzblau, SG; Kong, Y; Kurosu, M; Lemieux, MR; Mitachi, K; Park, F; Pressly, JD; Siricilla, S; Wang, Y; Yang, D, 2018
)
0.48
"Tetrazole, a bioisostere of the carboxylic acid group, can replace the carboxyl group in drugs to increase the lipophilicity, bioavailability and reduce side effects."( Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
Chang, L; Ding, C; Feng, LS; Gao, C; Wu, X; Xu, Z; Yan, XF; Zhao, F, 2019
)
0.51
" For preventing drug resistance and side-effects of anti-tuberculosis drugs, new methods for improving the bioavailability of APIs were investigated."( Properties of Therapeutic Deep Eutectic Solvents of l-Arginine and Ethambutol for Tuberculosis Treatment.
C Duarte, AR; P S Leitão, MI; Santos, F, 2018
)
0.72
" Ethambutol serum concentrations were best explained by a two-compartment model with first-order elimination, with a significant improvement in oral bioavailability following ART initiation."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.81
"Low serum ethambutol concentrations were commonly observed among HIV/TB patients in Botswana, and the oral bioavailability of ethambutol increased following ART initiation."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.31
" PZA exists in four enantiotropically-related polymorphs (Forms α, δ, β and γ), but only Form α is considered suitable for pharmaceutical products due to its stability and bioavailability properties."( Tackling quantitative polymorphic analysis through fixed-dose combination tablets production. Pyrazinamide polymorphic assessment.
Antonio, M; Maggio, RM; Raffaghelli, M, 2021
)
0.62
" In HIV+ children on lopinavir/ritonavir, bioavailability was reduced by 32% [median (IQR) steady-state Cmax = 0."( Population pharmacokinetics of ethambutol in African children: a pooled analysis.
Abdelwahab, MT; Andrieux-Meyer, I; Bekker, A; Chabala, C; Cotton, MF; Davies, G; Denti, P; Hesseling, A; Lee, J; McIlleron, H; Rabie, H; Tikiso, T; Wiesner, L; Zar, HJ, 2022
)
1.01

Dosage Studied

The predicted AUC0 for rifampicin dosed at 15 mg/kg was comparable to that of adults. The conduction velocity tended to decrease in the high ethambutol dosage (200 gm or more) group. These data support recently revised WHO recommendations for dosing of anti-TB drug.

ExcerptRelevanceReference
" But this effect is small and does not justify a change in the usual dosage of rifampicin."( [The use of mycobacteria in the estimation of the concentration of antibiotics, antimycotics and antituberculotics (author's transl)].
Iwainsky, H; Reutgen, H; Sesser, I, 1978
)
0.26
" Basing their comment on the published literature, they analyze the properties, pharmacology, toxicity, and side-effects of each medication, and define their dosage and modes of administration."( [Principles underlying the use of antituberculosis medication in children (author's transl)].
Besson-Leaud, M; Ollivier, A,
)
0.13
" It rests on an optimum dosage in connection with a best suited combination, taking into consideration the relations of sensitiveness and side effects as well as consequent long-term treatment."( [Modern therapy and after-care in urogenital tuberculosis].
Kalweit, H; Lenk, S; Rothkopf, M, 1978
)
0.26
" One group had received ethambutol in a mean dosage of 14."( Ethambutol and intra-ocular pressure.
Darbyshire, JH; Friedmann, AI; Kun, OJ; Pattisson, PR; Tall, R, 1978
)
2.01
" The patient's cooperation during a systematic triple drug therapy in adequate dosage is important."( [Present status and treatment of urogenital tuberculosis].
Haubensak, K; Osterhage, HR, 1975
)
0.25
" With both 600 and 1200 mg rifampicin dosage the bacteriological results at the end of a year were similar (5% bacteriologically unfavourable in each group)."( A comparative study of daily followed by twice- or once-weekly regimens of ethambutol and rifampicin in the retreatment of patients with pulmonary tuberculosis: second report.
, 1976
)
0.49
"The charge transfer complex formation between ethambutol and iodine was investigated and utilized as the basis for a sensitive spectrophotometric procedure for ethambutol and its dosage forms."( Sensitive assay procedure for ethambutol hydrochloride via charge transfer complex formation.
Dimattio, AS; Gerlach, ED; Tan, HS, 1977
)
0.8
" The administration of isoniazid in standard dosage for one year in these situations will help greatly to reduce tuberculosis as a community health problem in the future."( The Jewish Hospital of St. Louis therapeutic grand rounds number 10. Chemoprophylaxis of tuberculosis.
Avioli, LV; Byrd, R; Lefrak, SS; Senior, RM, 1975
)
0.25
" A dose-response experiment was performed with clarithromycin at 50, 100, 200, or 300 mg/kg of body weight administered daily by gavage to mice infected with approximately 10(7) viable MAC."( Activity of clarithromycin against Mycobacterium avium complex infection in beige mice.
Cynamon, MH; DeStefano, MS; Klemens, SP, 1992
)
0.28
" Three of the patients were receiving a maintenance dosage of 15 mg/kg per day."( Toxic ocular effects of ethambutol.
Kahana, LM, 1987
)
0.58
" Self-induction of rifampin clearance by chronic dosing with the drug may lead to subtherapeutic levels of rifampin."( Pharmacokinetics of antituberculosis drugs in patients.
el-Attar, H; Israili, ZH; Rogers, CM, 1987
)
0.27
" In the first study, when isoniazid was prescribed daily in a dosage of 20 mg/kg, 39% of the patients developed jaundice; however, when the dosage was reduced to 12 mg/kg, the incidence fell to 16%."( Three chemotherapy studies of tuberculous meningitis in children.
Duraipandian, M; Nagarajan, M; Prabhakar, R; Ramachandran, P; Ramakrishnan, CV; Tripathy, SP, 1986
)
0.27
" Dosage adjustment is mandatory for EMB in patients with compromised renal function in order to achieve optimal therapy and to avoid undesirable side effects."( Ethambutol kinetics in patients with impaired renal function.
Benet, LZ; Brater, DC; Lee, CS; Varughese, A, 1986
)
1.71
" Minor adverse reactions occurred with similar frequencies during daily (5%) and intermittent (5%) treatment but in no case was modification of rifampicin dosage required."( Safety of thrice-weekly rifampicin for tuberculosis in South-East Asian refugees.
McKenzie, DK; Mukerjee, CM, 1985
)
0.27
" Current dosage recommendations are based on total body weight (TBW); drug toxicity might result in obese patients receiving TBW doses."( Dosage of antituberculous drugs in obese patients.
Geiseler, PJ; Maddux, MS; Manis, RD, 1985
)
0.27
" The others received the same dosage of ethambutol and 450 mg."( Treatment of chronic drug-resistant pulmonary tuberculosis with rifampin and ethambutol.
Eidus, L; Jeanes, CW; Jessamine, AG, 1972
)
0.75
" The conduction velocity tended to decrease in the high ethambutol dosage (200 gm or more) group compared with the low dosage (200 gm or less) group."( Peripheral nerve conduction function in patients treated with antituberculotic agents, with special reference to ethambutol and isoniazid.
Sanagi, S; Takahashi, M; Takenaka, H; Takeuchi, H; Tarui, S, 1980
)
0.72
" Additional pediatric pharmacokinetic studies are necessary to confirm the current dosage recommendation and use of these agents in the pediatric patient."( Clinical pharmacology of antitubercular drugs.
Blumer, JL; Reed, MD, 1983
)
0.27
" This increase was independent of dosage of ethambutol."( Hyperuricaemia induced by ethambutol.
Agarwal, MC; Bihari, K; Narang, RK; Raina, AK; Sharma, SN; Singh, SN, 1983
)
0.83
" In a controlled study of culture-positive advanced pulmonary tuberculosis we have compared treatment regimens with PZA in a dosage of less than 2 g and with ethambutol (EMB)."( [Pyrazinamide versus ethambutol in short-term therapy of lung tuberculosis. A randomized study].
Brändli, O; Fiala, W; Häcki, MA, 1983
)
0.78
" Dosage of diazepam may require adjustment in patients with tuberculosis on chemotherapy."( Diazepam interaction with antituberculosis drugs.
Dengler, HJ; Greenblatt, DJ; Ochs, HR; Roberts, GM, 1981
)
0.26
" Animals were killed 1, 2, 4, 7, and 24 h after dosage and radioactivity in various tissues was measured."( Tissue distribution of [14C]ethambutol in mice.
Eisner, HJ; Kaleita, E; Kelly, RG, 1981
)
0.56
" An adaptation of the rapid oral desensitization protocol for penicillin was used, with the dosing intervals increased to account for the different kinetics of these drugs."( Oral desensitization to rifampin and ethambutol in mycobacterial disease.
Borish, LC; Matz, J; Rosenwasser, LJ; Routes, JM, 1994
)
0.56
"310 patients with pulmonary tuberculosis disseminating bacteria received isoniazid, rifampicin, streptomycin (ethambutol) and pirazinamid in different regimens and dosage forms."( [Combined chemotherapy of patients with tuberculosis - new regimens and dosage forms].
Elistratova, NA; Khalbaeva, IV; Koriakin, VA; Sokolova, GB; Ziia, AV, 1993
)
0.5
"For children aged 5 years or more, ethambutol can be recommended at a dosage of 15 mg/kg/day for routine treatment, without taking more precautions than for adults; this should be included in official recommendations."( Should ethambutol be recommended for routine treatment of tuberculosis in children? A review of the literature.
Trébucq, A, 1997
)
1.03
" PZA is significantly dialyzed and should be dosed after hemodialysis."( The effect of hemodialysis on isoniazid, rifampin, pyrazinamide, and ethambutol.
Childs, JM; Fish, DN; Malone, RS; Peloquin, CA; Spiegel, DM, 1999
)
0.54
" Mefloquine had borderline bactericidal activity at a dosage of 40 mg/kg daily (100% inhibition compared with a 1-week control), and significant inhibition was obtained at dosages of 40 mg/kg three times a week, as well as 20 mg/kg daily."( Mefloquine is active in vitro and in vivo against Mycobacterium avium complex.
Aralar, PA; Bermudez, LE; Inderlied, CB; Kolonoski, P; Wu, M; Young, LS, 1999
)
0.3
" Adverse reactions related to rifabutin were a major problem, and for 24 (41%) of 59 patients the dosage was decreased or the drug was withdrawn."( Early results (at 6 months) with intermittent clarithromycin-including regimens for lung disease due to Mycobacterium avium complex.
Brown, BA; Cegielski, P; Griffith, DE; Murphy, DT; Wallace, RJ, 2000
)
0.31
" The following details were recorded: age, sex, and systemic condition of the patients, daily dosage of EMB, duration of EMB treatment, visual function at the time of electrophysiologic investigation, time from the onset of blurred vision to the discontinuation of EMB treatment (symptom duration), and time from termination of EMB treatment until electrophysiologic investigation."( Ethambutol retinal toxicity: an electrophysiologic study.
Chiang, SC; Liu, JH; Wang, AG; Yen, MY, 2000
)
1.75
" The rifampicin and desacetylrifampicin content of complete urinary collections made from 0-4 and 4-8 hours after dosage were determined using both the HPLC and a much simpler colorimetric procedure."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
0.31
" The impairment of visual acuity and the duration of damage were related to the daily dosage significantly."( [Optic nerve neuropathy by ethambutol toxicity].
Chen, L; Liang, Y, 1999
)
0.6
"To prevent the damage of optic nerves by the toxicity of ethambutol, the appropriate small dosage of ethambutol is recommended, regular examination and monitoring of visual function is necessary."( [Optic nerve neuropathy by ethambutol toxicity].
Chen, L; Liang, Y, 1999
)
0.85
" The dissolution characteristics of the extemporaneous powder for suspension were also compared to the dissolution profiles of commercially available anti-tuberculosis tablet dosage forms."( Pharmaceutical formulation of a fixed-dose anti-tuberculosis combination.
Danckwerts, MP; Ebrahim, S; Pillay, V, 2003
)
0.32
"The powder for suspension for rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride all compared favourably to the dissolution rate from the commercially available tablet dosage forms."( Pharmaceutical formulation of a fixed-dose anti-tuberculosis combination.
Danckwerts, MP; Ebrahim, S; Pillay, V, 2003
)
0.55
"9 months) after starting ethambutol therapy at a dosage ranging from 13 to 20 mg/kg/day (mean = 17 mg/kg/day)."( Ethambutol and optic neuropathy.
Chuenkongkaew, W; Samsen, P; Thanasombatsakul, N, 2003
)
2.07
" There was no significant difference in the pharmacokinetic parameters of rifampicin as a component of Mairin-P and in combination with antitubercuous agents as free dosage forms."( [Assessment of the use of a multicomponent drug in the treatment of new cases of pulmonary tuberculosis].
Semenova, OV, 2003
)
0.32
" These findings suggest that P-VECPs in pigmented rats can detect chemically induced visual toxicity even in cases of repeated dosing of a drug."( P-VECP can reveal visual toxicity in pigmented rats of repeated doses of ethambutol.
Iwaki, Y; Kimura, M; Miyata, H; Nakamura, I; Sasaki, S; Yagi, K,
)
0.36
" Liver involvement of tuberculosis can have many facets and may be treated by gradual dosing of standard drugs."( Enlarged cervical lymph nodes and elevated liver chemistry tests: a therapeutic dilemma.
Dietrich, CG; Gartung, C; Geier, A; Lammert, F; Lorenzen, J; Matern, S; Wasmuth, HE,
)
0.13
" Additionally, in terms of management of EMB-induced optic neuropathy, it is important to properly manage ethambutol dosing in patients with renal impairment and to achieve proper transition to a maintenance dose once an appropriate loading dose has been reached."( Optical coherence tomography can measure axonal loss in patients with ethambutol-induced optic neuropathy.
Agarwal, M; Sadun, AA; Zoumalan, CI, 2005
)
0.78
"Integrating combinatorial lead optimization of [1,2]-diamine core structure based on ethambutol with high-throughput screening has led us to focus on three promising analogs (SQ37, SQ59 and SQ109) as potential anti-tubercular drug candidates from thousands of synthesized diamine analogs for further characterization of their biopharmaceutical and pharmacokinetic properties by using liquid chromatography/tandem mass spectrometry (LC/MS/MS) and cassette dosing for pharmacokinetic screening."( Simultaneous estimation of pharmacokinetic properties in mice of three anti-tubercular ethambutol analogs obtained from combinatorial lead optimization.
Glaze, E; Gorman, GS; Jia, L; Noker, PE; Protopopova, M; Tomaszewski, JE, 2005
)
0.78
"Serum drug concentrations were determined 2, 6, and 10 h after dosing in 36 HIV-infected patients with TB who were taking rifampin and in 49 who were taking ethambutol."( The clinical pharmacokinetics of rifampin and ethambutol in HIV-infected persons with tuberculosis.
Hafner, R; Peloquin, CA; Perlman, DC; Rainey, PM; Remmel, RP; Rosenkranz, S; Salomon, N; Segal, Y, 2005
)
0.78
"With daily dosing of rifampin (600 mg), 26 (77%) of 34 patients (95% confidence interval [CI], 59%-89%]) had a low maximum concentration of rifampin (<8 microg/mL), and 12 (35%; 95% CI, 20%-54%) had a very low maximum concentration (<4 microg/mL)."( The clinical pharmacokinetics of rifampin and ethambutol in HIV-infected persons with tuberculosis.
Hafner, R; Peloquin, CA; Perlman, DC; Rainey, PM; Remmel, RP; Rosenkranz, S; Salomon, N; Segal, Y, 2005
)
0.59
" Further studies are required to assess the implications of variations in antituberculosis drug concentrations for efficacy and safety before decisions are made to change the dosing strategy in patients at risk."( Determinants of rifampin, isoniazid, pyrazinamide, and ethambutol pharmacokinetics in a cohort of tuberculosis patients.
Burger, A; Folb, PI; McIlleron, H; Norman, J; Smith, P; Wash, P, 2006
)
0.58
" Alginate nanoparticles hold great potential in reducing dosing frequency of antitubercular drugs."( Pharmacokinetic and pharmacodynamic behaviour of antitubercular drugs encapsulated in alginate nanoparticles at two doses.
Ahmad, Z; Khuller, GK; Pandey, R; Sharma, S, 2006
)
0.33
" Dosing frequency had little effect on 2-mo culture status or tolerability of therapy."( Moxifloxacin versus ethambutol in the first 2 months of treatment for pulmonary tuberculosis.
Burman, WJ; Chaisson, RE; Choudhri, S; Daley, CL; Engle, M; Goldberg, S; Johnson, JL; Mosher, AW; Munsiff, SS; Muzanye, G; Vernon, A; Zhao, Z, 2006
)
0.66
" We concluded that polymeric nanoparticle based oral 4-drug combination bears significant potential to shorten the duration of TB chemotherapy, besides reducing the dosing frequency."( Chemotherapeutic efficacy of nanoparticle encapsulated antitubercular drugs.
Khuller, GK; Pandey, R; Sharma, S,
)
0.13
" Pyridoxine is preventative in low dosage and curative in high dosage."( [Isoniazid induced neuropathy: consider prevention].
De Broucker, T; Martinez-Almoyna, L; Steichen, O, 2006
)
0.33
" Although the advantage of aminoglycosides is easily achieved high blood concentration, if aminoglycoside dosage is exceed 15 mg/kg, the possibility of auditory disturbance increase."( [Perspective of pulmonary MAC infection treatment].
Kurashima, A, 2007
)
0.34
"Patients were treated in a controlled clinical trial with 2HRZE3/6HE with thrice-weekly direct dosing in the intensive phase and once-weekly with six doses self-administered in the continuation phase."( Evaluation of a non-rifampicin continuation phase (6HE) following thrice-weekly intensive phase for the treatment of new sputum positive pulmonary tuberculosis.
, 2007
)
0.34
" In current recommendations the dosage of EMB is calculated per kg body weight."( Ethambutol in paediatric tuberculosis: aspects of ethambutol serum concentration, efficacy and toxicity in children.
Detjen, A; Magdorf, K; Quarcoo, D; Thee, S; Wahn, U, 2007
)
1.78
"To present two studies investigating an appropriate EMB dosage in children, and observational data on its toxicity and efficacy."( Ethambutol in paediatric tuberculosis: aspects of ethambutol serum concentration, efficacy and toxicity in children.
Detjen, A; Magdorf, K; Quarcoo, D; Thee, S; Wahn, U, 2007
)
1.78
" It appears to be more valid to calculate the EMB dosage on the basis of body surface rather than body weight, leading to higher dosages especially in younger children."( Ethambutol in paediatric tuberculosis: aspects of ethambutol serum concentration, efficacy and toxicity in children.
Detjen, A; Magdorf, K; Quarcoo, D; Thee, S; Wahn, U, 2007
)
1.78
"Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing ethambutol dihydrochloride as the only active pharmaceutical ingredient (API) are reviewed."( Biowaiver monographs for immediate release solid oral dosage forms: ethambutol dihydrochloride.
Amidon, GL; Barends, DM; Becker, C; Dressman, JB; Junginger, HE; Kopp, S; Midha, KK; Shah, VP; Stavchansky, S, 2008
)
0.77
"Reduction in the dosing frequency of antituberculosis drugs (ATDs) by applying drug delivery technology has the potential to improve the patient compliance in tuberculosis (TB)."( Alginate nanoparticles as antituberculosis drug carriers: formulation development, pharmacokinetics and therapeutic potential.
Ahmad, Z; Khuller, GK; Pandey, R; Sharma, S,
)
0.13
" We present the six cases; four were clearly overdosed, but in two obese patients dosage was correctly calculated for total body weight (TBW)."( Ethambutol-induced optical neuropathy: risk of overdosing in obese subjects.
Alffenaar, JW; Hasenbosch, RE; Koopmans, SA; Kosterink, JG; van Altena, R; van der Werf, TS, 2008
)
1.79
"Analysis of the case histories and previous reports suggest that optical neuropathy may at least partly be caused by EMB overdosing due to daily dosing based on TBW instead of dosing on lean body mass."( Ethambutol-induced optical neuropathy: risk of overdosing in obese subjects.
Alffenaar, JW; Hasenbosch, RE; Koopmans, SA; Kosterink, JG; van Altena, R; van der Werf, TS, 2008
)
1.79
"Given an understanding of the risk factors for ethambutol optic toxicity, there exists a rationale for an optimization of ethambutol dosing protocols that can maximize the therapeutic effect while minimizing the incidence of optic toxicity."( Risk factors for ethambutol optic toxicity.
Sadun, AA; Talbert Estlin, KA, 2010
)
0.96
" Therapy was performed according to regimens 3 and 1, by using individual dosage regimens depending on the extent and severity of a specific process, the presence of complications, and age-related features."( [Optimization of chemotherapy regimens in children with primary pulmonary tuberculosis].
Dovgaliuk, IF; Ovchinnikova, IuE; Starshinova, AA, 2009
)
0.35
" The following three regimens were administered: regimen A (n = 9) consisted of CAM (400 mg/d), ethambutol (EB) [750 mg/d], and rifampicin (RFP) [450 mg/d]; regimen B (n = 12) consisted of CAM (800 mg/d), EB (750 mg/d), and RFP (450 mg/d); and regimen C (n = 13) consisted of CAM (800 mg/d), EB (1,000 mg/d), and RFP (600 mg/d) during the first 2 months followed by a reduction of the dosage of EB from 1,000 to 750 mg/d."( Therapeutic effects of various initial combinations of chemotherapy including clarithromycin against Mycobacterium avium complex pulmonary disease.
Fukunaga, K; Hasegawa, N; Ishii, K; Ishizaka, A; Miyairi, M; Nishimura, T; Ohtani, S; Takeshita, K; Tasaka, S; Urano, T, 2009
)
0.57
"6%), which included a daily dosage of 400 mg of CAM (9."( Therapeutic effects of various initial combinations of chemotherapy including clarithromycin against Mycobacterium avium complex pulmonary disease.
Fukunaga, K; Hasegawa, N; Ishii, K; Ishizaka, A; Miyairi, M; Nishimura, T; Ohtani, S; Takeshita, K; Tasaka, S; Urano, T, 2009
)
0.35
" The current World Health Organization (WHO) guidelines recommend an oral dosage of 10 (8-12) mg per kg body weight."( Rifampicin serum levels in childhood tuberculosis.
Detjen, A; Magdorf, K; Thee, S; Wahn, U, 2009
)
0.35
" In children, it appears to be more valid to calculate RMP dosage on the basis of body surface area rather than body weight, leading to higher dosages especially in younger children."( Rifampicin serum levels in childhood tuberculosis.
Detjen, A; Magdorf, K; Thee, S; Wahn, U, 2009
)
0.35
"Therapeutic drug monitoring allows to determine the best dosage regimen adapted to each patient optimizing the therapeutic benefits, while minimizing the risk for side effects."( Determination of antituberculosis drug concentration in human plasma by MALDI-TOF/TOF.
Ascenzi, P; Bevilacqua, N; Gullotta, F; Lauria, FN; Mancone, C; Notari, S; Pucillo, LP; Sergi, M; Tempestilli, M; Tripodi, M; Urso, R, 2010
)
0.36
"A questionnaire regarding what antitubercular drugs, their dosage and for how long was asked to attending faculty in an International Conference on musculoskeletal infections."( A survey of prescribing pattern for osteoarticular tuberculosis: orthopaedic surgeons' and infectious disease experts' perspective.
Agarwal, A; Arora, A; Kumar, S, 2009
)
0.35
" A dosage adjustment of bisoprolol is necessary if the clinical status of the patient requires treatment with the antituberculosis drug rifampicin."( [Urinary bladder tuberculosis and Bacillus Calmette-Guérin instillation: reduced efficacy of bisoprolol in hypertension].
Drechsler, A; Kirch, W, 2010
)
0.36
" Use of pharmacodynamic/pharmacokinetic models has resulted in design of new doses and dosing schedules for disseminated MAC, as well as new susceptibility breakpoints for ethambutol and moxifloxacin."( Pharmacokinetic/pharmacodynamic-based treatment of disseminated Mycobacterium avium.
Deshpande, D; Gumbo, T, 2011
)
0.56
" The better results of lowering serum uric acid and protecting against renal failure were at the dosage of Que between 10 and 20 mg/kg."( [Preventive and therapeutic effects of quercetin on hyperuricemia and renal injury in rats].
Fu, R; He, W; Yao, F; Zhang, R, 2011
)
0.37
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Rifampicin concentrations during the dosing interval were determined by HPLC at three different timepoints: (i) after 2 weeks of TB therapy and before starting HIV therapy (T0); (ii) after 4 weeks of combined therapy (T1); and (iii) after 10 weeks of combined therapy (T2)."( Systemic exposure to rifampicin in patients with tuberculosis and advanced HIV disease during highly active antiretroviral therapy in Burkina Faso.
Bonkoungou, V; Carvalho, AC; Comelli, M; Cusato, M; Dembélé, SM; Kouanda, S; Matteelli, A; Nacanabo, R; Regazzi, M; Saleri, N; Villani, P, 2012
)
0.38
" Thus, new and individualized ethambutol dosing regimens need to be designed for obese and extremely obese patients."( Ethambutol pharmacokinetic variability is linked to body mass in overweight, obese, and extremely obese people.
Gumbo, T; Hall, RG; Leff, RD; Meek, C; Swancutt, MA, 2012
)
2.11
" In this article, a case series is presented to illustrate the value of individualized TB drug dosing in four patients with low TB drug concentrations."( Therapeutic drug monitoring in the treatment of tuberculosis patients.
Aarnoutse, R; Boeree, M; Ijdema, D; Magis-Escurra, C; van den Boogaard, J, 2012
)
0.38
" Average CAM dosage was increased from the early (517 mg/day) to the later (800 mg/day) period."( Relationship between clinical efficacy for pulmonary MAC and drug-sensitivity test for isolated MAC in a recent 6-year period.
Abe, M; Kato, S; Kobashi, Y; Mouri, K; Obase, Y; Oka, M, 2012
)
0.38
" Trials of new drugs and new dosing strategies are needed."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
0.38
" New dosing strategies for rifampicin and ethambutol should be studied to increase the exposure to these drugs and thus maximise their impact."( Synergistic activity of rifampicin and ethambutol against slow-growing nontuberculous mycobacteria is currently of questionable clinical significance.
Boeree, MJ; Hoefsloot, W; Mouton, JW; van Ingen, J; van Soolingen, D, 2013
)
0.92
" The administration of tacrolimus (1 mg) was started as the dosage of oral glucocorticoids was tapered."( Paradoxical response to disseminated non-tuberculosis mycobacteriosis treatment in a patient receiving tumor necrosis factor-α inhibitor: a case report.
Imamura, Y; Izumikawa, K; Kakeya, H; Kohno, S; Miyazaki, T; Nakamura, S; Takazono, T; Yanagihara, K, 2014
)
0.4
" This study demonstrates notable individual variability, indicating that dosing of these medications requires individual monitoring and provides additional information to guide the clinician when treating elephants."( The pharmacokinetics of a single oral or rectal dose of concurrently administered isoniazid, rifampin, pyrazinamide, and ethambutol in Asian elephants (Elephas maximus).
Egelund, EF; Hunter, RP; Isaza, R; P Brock, A; Peloquin, CA, 2014
)
0.61
"Patients were enrolled in a single-arm clinical trial to receive intermittent dosing after at least 14 initial daily doses of RMP+PZA+EMB."( Intermittent tuberculosis treatment for patients with isoniazid intolerance or drug resistance.
Bock, N; Bozeman, L; Goldberg, SV; Hamilton, CD; Heilig, CM; Hershfield, E; Kyle, RP; Narita, M; Reves, R; Tapy, JM; Wing, D, 2014
)
0.4
" BIW dosing was used in 77 and TIW in 21."( Intermittent tuberculosis treatment for patients with isoniazid intolerance or drug resistance.
Bock, N; Bozeman, L; Goldberg, SV; Hamilton, CD; Heilig, CM; Hershfield, E; Kyle, RP; Narita, M; Reves, R; Tapy, JM; Wing, D, 2014
)
0.4
" There was a nonlinear increase in exposure to rifampin without an apparent ceiling effect and a greater estimated fall in bacterial load in the higher dosing groups."( A dose-ranging trial to optimize the dose of rifampin in the treatment of tuberculosis.
Aarnoutse, RE; Boeree, MJ; Burger, D; Dawson, R; Diacon, AH; du Bois, J; Gillespie, SH; Heinrich, N; Hoelscher, M; Magis-Escurra, C; McHugh, TD; Narunsky, K; Phillips, PP; Plemper van Balen, G; Rehal, S; van Ingen, J; van Soolingen, D; Venter, A, 2015
)
0.42
"Current guidelines for dosing of anti-TB drugs in children advocate higher doses for rifampicin and isoniazid despite limited availability of paediatric data on the pharmacokinetics of these drugs, especially from Africa, where the burden of childhood disease remains high."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
0.64
" Rifampicin, isoniazid, pyrazinamide and ethambutol were dosed at 10, 5, 25 and 20 mg/kg, respectively."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
0.91
" Predicted AUC0 -∞ for rifampicin dosed at 15 mg/kg was comparable to that of adults while the dose required to achieve ethambutol exposure similar to that in adults was 55 mg/kg or higher."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
0.85
"These data support recently revised WHO recommendations for dosing of anti-TB drugs in children, but dosing of ethambutol in children also appears inadequate by comparison with adult pharmacokinetic data."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
0.85
" Drugs like tetrandrine may help to reduce drug dosage thus alleviate side effects."( Tetrandrine reverses drug resistance in isoniazid and ethambutol dual drug-resistant Mycobacterium tuberculosis clinical isolates.
Ji, Z; Li, L; Xu, K; Yan, J; Zhang, Z, 2015
)
0.67
" We conducted this study with the aims of determining the plasma concentrations of isoniazid, rifampicin, pyrazinamide and ethambutol achieved with different dosage of the anti-tubercular drugs so as to provide supportive evidence to the revised dosages and to evaluate the effects of malnutrition on the pharmacokinetics of these drugs in children."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
0.87
"Prospective drug estimation study was conducted in two groups of children, age 6 months to 15 years, with tuberculosis, with or without severe malnutrition, receiving different dosage of daily anti- tubercular therapy."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
0.66
"7%) children in the two dosing regimen, respectively."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
0.66
" On the basis of limited experience, the combination of tube thoracostomy or catheter drainage and high-end dosing of anti-TB drugs has been recommended as an initial approach to these lesions."( Therapeutic drug monitoring and the conservative management of chronic tuberculous empyema: case report and review of the literature.
Barrie, J; Long, R; Peloquin, CA, 2015
)
0.42
" He was treated with computed tomography-guided catheter drainage and TDM-guided high-end dosed anti-TB drugs (serum and pleural fluid drug concentrations) over a 10 month period."( Therapeutic drug monitoring and the conservative management of chronic tuberculous empyema: case report and review of the literature.
Barrie, J; Long, R; Peloquin, CA, 2015
)
0.42
" The range of dosage was 15-19 mg/kg/day."( Visual function test for early detection of ethambutol induced ocular toxicity at the subclinical level.
Kim, KL; Park, SP, 2016
)
0.7
"The dosing of drugs in critically ill patients undergoing renal replacement therapy is based on limited data."( Single- and multiple-dose pharmacokinetics of ethambutol and rifampicin in a tuberculosis patient with acute respiratory distress syndrome undergoing extended daily dialysis and ECMO treatment.
Ciesek, S; Hoeper, MM; Kielstein, JT; Kühn, C; Schmidt, JJ; Strunk, AK; Welte, T, 2016
)
0.69
" We pooled data by study quality, design, region, dosing modality and patient characteristics."( Therapeutic drug monitoring in anti-tuberculosis treatment: a systematic review and meta-analysis.
Al-Efraij, K; Campbell, JR; Cook, VJ; Johnston, J; Marra, F; Mota, L, 2016
)
0.43
" These findings point to a discrepancy between accepted 2 h TDM thresholds and TB drug dosing recommendations."( Therapeutic drug monitoring in anti-tuberculosis treatment: a systematic review and meta-analysis.
Al-Efraij, K; Campbell, JR; Cook, VJ; Johnston, J; Marra, F; Mota, L, 2016
)
0.43
" Coadministration of Kaletra (lopinavir/ritonavir) with delamanid resulted in an approximately 25% higher delamanid area under the concentration-time curve from time 0 to the end of the dosing interval (AUCτ)."( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects.
Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016
)
0.43
" The aim of this analysis was to characterize factors contributing to the variability in exposure and to evaluate drug exposures using alternative doses, thus providing evidence to support revised dosing recommendations for drug-susceptible and multidrug-resistant tuberculosis (MDR-TB)."( Pharmacokinetics of Pyrazinamide and Optimal Dosing Regimens for Drug-Sensitive and -Resistant Tuberculosis.
Chirehwa, MT; Denti, P; McIlleron, H; Mthiyane, T; Onyebujoh, P; Rustomjee, R; Smith, P, 2017
)
0.46
" There is an urgent need to improve the current therapy so as to reduce treatment duration and dosing frequency."( Nano-Formulation of Ethambutol with Multifunctional Graphene Oxide and Magnetic Nanoparticles Retains Its Anti-Tubercular Activity with Prospects of Improving Chemotherapeutic Efficacy.
Bhakta, S; Chrzastek, A; Fakurazi, S; Hussein, MZ; Maitra, A; Naeemullah, B; Saifullah, B, 2017
)
0.78
" Its treatment is complicated by patients' noncompliance due to dosing frequency, lengthy treatment, and adverse side effects associated with current chemotherapy."( Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide.
Bhakta, S; Chrzastek, A; Fakurazi, S; Hussein, MZ; Maitra, A; Naeemullah, B; Saifullah, B, 2017
)
0.71
" As irrational use and inadequate dosing of anti-TB drugs may contribute to the epidemic of drug-resistant TB, we assessed the drug types and dosages prescribed in the treatment of TB cases in a representative sample of health care facilities in Yunnan."( Prescription practice of anti-tuberculosis drugs in Yunnan, China: A clinical audit.
Chen, J; Chiang, CY; Innes, AL; Li, L; Xu, L, 2017
)
0.46
" Outcomes of interest included the regimen used in the treatment of new and retreatment TB patients; and the proportion of patients treated with adequate dosing of anti-TB drugs."( Prescription practice of anti-tuberculosis drugs in Yunnan, China: A clinical audit.
Chen, J; Chiang, CY; Innes, AL; Li, L; Xu, L, 2017
)
0.46
" The ability of dosed TB drugs to reach and sterilize bacteria within poorly-vascularized necrotic regions (caseum) of pulmonary granulomas is crucial for successful therapeutic intervention."( Spatial Quantification of Drugs in Pulmonary Tuberculosis Lesions by Laser Capture Microdissection Liquid Chromatography Mass Spectrometry (LCM-LC/MS).
Blanc, L; Chen, PY; Dartois, V; Prideaux, B; Zimmerman, M, 2018
)
0.48
"Paraguayan children were treated according to the revised paediatric dosing scheme of the World Health Organization."( Evaluation of dried blood spot sampling for pharmacokinetic research and therapeutic drug monitoring of anti-tuberculosis drugs in children.
Aarnoutse, RE; Aguirre, S; Alffenaar, JW; Chaparro, G; Coronel, R; Gomez, R; Gonzalez, F; Huisman, J; Jongedijk, E; Kerkhoff, J; Magis-Escurra, C; Martial, LC; Martinez, N; Molinas, G; Pérez, D; Rodríguez, M; Roman, M; Touw, DJ, 2018
)
0.48
"Our findings showed that NPs gave sustained release of drugs inside plasma and organs, thus decreasing dosage frequency, and their weekly dosage had therapeutic efficacy equivalent to daily dosage of free drugs."( Therapeutic implications of nano-encapsulated rifabutin, azithromycin & ethambutol against experimental
Grewal, TK; Majeed, S; Sharma, S, 2018
)
0.71
" We evaluated plasma drug concentrations of rifampicin (RIF), isoniazid (INH), pyrazinamide (PZA), and ethambutol (EMB) among children undergoing TB treatment in Tanzania when these dosing recommendations were being implemented."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
0.77
" Differences in median drug concentrations were compared on the basis of the weight-based dosing strategy using the Mann-Whitney U test."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
0.56
"Among this cohort of human immunodeficiency virus-negative Tanzanian children, use of the revised dosing strategy for treating childhood TB did not result in the target drug concentration for RIF, INH, or EMB being reached."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
0.56
"To perform a population pharmacokinetic study of ethambutol in HIV/TB patients, and to evaluate an intensified ethambutol weight-based dosing strategy to support pharmacokinetic target attainment."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.16
" Monte Carlo simulations were performed to compare pharmacokinetic target attainment under standard and intensified weight-based ethambutol dosing strategies."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.11
" Supplementary ethambutol dosing among HIV/TB patients may provide a strategy to optimize anti-TB treatment regimens in this high-risk population."( Optimizing ethambutol dosing among HIV/tuberculosis co-infected patients: a population pharmacokinetic modelling and simulation study.
Bisson, GP; Gumbo, T; Ivaturi, V; Mehta, K; Modongo, C; Pasipanodya, JG; Ravimohan, S; Srivastava, S; Vinnard, C; Weissman, D; Zetola, NM, 2019
)
1.26
" Based on the guidelines of the American Thoracic Society, she was started on weight-based dosing of clarithromycin, levofloxacin, ethambutol, isoniazid and injection amikacin daily."( Pulmonary
Gopalan, N; Hanna, LE; Joseph, B; Kannayan, S; Padmapriyadarsini, C; Perumal, BK; Saranathan, R; Sivaramakrishnan, GN,
)
0.34
" Further studies are needed to identify appropriate regimens with adequate dosing of ATT for the management of paediatric TBM to improve treatment outcomes."( Tuberculous meningitis in children: Clinical management & outcome.
Daniel, BD; Grace, GA; Natrajan, M, 2019
)
0.51
"Linezolid is increasingly used for the treatment of tuberculosis resistant to first-line agents, but the most effective dosing strategy is yet unknown."( Fourteen-Day Bactericidal Activity, Safety, and Pharmacokinetics of Linezolid in Adults with Drug-Sensitive Pulmonary Tuberculosis.
Burger, DA; Dawson, R; De Jager, VR; Diacon, AH; Everitt, D; Mendel, CM; Narunsky, K; Nedelman, J; Pappas, F; Vanker, N, 2020
)
0.56
" New data on optimal drug selection and dosing are emerging with the inclusion of children in clinical trials and ongoing research on age-related pharmacokinetics and pharmacodynamics."( Tuberculosis treatment in children: The changing landscape.
Huynh, J; Marais, BJ; Schaaf, HS; Thwaites, G, 2020
)
0.56
"To allow for tailored dosing and overcome swallowing difficulties, compounded liquid medication is often required in pediatric patients."( Stability of Azathioprine, Clonidine Hydrochloride, Clopidogrel Bisulfate, Ethambutol Hydrochloride, Griseofulvin, Hydralazine Hydrochloride, Nitrofurantoin, and Thioguanine Oral Suspensions Compounded with SyrSpend SF pH4.
Anagnostou, K; Cunha, CN; da Silva, SL; Dijkers, E; Ferreira, AO; Polonini, H,
)
0.36
" Mean daily dosage of EMB was 17."( Prospective study to evaluate incidence and indicators for early detection of ethambutol toxicity.
Dhiman, R; Guleria, R; Mandal, S; Mohan, A; Padhy, SK; Phuljhele, S; Saxena, R; Sharma, P, 2021
)
0.85
" Blood sampling was also performed 120  minutes after dosing for the detection of Cmax purpose."( Effect of interval between food intake and drug administration at fasting condition on the plasma concentrations of first-line anti-tuberculosis drugs in Chinese population.
Chu, N; Du, Y; Guo, R; Han, X; Pang, Y; Wang, J; Wang, Q, 2020
)
0.56
"Optimal dosing of children with tuberculous meningitis (TBM) remains uncertain and is currently based on the treatment of pulmonary tuberculosis in adults."( Population Pharmacokinetic Properties of Antituberculosis Drugs in Vietnamese Children with Tuberculous Meningitis.
Bang, ND; Day, JN; Hoglund, RM; Ngo, VN; Nosoongnoen, W; Panjasawatwong, N; Pouplin, T; Tarning, J; Wattanakul, T, 2020
)
0.56
"In 2010, the World Health Organization (WHO) revised dosing guidelines for treatment of childhood tuberculosis."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
0.72
" Nonlinear mixed-effects modeling and simulation was used to design the optimal FDC and weight-band dosing strategy for achieving the pharmacokinetic targets based on literature-derived adult AUC0-24h for rifampicin (38."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
0.72
" Optimal dosing of all drugs cannot be achieved with the current FDCs."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
0.72
" Although ethambutol has been demonstrated to inhibit macrolide resistance, the ethambutol dosage is sometimes decreased due to concerns about optic neuropathy."( Low-dosage ethambutol, less than 12.5 mg/kg/day, does not worsen the clinical outcomes of pulmonary Mycobacterium avium and Mycobacterium intracellulare disease: a retrospective cohort study.
Fujiwara, K; Furuuchi, K; Hanada, K; Kaburaki, S; Kurashima, A; Morimoto, K; Ohta, K; Shiraishi, Y; Tanaka, Y; Uesugi, F; Watanabe, F; Yoshiyama, T, 2022
)
1.51
" Daily ethambutol dosage was not identified as a prognostic factor for any of the outcomes."( Low-dosage ethambutol, less than 12.5 mg/kg/day, does not worsen the clinical outcomes of pulmonary Mycobacterium avium and Mycobacterium intracellulare disease: a retrospective cohort study.
Fujiwara, K; Furuuchi, K; Hanada, K; Kaburaki, S; Kurashima, A; Morimoto, K; Ohta, K; Shiraishi, Y; Tanaka, Y; Uesugi, F; Watanabe, F; Yoshiyama, T, 2022
)
1.57
"An ethambutol dosage of 12."( Low-dosage ethambutol, less than 12.5 mg/kg/day, does not worsen the clinical outcomes of pulmonary Mycobacterium avium and Mycobacterium intracellulare disease: a retrospective cohort study.
Fujiwara, K; Furuuchi, K; Hanada, K; Kaburaki, S; Kurashima, A; Morimoto, K; Ohta, K; Shiraishi, Y; Tanaka, Y; Uesugi, F; Watanabe, F; Yoshiyama, T, 2022
)
1.73
" We describe the population pharmacokinetics of ethambutol in children with TB to guide dosing in this population."( Population pharmacokinetics of ethambutol in African children: a pooled analysis.
Abdelwahab, MT; Andrieux-Meyer, I; Bekker, A; Chabala, C; Cotton, MF; Davies, G; Denti, P; Hesseling, A; Lee, J; McIlleron, H; Rabie, H; Tikiso, T; Wiesner, L; Zar, HJ, 2022
)
1.26
"We performed (1) minimum inhibitory concentration experiment, (2) isoniazid dose-response study using the hollow fiber system model (HFS-Mkn) to determine PK/PD optimized exposure, and (3) another HFS-Mkn study to determine the efficacy of high dose isoniazid (15 mg/kg/day) with standard dose rifampin (10 mg/kg/day) and ethambutol (15 mg/kg/day)."( Isoniazid pharmacokinetics/pharmacodynamics as monotherapy and in combination regimen in the hollow fiber system model of Mycobacterium kansasii.
Boorgula, GD; Gumbo, T; Heysell, SK; Shankar, P; Singh, S; Srivastava, S, 2023
)
1.08
"36 kg, mean daily dosage of ethambutol was 17."( Ocular toxicity among patients taking anti-tubercular treatment.
Chapagain, S; Dahal, HN; Sitaula, RK; Sitaula, S; Thapa, S, 2022
)
1.02
" Duration between optic nerve toxicity , usage of ethambutol and the drug dosage were noted."( Ethambutol induced toxic optic neuropathy - A retrospective study in a tertiary eye care centre in Southern India.
Balakrishnan, HK; Jayasri, KN; Kowsalya, A; Sajja, S; Shanmugam, MK, 2022
)
2.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antitubercular agentA substance that kills or slows the growth of Mycobacterium tuberculosis and is used in the treatment of tuberculosis.
environmental contaminantAny minor or unwanted substance introduced into the environment that can have undesired effects.
xenobioticA xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
[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]

Drug Classes (2)

ClassDescription
ethanolamines
ethylenediamine derivativeAny organic amino compound that is a derivative of ethylenediamine.
[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 Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvMIC3.12501.56004.69839.4100AID1698034
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (971)

Assay IDTitleYearJournalArticle
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID540875Antibacterial activity against Mycobacterium tuberculosis Rv18 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1687560Antitubercular activity against PAS/INH/EMB/RMP-resistant Mycobacterium tuberculosis Spec.210 assessed as inhibition of microbial growth by classical test tube method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID1333278Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 4 times MIC measured after 6 hrs by luciferase reporter gene assay (Rvb = 212.7%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1698035Cytotoxicity against human HEK293 cells assessed as inhibition of cell growth at 25 uM incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design and synthesis of new indanol-1,2,3-triazole derivatives as potent antitubercular and antimicrobial agents.
AID405182Tmax in tuberculosis patient at 750 mg, po coadministered with 450 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID145296Tested for antibacterial activity against Mycobacterium tuberculosis H37Rv kanamycin resistant strain1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID569261Antimicrobial activity against methicillin-resistant Staphylococcus aureus 8732011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1501037Antitubercular activity against Mycobacterium tuberculosis H37Rv by Lowensteine-Jensen method2017European journal of medicinal chemistry, Oct-20, Volume: 139Recent advances of pyrazole-containing derivatives as anti-tubercular agents.
AID439075Antitubercular activity against drug-sensitive Mycobacterium tuberculosis by radiometric BACTEC460 method2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and evaluation of (S,S)-N,N'-bis-[3-(2,2',6,6'-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.
AID495228Antimicrobial activity against Mycobacterium tuberculosis 32C3 harboring embB497 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1765358Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID1143263Antimycobacterial activity against Mycobacterium tuberculosis Beijing (E-47/94) assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID569255Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID736913Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by fluorescence assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Antimycobacterial activity evaluation, time-kill kinetic and 3D-QSAR study of C-(3-aminomethyl-cyclohexyl)-methylamine derivatives.
AID1467546Antimicrobial activity against Mycobacterium tuberculosis H37Rv by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
One-pot microwave assisted stereoselective synthesis of novel dihydro-2'H-spiro[indene-2,1'-pyrrolo-[3,4-c]pyrrole]-tetraones and evaluation of their antimycobacterial activity and inhibition of AChE.
AID559763Antimycobacterial activity against Mycobacterium smegmatis MC2 155 harboring PknG K181M mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID1463961Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 7357/1998 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1862168Antimycobacterial activity against Mycobacterium tuberculosis variant bovis BCG for 7 days by resazurin-based microdilution assay2022Bioorganic & medicinal chemistry, 09-01, Volume: 69Synthesis and evaluation of inhibitors of Mycobacterium tuberculosis UGM using bioisosteric replacement.
AID765271fAUC/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID588215FDA HLAED, alkaline phosphatase increase2004Current 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.
AID1463960Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 234/2005 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID540907Antibacterial activity against HYG cassette-negative EMB-resistant Mycobacterium tuberculosis B52 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID495229Antimicrobial activity against Mycobacterium tuberculosis 32C4 harboring embB497 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID143719In vitro antibacterial activity of compound against Mycobacterium avium MAC ATCC 157692002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID540898Antibacterial activity against Mycobacterium tuberculosis B92 harboring embB GAC-GCC (D354A) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1331132Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 28 days by MABA method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Design, development of new synthetic methodology, and biological evaluation of substituted quinolines as new anti-tubercular leads.
AID540899Antibacterial activity against HYG cassette-negative EMB-resistant Mycobacterium tuberculosis Rv8 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1589053Antimycobacterial against Mycobacterium tuberculosis H37Rv incubated for 7 days by MABA assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
5-Chloro-2-thiophenyl-1,2,3-triazolylmethyldihydroquinolines as dual inhibitors of Mycobacterium tuberculosis and influenza virus: Synthesis and evaluation.
AID1687469Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID627940Binding affinity to Mycobacterium tuberculosis fatty acid synthase 1 at 500 uM by STD NMR spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Pyrazinamide, but not pyrazinoic acid, is a competitive inhibitor of NADPH binding to Mycobacterium tuberculosis fatty acid synthase I.
AID1204851Antitubercular activity against Isoniazid-resistant Mycobacterium tuberculosis assessed as parasite growth inhibition by REMA method2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID540873Antibacterial activity against Mycobacterium tuberculosis B59 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID565993Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by twofold agar dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID540910Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis B5202 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID540868Antibacterial activity against Mycobacterium tuberculosis B56 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1403710Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 25 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID599274Cytotoxicity against human MRC5 cells assessed as cell viability at 100 uM after 72 hrs by XTT assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID562268Antimicrobial activity against Mycobacterium tuberculosis harboring Mycobacterium smegmatis embB M292V mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1435842Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by resazurin reduction microplate assay2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID285161Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID1263164Antituberculosis activity against Mycobacterium tuberculosis H37Rv MTCC 300 at 6.25 ug/ml after 4 weeks by Lowenstein-Jensen medium method2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Pyrazole clubbed triazolo[1,5-a]pyrimidine hybrids as an anti-tubercular agents: Synthesis, in vitro screening and molecular docking study.
AID251785Antimycobacterial activity of compound against Mycobacterium tuberculosis H37Rv at 1.88 ug/mL2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Antituberculous activity of some aryl semicarbazone derivatives.
AID294761Antibacterial activity against Staphylococcus aureus after 2 weeks by broth dilution method2007Bioorganic & 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.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug 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.
AID1916620Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition measured after 7 days by broth microdilution assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1439666Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
A robust synthesis of functionalized 2H-indazoles via solid state melt reaction (SSMR) and their anti-tubercular activity.
AID633936Antimycobacterial activity against multiple drug-resistant Mycobacterium tuberculosis isolate T113 by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Mefloquine-oxazolidine derivatives, derived from mefloquine and arenecarbaldehydes: In vitro activity including against the multidrug-resistant tuberculosis strain T113.
AID502043Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATTC 27294 by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas.
AID1071121Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 3.13 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1071108Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 12.5 to 50 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID425190Antimycobacterial activity against multi drug-resistant Mycobacterium tuberculosis2009Bioorganic & 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.
AID522854Cytotoxicity against human THP1 cells2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
AID1756892Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC27294 measured after 28 days by two-fold serial dilution method2021European journal of medicinal chemistry, Apr-05, Volume: 215Antitubercular properties of thiazolidin-4-ones - A review.
AID1076894Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition at 50 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Development of antimycobacterial tetrahydrothieno[2,3-c]pyridine-3-carboxamides and hexahydrocycloocta[b]thiophene-3-carboxamides: Molecular modification from known antimycobacterial lead.
AID599246Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 after 3 days by MTT assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID1864508Substrate uptake at human OCT3 overexpressed in HEK293 cells incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1174110Antimycobacterial activity against isoniazid, rifampin, streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1204850Antitubercular activity against Rifampicin-resistant Mycobacterium tuberculosis assessed as parasite growth inhibition by REMA method2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID540905Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis Rv4401 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID444318Cytotoxicity against mouse J774 cells assessed as cell viability at 10 ug/ml by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID1072706Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2014Bioorganic & 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.
AID1333106Antimycobacterial activity against Mycobacterium smegmatis MC2 155 after 24 hrs by broth dilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1391359Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Dibenzofuran, dibenzothiophene and N-methyl carbazole tethered 2-aminothiazoles and their cinnamamides as potent inhibitors of Mycobacterium tuberculosis.
AID1854284Antitubercular 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 assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID1383956Bactericidal activity against MDR Mycobacterium tuberculosis isolate 591 after 4 weeks by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID1577333Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 9449/2007 after 21 days2019Journal 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.
AID664309Antituberculosis activity against Mycobacterium tuberculosis H37Rv at 6.25 ug/ml by BACTEC MGIT method2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents.
AID433905Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar microdilution assay2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antitubercular screening of imidazole derivatives.
AID565649Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC M300V mutant gene after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID440895Antimycobacterial activity against multidrug resistant Mycobacterium smegmatis MC2 by agar dilution method2009European 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.
AID1488485Selectivity index, ratio of CC50 for Swiss mouse BMDM to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents.
AID565646Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC M300L mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID448381Cytotoxicity against mouse J774 macrophage assessed as cell viability at 1 ug/mL after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
AID540885Antibacterial activity against Mycobacterium tuberculosis B70 harboring embB ATG-ATC (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1437019Antimycobacterial activity against isoniazid/rifampicin/ethambutol-sensitive Mycobacterium tuberculosis H37Rv after 4 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
AID1484392Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by NCCLS method2017European journal of medicinal chemistry, Jun-16, Volume: 133Isoniazid derivatives and their anti-tubercular activity.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID534422Antibacterial activity against Mycobacterium bovis BCG-japan2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1594637Antimycobacterial activity against Mycobacterium tuberculosis assessed as inhibition of parasite growth at 1 ug/ml incubated for 6 days by REMA method relative to untreated control2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1240997Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 days by MTT assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Guanidinium compounds with sub-micromolar activities against Mycobacterium tuberculosis. Synthesis, characterization and biological evaluations.
AID1071102Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID143718In vitro antibacterial activity of compound against Mycobacterium avium MAC ANI (wild type strain) isolated from infected patients.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID540900Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis Rv8100 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID588214FDA HLAED, liver enzyme composite activity2004Current 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.
AID333645Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 0.006 mg/ml by rapid radiometric method2004Journal of natural products, Nov, Volume: 67, Issue:11
Antibacterial activity of naphthoquinones and triterpenoids from Euclea natalensis root bark.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current 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.
AID1224523Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 1 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-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.
AID775976Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 28 days by agar dilution method2013European journal of medicinal chemistry, Nov, Volume: 69Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID1696664Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth by MABA assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design and synthesis of purine connected piperazine derivatives as novel inhibitors of Mycobacterium tuberculosis.
AID1312205Antibacterial activity against actively replicative Mycobacterium tuberculosis H37Rv measured after 7 days by MABA assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors.
AID1609004Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ITM-M006710 after 48 hr by resazurin dye based microdilution method2019European journal of medicinal chemistry, Nov-01, Volume: 181Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID294765Antibacterial activity against methicillin-resistant Staphylococcus aureus 910 after 2 weeks by broth dilution method2007Bioorganic & 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.
AID289147Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID1372630Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition at 25 uM after 48 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID445329Cytotoxicity against human THP1 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1609005Antimycobacterial activity against Mycobacterium aurum DSM 43999 after 72 hr by resazurin dye based microdilution method2019European journal of medicinal chemistry, Nov-01, Volume: 181Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.
AID765269fT>MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1464087Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue staining based assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
meso-Dihydroguaiaretic acid derivatives with antibacterial and antimycobacterial activity.
AID565651Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC T270I mutant gene after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID574591Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 obtained from pus of patient at 5 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial 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.
AID1374425Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by REMA2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Synthesis, antimicrobial activity and acid dissociation constants of methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives.
AID594795Antituberculosis activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & 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.
AID1738816Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth incubated for 1 week by alamar blue based assay2020European journal of medicinal chemistry, Aug-01, Volume: 199Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
AID670864Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar diffusion method2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Synthesis and in vitro antitubercular activity of 4-aryl/alkylsulfonylmethylcoumarins as inhibitors of Mycobacterium tuberculosis.
AID1272622Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 21 days by broth microdilution method2016Bioorganic & 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.
AID562265Antimicrobial activity against Mycobacterium tuberculosis harboring Mycobacterium smegmatis embB gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID632212Antituberculosis activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis.
AID495205Antimicrobial activity against wild type Mycobacterium tuberculosis 8C1 after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1266237Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by alamar blue assay2016Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.
AID285160Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID540872Antibacterial activity against Mycobacterium tuberculosis Rv8 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID117753Antitubercular activity (100 mg/kg) in the 31-day murine model1981Journal 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.
AID1193922Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & 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.
AID117756Antitubercular activity (12.5 mg/kg) in the 31-day murine model1981Journal 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.
AID1706863Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current 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.
AID522850Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as extracellular bacterial killing2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
AID1058227Antimycobacterial activity against Mycobacterium fortuitum2013Bioorganic & 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.
AID540889Antibacterial activity against Mycobacterium tuberculosis Rv10 harboring embB TTC-CTC (F320L) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID421756Antibacterial activity against Mycobacterium fortuitum after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID729739Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antitubercular activity of amino alcohol fused spirochromone conjugates.
AID562258Antimicrobial activity against Mycobacterium smegmatis expressing EmbC D280G mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID559767Antimycobacterial activity against Mycobacterium smegmatis harboring PknG Msm gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID370071Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35822 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID529525Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis isolate NJT210EMB-R-C1 assessed as bacterial colony formation at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID445334Selectivity for Mycobacterium tuberculosis H37Rv over human MRC5 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID444317Cytotoxicity against mouse J774 cells infected with Mycobacterium bovis BCG assessed as cell viability at 1 ug/ml by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID1706865Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID454542Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
A highly atom economic, chemo-, regio- and stereoselective synthesis and evaluation of spiro-pyrrolothiazoles as antitubercular agents.
AID1602928Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1400027Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC100 for replicating Mycobacterium tuberculosis H37Rv by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1069174Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by BacTiter-Glo assay2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1294351Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by BacTiter-Glo cell viability assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID1163978Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID441083Antimycobacterial activity against Mycobacterium tuberculosis CIB99 after 5 to 7 days by microplate alamar blue assay2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID540882Antibacterial activity against Mycobacterium tuberculosis B95 harboring embB ATG-ATA (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1315652Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured daily for 8 days by GFP-based fluorescence assay2016Journal of natural products, 06-24, Volume: 79, Issue:6
Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178.
AID574809Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 horboring rpoB H526Y, katG D329A/R463L, gyrA D94G/S95T, rrs A1401G by CLSI method2010Antimicrobial 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.
AID1180392Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 50 uM after 72 hrs by MTT assay2014Bioorganic & 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.
AID562263Antimicrobial activity against Mycobacterium tuberculosis embA gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID523292Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as 2 log reduction in bacterial burden in lungs orally treated in water-1% methylcellulose upto 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID144139Antibacterial activity against Mycobacterium intracellular.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID540884Antibacterial activity against Mycobacterium tuberculosis B97 harboring embB ATG-ATC (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID370118Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 4 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current 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.
AID540924Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis BAS7 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1202003Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in Swiss mouse assessed as lung bacterial colony forming units at 10 mg/kg, po dosed daily for 28 days measured up to day 40 (Rvb = 31 10'7 CFU)2015European journal of medicinal chemistry, May-05, Volume: 95Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis.
AID658541Antimycobacterial activity against Mycobacterium smegmatis MC2 2700 expressing Mycobacterium tuberculosis fatty acid synthase 1 gene after 72 hrs by MTT assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antibacterial acylphloroglucinols from Hypericum olympicum.
AID1891918Antimycobacterial activity against Streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 35820 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1174927Antitubercular activity against Mycobacterium tuberculosis isolate 917/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID540888Antibacterial activity against Mycobacterium tuberculosis B68 harboring embB TTC-TTA (F320L) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1390097Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 50 ug/ml after 48 hrs by MTT assay2018Bioorganic & 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.
AID1488486Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability after 24 hrs by MTS assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents.
AID1124850Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antimycobacterial activities of some new thiazolylhydrazone derivatives.
AID589952Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.
AID1236139Cytotoxicity against human THP1 cells assessed as cell growth inhibition after 48 hrs by resazurin dye reduction method2015Journal of natural products, Aug-28, Volume: 78, Issue:8
Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity.
AID405179Cmax in tuberculosis patient at 750 mg, po coadministered with 600 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID656228Antimycobacterial activity against isoniazid-, rifampin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1079933Acute 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
AID1624152Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 4 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID1916606Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as bacterial growth inhibition measured after 7 days by MABA method2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID748581Antitubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in log10CFU at 100 mg/kg, po qd administered 7 days post-infection for 28 days relative to control2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.
AID1188166Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition by microdilution AlamarBlue broth assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Sequential synthesis of amino-1,4-naphthoquinone-appended triazoles and triazole-chromene hybrids and their antimycobacterial evaluation.
AID370069Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1406778Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition at 25 ug/ml after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.
AID1463959Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 9449/2007 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID405184Half life in tuberculosis patient at 750 mg, po coadministered with 450 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID529533Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-ATA mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1243388Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of phaitanthrin congeners as anti-mycobacterial agents.
AID1174107Antimycobacterial activity against isoniazid, rifampin, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1435648Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 1 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID405183Half life in tuberculosis patient at 750 mg, po coadministered with 600 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1236140Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 48 hrs by resazurin dye reduction method2015Journal of natural products, Aug-28, Volume: 78, Issue:8
Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity.
AID599275Cytotoxicity against human MRC5 cells assessed as cell viability at 30 uM after 72 hrs by XTT assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID143706In Vitro antimicrobial activity against the Mycobacterium avium complex (MAC) Wild type strain AN12000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
AID1224519Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-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.
AID1463962Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 8666/2010 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID656232Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1400025Selectivity ratio of MIC for antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv harboring pFCA-luxAB to MIC100 for antibacterial activity against replicating Mycobacterium tuberculosis H37Rv2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1061090Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as parasite growth inhibition after 28 days by agar dilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl)phenothiazine-[1,2,3]triazole hybrids.
AID265977Cytotoxicity against Vero cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID1315571Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, characterization and antitubercular activities of novel pyrrolyl hydrazones and their Cu-complexes.
AID562239Antimycobacterial activity against Mycobacterium smegmatis by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID569262Antimicrobial activity against Escherichia coli DH5alpha2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID476702Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 4 weeks by agar slant proportion method2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Substituted hydrazinecarbothioamide as potent antitubercular agents: synthesis and quantitative structure-activity relationship (QSAR).
AID574811Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis H37Rv by CLSI method2010Antimicrobial 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.
AID1854276Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID429097Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates from tuberculosis patient assessed as percent specific isolates at 2 ug/ml by absolute-concentration method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations.
AID1463957Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 4 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1698034Inhibition of InhA in Mycobacterium tuberculosis H37Rv assessed antitubercular activity by measuring inhibition of bacterial growth incubated for 7 days by MABA assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Design and synthesis of new indanol-1,2,3-triazole derivatives as potent antitubercular and antimicrobial agents.
AID1464091Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of mycobacterial growth incubated for 2 weeks by MABA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
meso-Dihydroguaiaretic acid derivatives with antibacterial and antimycobacterial activity.
AID540903Antibacterial activity against HYG cassette-negative EMB-resistant Mycobacterium tuberculosis Rv44 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID771922Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 28 days by agar dilution method2014Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 23, Issue:4
Synthesis, antitubercular and anticancer activity of new Baylis-Hillman adduct-derived
AID1891915Antimycobacterial activity against Mycobacterium chelonae ATCC 6841 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID540914Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis B5402 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID432680Antimycobacterial against Mycobacterium tuberculosis H37Rv by agar dilution method2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
A facile synthesis and antimycobacterial evaluation of novel spiro-pyrido-pyrrolizines and pyrrolidines.
AID448530Cytotoxicity against mouse J774 macrophage assessed as cell viability at 10 ug/mL after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
AID333829Antimycobacterial activity against Mycobacterium phlei ATCC 11758 after 72 hrs by MTT assay2004Journal of natural products, Dec, Volume: 67, Issue:12
Antimycobacterial coumarins from the sardinian giant fennel (Ferula communis).
AID540920Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis RvAS9 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1546638Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth after 7 days by alamar blue assay2020Journal of natural products, 01-24, Volume: 83, Issue:1
Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents.
AID495235Antimicrobial activity against Mycobacterium tuberculosis NJT210GCC harboring embB406 GGC-GCC(Gly-Ala) mutation in embB gene after 4 weeks2010Antimicrobial 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.
AID540897Antibacterial activity against Mycobacterium tuberculosis B96 harboring embB GAT-TAT (D328Y) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1060900Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as parasite growth inhibition after 28 days by agar dilution method2014European journal of medicinal chemistry, Jan, Volume: 71Rational design and synthesis of novel dibenzo[b,d]furan-1,2,3-triazole conjugates as potent inhibitors of Mycobacterium tuberculosis.
AID1624156Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 8 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID370116Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 1 hr2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1204021Anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of microbial growth incubated for 5 days by MABA method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2,3-triazolylbenzohydrazides.
AID603735Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis and antimycobacterial activity of highly functionalized tetrahydro-4(1H)-pyridinones.
AID574804Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 obtained from sputum of patient at 5 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial 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.
AID738685Selectivity index, ratio of CC50 for african green monkey Vero cells tp MIC for Mycobacterium tuberculosis H37Rv2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
Synthesis and biological evaluation of trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxyalkylamine derivatives against drug susceptible, non-replicating M. tuberculosis H37Rv and clinical multidrug resistant strains.
AID1241003Selectivity index, ratio of CC50 for human MRC5 cells to MIC for Mycobacterium tuberculosis H37Rv2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Guanidinium compounds with sub-micromolar activities against Mycobacterium tuberculosis. Synthesis, characterization and biological evaluations.
AID1333168Induction of membrane integrity impairment in Mycobacterium bovis BCG ATCC 35734 assessed as reduction in intracellular pH at 16 times MIC by CMFDA dye based fluorescence spectroscopic method2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID540883Antibacterial activity against Mycobacterium tuberculosis B84 harboring embB ATG-ATC (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID562259Antimicrobial activity against Mycobacterium smegmatis expressing EmbC M286I mutant gene at 32 ug/ml2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID449435Antimycobacterial activity against Mycobacterium tuberculosis XDR infected in MDBK by BACTEC analysis2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Pentacyclo-undecane derived cyclic tetra-amines: synthesis and evaluation as potent anti-tuberculosis agents.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID694227Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID495216Antimicrobial activity against Mycobacterium tuberculosis 16C11 harboring embB397 CCG-TCG(Pro-Ser) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID587704Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 24 hrs by alamar blue assay2011European journal of medicinal chemistry, Mar, Volume: 46, Issue:3
Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives.
AID1058226Antimycobacterial activity against Mycobacterium kansasii2013Bioorganic & 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.
AID569258Antimycobacterial activity against Mycobacterium avium subsp. hominissuis 1042011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID649473Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 days by MTT assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Anti-mycobacterial activities of some cationic and anionic calix[4]arene derivatives.
AID1297705Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Benzo[d]thiazol-2-yl(piperazin-1-yl)methanones as new anti-mycobacterial chemotypes: Design, synthesis, biological evaluation and 3D-QSAR studies.
AID539118Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Pyrazole derivatives from azines of substituted phenacyl aryl/cyclohexyl sulfides and their antimycobacterial activity.
AID1435638Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate Alamar blue assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Synthesis, biological evaluation and in silico molecular modeling of pyrrolyl benzohydrazide derivatives as enoyl ACP reductase inhibitors.
AID540890Antibacterial activity against Mycobacterium tuberculosis B71 harboring embB TTC-CTC (F320L) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID370255Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 40 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID405575Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks by agar dilution method2008Journal of natural products, Jun, Volume: 71, Issue:6
Dihydroagarofuranoid sesquiterpenes, a lignan derivative, a benzenoid, and antitubercular constituents from the stem of Microtropis japonica.
AID551508Antimycobacterial activity against Mycobacterium phlei ATCC 19249 after 72 hrs by broth microtiter dilution method2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.
AID539834Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
A facile 1,3-dipolar cycloaddition of azomethine ylides to 2-arylidene-1,3-indanediones: synthesis of dispiro-oxindolylpyrrolothiazoles and their antimycobacterial evaluation.
AID1296385Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 8666/2010 after 14 days by microdilution method2016Journal 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.
AID510548Tmax in diabetic tuberculosis patient at 15 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1372625Inhibition 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 enzym2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1406743Cytotoxicity against HEK293 cells assessed as inhibition of cell viability at 25 ug/ml after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis of carbohydrazides and carboxamides as anti-tubercular agents.
AID1273073Antitubercular activity against Mycobacterium tuberculosis BCG after 7 days by alamar blue assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and anti-tuberculosis activity of glycitylamines.
AID529538Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 GTG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1624154Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 6 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID1265024Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2015European journal of medicinal chemistry, Dec-01, Volume: 106Design of new phenothiazine-thiadiazole hybrids via molecular hybridization approach for the development of potent antitubercular agents.
AID540891Antibacterial activity against Mycobacterium tuberculosis B99 harboring embB CGC-CAC (R321H) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID144146Antibacterial activity against Mycobacterium kansasii1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540908Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis B5200 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID565659Antimicrobial activity against Mycobacterium smegmatis expressing EmbC M286V mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID599009Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Antimycobacterial activity of novel 1,2,4-oxadiazole-pyranopyridine/chromene hybrids generated by chemoselective 1,3-dipolar cycloadditions of nitrile oxides.
AID333828Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 after 72 hrs by MTT assay2004Journal of natural products, Dec, Volume: 67, Issue:12
Antimycobacterial coumarins from the sardinian giant fennel (Ferula communis).
AID540886Antibacterial activity against Mycobacterium tuberculosis Rv11 harboring embB ATG-CTG (M306L) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1681007Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth incubated for 7 days by alamar blue assay2020Bioorganic & medicinal chemistry letters, 10-01, Volume: 30, Issue:19
Novel isoniazid embedded triazole derivatives: Synthesis, antitubercular and antimicrobial activity evaluation.
AID370271Cmax in human at 850 mg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1300945Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution technique2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Click-based synthesis and antitubercular evaluation of novel dibenzo[b,d]thiophene-1,2,3-triazoles with piperidine, piperazine, morpholine and thiomorpholine appendages.
AID1253865Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2015Bioorganic & 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.
AID1167605Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold agar dilution method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.
AID717596Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Molecular hybridization of bioactives: synthesis and antitubercular evaluation of novel dibenzofuran embodied homoisoflavonoids via Baylis-Hillman reaction.
AID565654Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC D249G mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID495206Antimicrobial activity against wild type Mycobacterium tuberculosis 8C1 after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID529534Antimycobacterial 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 method2008Antimicrobial 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.
AID1463958Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 131 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1915642Antimycobacterial activity against Mycobacterium tuberculosis My 331/88 (H37Rv) assessed as reduction in bacterial growth incubated for 14 days by microdilution method2021European journal of medicinal chemistry, Jan-15, Volume: 210An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
AID437746Antitubercular activity against Mycobacterium tuberculosis H37Rv after 30 days by agar microdilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Application of Huisgen (3+2) cycloaddition reaction: synthesis of 1-(2,3-dihydrobenzofuran-2-yl-methyl [1,2,3]-triazoles and their antitubercular evaluations.
AID495221Antimicrobial activity against Mycobacterium tuberculosis 16C14 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID145298Antibacterial activity against Mycobacterium tuberculosis H37Rv.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID562266Antimicrobial activity against Mycobacterium tuberculosis harboring Mycobacterium smegmatis embB M292L mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1378018Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID421758Antibacterial activity against Mycobacterium smegmatis mc2 2700 after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID1691023Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 1 week by microplate alamar blue assay2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID565996Antimycobacterial activity against Mycobacterium bovis BCG after 7 days by broth microdilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID775491Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Synthesis, characterization and in vitro biological evaluation of some novel 1,3,5-triazine-Schiff base conjugates as potential antimycobacterial agents.
AID1416768Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks by broth microdilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and
AID733061Antitubercular activity against Mycobacterium tuberculosis H37Rv by BacTiter-Gl Microbial Cell Viability assay2013Bioorganic & 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.
AID1706864Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID370072Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35837 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1864500Substrate activity at human OCT1 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1174923Antitubercular activity against Mycobacterium tuberculosis isolate 29/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID738687Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
Synthesis and biological evaluation of trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxyalkylamine derivatives against drug susceptible, non-replicating M. tuberculosis H37Rv and clinical multidrug resistant strains.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1227981Antimycobacterial activity against GFP expressing Mycobacterium tuberculosis H37Ra assessed as microbial growth inhibition incubated at 37 degC for 7 days by fluorescence based assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Eremophilane Sesquiterpenes and Diphenyl Thioethers from the Soil Fungus Penicillium copticola PSU-RSPG138.
AID289148Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis CIBIN 687 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID294759Antibacterial activity against Mycobacterium tuberculosis H37Rv after 2 weeks by broth dilution method2007Bioorganic & 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.
AID733062Antitubercular activity against Mycobacterium tuberculosis H37Rv by microdilution alamar Blue broth assay2013Bioorganic & 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.
AID562264Antimicrobial activity against Mycobacterium tuberculosis embA V280M gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID405180Cmax in tuberculosis patient at 750 mg, po coadministered with 450 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1435652Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 234/2005 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1624150Antitubercular activity against isoniazid/ethionamide resistant Mycobacterium tuberculosis isolate 2 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID1072704Cytotoxicity against mouse RAW264.7 cells at 50 uM after 72 hrs by MTT assay2014Bioorganic & 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.
AID1577327Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis Praha 1 after 14 days2019Journal 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.
AID1055551Antimycobacterial activity against Mycobacterium tuberculosis2013European journal of medicinal chemistry, , Volume: 70Novel camphane-based anti-tuberculosis agents with nanomolar activity.
AID1464094Selectivity index, ratio of IC50 for cytotoxicity against African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
meso-Dihydroguaiaretic acid derivatives with antibacterial and antimycobacterial activity.
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New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
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AID1296387Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 4 after 14 days by microdilution method2016Journal 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.
AID143712In Vitro antimicrobial activity against the Mycobacterium tuberculosis (MT) Wild type strain MT-22000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
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New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID569256Antimycobacterial activity against Mycobacterium bovis BCG str. Tokyo 1722011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1437026Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by agar dilution method2017Bioorganic & 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.
AID1477417Antibacterial activity against 6-((3-Fluorobenzyl)(methyl)amino)-N-(4-methoxyphenyl)-pyrimidine-4-carboxamide-resisitant Mycobacterium tuberculosis H37Rv grown in GAST/Fe medium measured on day 14 post inoculation by broth microdilution method2017Journal 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.
AID445288Antibacterial activity against Mycobacterium smegmatis by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1916599Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition measured after 7 days by MABA method2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1071659Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition by Alamar Blue staining-based broth microdilution assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
Antimycobacterial evaluation of novel hybrid arylidene thiazolidine-2,4-diones.
AID441084Ratio of ethambutol MIC to compound MIC for Mycobacterium tuberculosis CIB992009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID495199Antimicrobial activity against wild type Mycobacterium tuberculosis 8C6 after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1864505Inhibition of human OCT3 mediated methylscopolamine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID510545Cmax in diabetic tuberculosis patient at 15 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current 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.
AID765272Cmax/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID589953Selectivity index, ratio of CC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.
AID770315Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2013Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
Design, synthesis and antitubercular evaluation of novel 2-substituted-3H-benzofuro benzofurans via palladium-copper catalysed Sonagashira coupling reaction.
AID540869Antibacterial activity against Mycobacterium tuberculosis B52 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID562262Antimicrobial activity against Mycobacterium smegmatis expressing EmbC D280G mutant gene at 32 ug/ml after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID445289Antibacterial activity against Staphylococcus aureus by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID775492Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 5 days by microplate Alamar Blue assay2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Synthesis, characterization and in vitro biological evaluation of some novel 1,3,5-triazine-Schiff base conjugates as potential antimycobacterial agents.
AID563697Antibacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID1761698Antitubercular activity against Mycobacterium tuberculosis mc2 6230 assessed as inhibition of bacterial growth incubated for 5 days by REMA2021Journal of natural products, 02-26, Volume: 84, Issue:2
Structures and Biosynthetic Pathway of Coprisamides C and D, 2-Alkenylcinnamic Acid-Containing Peptides from the Gut Bacterium of the Carrion Beetle
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OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
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Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity.
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Antimycobacterial agents. 1. Thio analogues of purine.
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AID1577337Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 7357/1998 after 21 days2019Journal 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.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID333830Antimycobacterial activity against Mycobacterium aurum after 120 hrs by MTT assay2004Journal of natural products, Dec, Volume: 67, Issue:12
Antimycobacterial coumarins from the sardinian giant fennel (Ferula communis).
AID289152Antimycobacterial activity against streptomycin, isoniazid, ethambutol-resistant Mycobacterium tuberculosis CIBIN 112 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID563689Antibacterial activity against Mycobacterium tuberculosis H37Ra by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID497751Antimicrobial activity against Mycobacterium tuberculosis harboring mutation in embB306 gene after 4 weeks2010Antimicrobial 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.
AID1058222Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by BacTiter-Glo method2013Bioorganic & 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.
AID370256Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 80 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID565228Antimicrobial activity against Mycobacterium chelonae ATCC 35752 by resazurine microtiter assay2009Antimicrobial 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.
AID440893Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2009European 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.
AID301999Cytotoxicity against Vero cells after 48 hrs by XTT method2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase.
AID1854286Antitubercular 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 assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID1401966Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID1706866Antimycobacterial activity against Mycobacterium chelonae ATCC 35752 by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID495219Antimicrobial activity against wild type Mycobacterium tuberculosis 16C12 assessed as inhibition of growth after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID540876Antibacterial activity against Mycobacterium tuberculosis B74 harboring embB GAC-GGC (D300G) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID495214Antimicrobial activity against wild type Mycobacterium tuberculosis 16C10 after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1602935Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 3 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID510549Tmax in tuberculosis patient at 15 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
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A facile synthesis of carbocycle-fused mono and bis-1,2,3-selenadiazoles and their antimicrobial and antimycobacterial studies.
AID1612596Antibacterial activity against Mycobacterium tuberculosis H37Rv by MABA2019European journal of medicinal chemistry, Feb-01, Volume: 163Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
AID117759Antitubercular activity (25 mg/kg) in the 31-day murine model1981Journal 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.
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Synthesis and antitubercular evaluation of amidoalkyl dibenzofuranols and 1H-benzo[2,3]benzofuro[4,5-e][1,3]oxazin-3(2H)-ones.
AID1713722Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth by microdilution alamar blue broth assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
A facile stereoselective synthesis of dispiro-indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids and evaluation of their antimycobacterial, anticancer and AchE inhibitory activities.
AID565231Antimicrobial activity against Mycobacterium chelonae 9917 harboring pZS01 carrying mspA gene by resazurine microtiter assay2009Antimicrobial 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.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1891913Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID449433Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by broth macrodilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Pentacyclo-undecane derived cyclic tetra-amines: synthesis and evaluation as potent anti-tuberculosis agents.
AID145138In vitro antibacterial activity against Mycobacterium tuberculosis MT-2 (wild type strain) isolated from infected patients.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID495223Antimicrobial activity against Mycobacterium tuberculosis 16C16 harboring embB1024 GAC-AAC(Asp-Asn) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID302000Selectivity index, ratio of IC50 for Vero cells to MIC of Mycobacterial tuberculosis H37Rv2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase.
AID117764Antitubercular activity (50 mg/kg) in the 31-day murine model1981Journal 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.
AID733054Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2013Bioorganic & 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.
AID1058225Antimycobacterial activity against Mycobacterium chelonae2013Bioorganic & 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.
AID510546Cmax in tuberculosis patient at 15 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1143264Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID432682Antimycobacterial against Mycobacterium smegmatis MC2 by agar dilution method2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
A facile synthesis and antimycobacterial evaluation of novel spiro-pyrido-pyrrolizines and pyrrolidines.
AID510547Ratio of Cmax in diabetic tuberculosis patient to Cmax in tuberculosis patient at 15 mg/kg, po2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID540896Antibacterial activity against Mycobacterium tuberculosis B53 harboring embB GAT-TAT (D328Y) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID777340Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 24 hrs by agar microdilution method2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Identification of 1-[4-Benzyloxyphenyl)-but-3-enyl]-1H-azoles as New Class of Antitubercular and Antimicrobial Agents.
AID529541Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 ATA mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1163982Cytotoxicity against mouse RAW264.7 cells at 50 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1864503Inhibition of human OCT3 mediated Famotidine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID448532Cytotoxicity against Mycobacterium bovis Bacillus Calmette-Guerin infected mouse J774 macrophage assessed as cell viability at 1 ug/mL after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
AID1782928Selectivity index, ratio of CC50 for mouse RAW264.7 cells to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 272942021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID619448Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis of 3-heteroarylthioquinoline derivatives and their in vitro antituberculosis and cytotoxicity studies.
AID1403703Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 1 week in presence of verapamil by MABA method2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1143269Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis 17003 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID144303Antimycobacterial activity was evaluated against Mycobacterium smegmatis; Active2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Ethambutol analogues as potential antimycobacterial agents.
AID529524Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis isolate NJT210EMB-R-C2 assessed as bacterial colony formation at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1463956Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 1 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID656230Antimycobacterial activity against isoniazid-, rifampin-, streptomycin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID522849Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
AID540909Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis B5201 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID495200Antimicrobial activity against Mycobacterium tuberculosis 8C5 harboring embC13 CGG-CTG(Arg-Leu) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID433906Antimycobacterial activity against Mycobacterium tuberculosis H37Ra after 5 days by microplate alamar blue assay2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antitubercular screening of imidazole derivatives.
AID559766Antimycobacterial activity against PknGMsm-deficient Mycobacterium smegmatis harboring PknG Mtb gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID522853Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as intracellular bacterial killing after 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
AID1272620Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by broth microdilution method2016Bioorganic & 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.
AID603726Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis and screening of (E)-1-(β-D-galactopyranosyl)-4-(aryl)but-3-ene-2-one against Mycobacterium tuberculosis.
AID439073Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 2 weeks2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and evaluation of (S,S)-N,N'-bis-[3-(2,2',6,6'-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.
AID1143265Antimycobacterial activity against Mycobacterium tuberculosis D-211 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1333143Induction of membrane disruption in Mycobacterium bovis BCG ATCC 35734 at 60 uM up to 3 hrs by Sytox green uptake assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1143268Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis 19000 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID396660Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and evaluation of in vitro anti-tuberculosis activity of N-substituted glycolamides.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID429856Antibacterial activity against Mycobacterium fortuitum after 72 hrs2009Journal of natural products, Jun, Volume: 72, Issue:6
Antibacterial diterpenes from Plectranthus ernstii.
AID725967Cytotoxicity against HEK293T cells assessed as growth inhibition at 50 uM by MTT assay relative to control2013Bioorganic & 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.
AID559761Antimycobacterial activity against Mycobacterium smegmatis MC2 155 by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID448533Cytotoxicity against Mycobacterium bovis Bacillus Calmette-Guerin infected mouse J774 macrophage assessed as cell viability at 10 ug/mL after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
AID285159Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID574792Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 obtained from sputum of patient at 5 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial 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.
AID495237Antimicrobial activity against Mycobacterium tuberculosis NJT210TGC harboring embB406 GGC-TGC(Gly-Cys) mutation in embB gene after 4 weeks2010Antimicrobial 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.
AID1891917Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID271342Antitubercular activity against Mycobacterium tuberculosis H37Rv2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Search of antitubercular activities in tetrahydroacridines: synthesis and biological evaluation.
AID1196886Cytotoxicity against mouse RAW264.7 cells at 50 uM after 48 hrs by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID370257Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 160 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID649311Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 10 uM after 6 days by MTT assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Anti-mycobacterial activities of some cationic and anionic calix[4]arene derivatives.
AID1383955Bactericidal activity against Mycobacterium tuberculosis H37Rv after 4 weeks by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID388924Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 days by mycobacteria growth indicator tube system2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Synthesis and antitubercular activity of ferrocenyl diaminoalcohols and diamines.
AID285162Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID370246Half life in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID302004Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at MIC2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase.
AID529535Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 5310 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID370244AUC (0 to t) in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1467547Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
One-pot microwave assisted stereoselective synthesis of novel dihydro-2'H-spiro[indene-2,1'-pyrrolo-[3,4-c]pyrrole]-tetraones and evaluation of their antimycobacterial activity and inhibition of AChE.
AID289150Antimycobacterial activity against streptomycin and isoniazid-resistant Mycobacterium tuberculosis CIBIN 675 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID1372629Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week in presence of efflux pump inhibitor piperine by MABA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1688940Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as reduction in microbial growth after 7 days by Alamar blue assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.
AID1624155Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 7 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID599272Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 after 3 days by MTT assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID725968Cytotoxicity against HEK293T cells assessed as growth inhibition at 25 uM by MTT assay relative to control2013Bioorganic & 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.
AID441081Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 to 7 days by microplate alamar blue assay2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID479064Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 2 weeks2010Journal of natural products, May-28, Volume: 73, Issue:5
Secondary metabolites from the roots of Litsea hypophaea and their antitubercular activity.
AID1188155Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID495224Antimicrobial activity against Mycobacterium tuberculosis 16C16 harboring embB1024 GAC-AAC(Asp-Asn) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID104011Activity against Mycobacterium tuberculosis (H37Rv) using the standard BACTEC radiometric growth assay2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
A new class of antituberculosis agents.
AID1241002Cytotoxicity against human MRC5 cells after 24 hrs2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Guanidinium compounds with sub-micromolar activities against Mycobacterium tuberculosis. Synthesis, characterization and biological evaluations.
AID1417199Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as tubercular foci index at 20 mg/kg, po administered via gavage over 42 days (excluding weekends) (Rvb = 23.6 +/- 0.09 No_unit)2018European journal of medicinal chemistry, Sep-05, Volume: 157Conjugation of a 5-nitrofuran-2-oyl moiety to aminoalkylimidazoles produces non-toxic nitrofurans that are efficacious in vitro and in vivo against multidrug-resistant Mycobacterium tuberculosis.
AID309703Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Preparation and antitubercular activities of alkylated amino alcohols and their glycosylated derivatives.
AID662304Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 28 days2012Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11
Synthesis and antimycobacterial activity of prodrugs of sulfur dioxide (SO2).
AID1477416Antibacterial activity against wild type Mycobacterium tuberculosis H37Rv grown in GAST/Fe medium measured on day 14 post inoculation by broth microdilution method2017Journal 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.
AID1762620Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as reduction in bacterial growth after 6 to 8 days by green fluorescent protein microplate assay
AID1765351Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition after 7 days by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID540915Antibacterial activity against HYG cassette-negative Mycobacterium tuberculosis H37Rv by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1782924Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 9 days by resazurin microtiter assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID1697877Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition
AID540912Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis B5400 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1488484Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 after 4 weeks by Agar-based proportion Assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents.
AID567906Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Synthesis and antitubercular evaluation of novel substituted aryl and thiophenyl tethered dihydro-6H-quinolin-5-ones.
AID562269Inhibition of Mycobacterium tuberculosis EmbC assessed as effect on LAM production at 1 ug/ml after 2 hrs by immunoblotting2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1174111Antimycobacterial activity against isoniazid, rifampin, ethambutol-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1163980Antimycobacterial 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 inhibitor2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1782929Selectivity index, ratio of CC50 for human HepG2 cells to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 272942021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID565653Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC D249G mutant gene after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1278842Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate Alamar blue assay2016Bioorganic & 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.
AID1577331Antimycobacterial activity against XDR Mycobacterium tuberculosis Praha 131 after 14 days2019Journal 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.
AID495220Antimicrobial activity against Mycobacterium tuberculosis 16C14 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1253866Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis FJ05120 after 3 to 4 weeks by microplate alamar blue assay2015Bioorganic & 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.
AID421757Antibacterial activity against Mycobacterium smegmatis after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID289151Antimycobacterial activity against streptomycin, isoniazid, rifampicin, pyrazinamide-resistant Mycobacterium tuberculosis CIBIN 234 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID143709In Vitro antimicrobial activity against the Mycobacterium avium complex (MAC) Wild type strain ISS 4862000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
AID495234Antimicrobial activity against wild type Mycobacterium tuberculosis NJT210CGG-CAG after 4 weeks2010Antimicrobial 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.
AID670191Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Synthesis of Leubethanol derivatives and evaluation against Mycobacterium tuberculosis.
AID633934Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Mefloquine-oxazolidine derivatives, derived from mefloquine and arenecarbaldehydes: In vitro activity including against the multidrug-resistant tuberculosis strain T113.
AID1612597Antibacterial activity against Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Feb-01, Volume: 163Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
AID1765357Antimycobacterial activity against Streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 35820 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID439077Antitubercular activity against isoniazid, rifampin, ethambutol, streptomycin-resistant Mycobacterium tuberculosis by radiometric BACTEC460 method2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and evaluation of (S,S)-N,N'-bis-[3-(2,2',6,6'-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID540866Antibacterial activity against Mycobacterium tuberculosis Rv44 harboring embB ATG-ATA (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1456569Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1435654Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID529536Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 CTG-ATG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID775978Inhibition 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 analy2013European journal of medicinal chemistry, Nov, Volume: 69Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540923Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis BAS6 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID333831Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 after 72 hrs by MTT assay2004Journal of natural products, Dec, Volume: 67, Issue:12
Antimycobacterial coumarins from the sardinian giant fennel (Ferula communis).
AID370245Tmax in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1864509Substrate uptake in empty vector transfected (OCT3 null) HEK293 cells incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1367810Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis and in vitro anti-tuberculosis activity of benzo[6,7]cyclohepta[1,2-b]pyridine-1,2,3-triazole derivatives.
AID1247162Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
One-pot synthesis of new triazole--Imidazo[2,1-b][1,3,4]thiadiazole hybrids via click chemistry and evaluation of their antitubercular activity.
AID564983Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID429093Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates from tuberculosis patient assessed as percent sensitive isolates at 2 ug/ml by absolute-concentration method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations.
AID1333275Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 4 times MIC measured after 6 hrs by luciferase reporter gene assay (Rvb = 152%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1736274Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days by MABA method2020European journal of medicinal chemistry, Feb-15, Volume: 188Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
AID444319Cytotoxicity against mouse J774 cells assessed as cell viability at 100 ug/ml by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID656231Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID540917Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis RvAS2 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1303841Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis and antitubercular evaluation of novel dibenzo[b,d]thiophene tethered imidazo[1,2-a]pyridine-3-carboxamides.
AID522851Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as extracellular bacterial killing after 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
AID765270AUC/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID565652Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC T270I mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID565647Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC M300I mutant gene after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID432681Antimycobacterial against multidrug resistant Mycobacterium tuberculosis by agar dilution method2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
A facile synthesis and antimycobacterial evaluation of novel spiro-pyrido-pyrrolizines and pyrrolidines.
AID670190Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by MABA method2012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Synthesis of Leubethanol derivatives and evaluation against Mycobacterium tuberculosis.
AID495230Antimicrobial activity against Mycobacterium tuberculosis 32C5 harboring embB324 GGC-CGC(Gly-Arg) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1224525Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 4 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-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.
AID289153Cytotoxicity against Vero cells2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID540877Antibacterial activity against Mycobacterium tuberculosis Rv7 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID278000Antitubercular activity against Mycobacterium tuberculosis 90-2213872007Journal of natural products, Feb, Volume: 70, Issue:2
Antitubercular dihydroagarofuranoid sesquiterpenes from the roots of Microtropis fokienensis.
AID565655Ratio of MIC for Mycobacterium tuberculosis expressing wild type EmbC gene to MIC for Mycobacterium tuberculosis expressing EmbC D249G mutant gene2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID617851Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis CIBIN/UMF15:99 isolate by microplate Alamar blue assay2011Journal of natural products, Sep-23, Volume: 74, Issue:9
Stereochemical analysis of leubethanol, an anti-TB-active serrulatane, from Leucophyllum frutescens.
AID587705Partition coefficient, log P of the compound2011European journal of medicinal chemistry, Mar, Volume: 46, Issue:3
Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives.
AID589951Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 48 hrs by resazurin microplate broth microdilution method2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.
AID613870Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis, antitubercular activity, and SAR study of N-substituted-phenylamino-5-methyl-1H-1,2,3-triazole-4-carbohydrazides.
AID1193923Cytotoxicity against mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2015Bioorganic & 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.
AID405177AUC (0 to 24 hrs) in tuberculosis patient at 750 mg, po coadministered with 600 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID529542Antimycobacterial activity against Mycobacterium tuberculosis isolate 210 at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID540922Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis BAS5 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1204849Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as parasite growth inhibition after 7 days by broth microdilution assay2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID658539Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 after 72 hrs by MTT assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antibacterial acylphloroglucinols from Hypericum olympicum.
AID1400023Antibacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 15 days under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID565229Antimicrobial activity against Mycobacterium chelonae ATCC 35752 harboring pZS01 carrying mspA gene by resazurine microtiter assay2009Antimicrobial 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.
AID534421Antibacterial activity against Mycobacterium bovis BCG-Denmark2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID1585696Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID495227Antimicrobial activity against Mycobacterium tuberculosis 32C2 harboring embB497 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1174926Antitubercular activity against Mycobacterium tuberculosis isolate 778/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID1296388Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 131 after 14 days by microdilution method2016Journal 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.
AID495207Antimicrobial activity against wild type Mycobacterium tuberculosis 210 after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1688198Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by MABA assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.
AID1193920Inhibition of Mycobacterium tuberculosis DNA GyrA/B heterotetramer assessed as inhibition of pBR322 supercoiling after 30 mins by gel electrophoresis2015Bioorganic & 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.
AID370272AUC (0 to t) in human at 850 mg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1706676Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition by MABA2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB.
AID1653413Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by BACTEC radiometric growth assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID548359Antitubercular activity against Mycobacterium tuberculosis ATCC 27294 by Alamar blue assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives.
AID1845745Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition by microplate alamar blue assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32A comprehensive review on the biological interest of quinoline and its derivatives.
AID344043Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks2008Journal of natural products, Jul, Volume: 71, Issue:7
Constituents of the root wood of Zanthoxylum wutaiense with antitubercular activity.
AID540209Volume of distribution at steady state in human after iv administration2008Drug 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.
AID1417200Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as colony forming units per lung mass unit at 20 mg/kg, po administered via gavage over 42 days (excluding weekends) (Rvb = 169.1 +/- 11.83 x 10'3 No_unit)2018European journal of medicinal chemistry, Sep-05, Volume: 157Conjugation of a 5-nitrofuran-2-oyl moiety to aminoalkylimidazoles produces non-toxic nitrofurans that are efficacious in vitro and in vivo against multidrug-resistant Mycobacterium tuberculosis.
AID565650Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC M300V mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID445333Selectivity for Mycobacterium tuberculosis H37Rv over human A549 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID370263Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as reduction in viable lung bacterial count at 160 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1193921Inhibition of Mycobacterium smegmatis DNA GyrB domain assessed as inhibition of inorganic phosphate release after 100 mins at room temperature by ATPase assay2015Bioorganic & 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.
AID1687471Antitubercular activity against Mycobacterium tuberculosis Spec.192 assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID1071122Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 6.25 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID565657Antimicrobial activity against Mycobacterium smegmatis expressing EmbC M286I mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1174920Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID1864501Inhibition of human OCT3 mediated ASP+ uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID289149Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis CIBIN 650 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID540918Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis RvAS3 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID565995Antimycobacterial activity against Mycobacterium smegmatis MC2 155 after 72 hrs by broth microdilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID1204852Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis assessed as parasite growth inhibition by REMA method2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID143711In Vitro antimicrobial activity against the Mycobacterium tuberculosis (MT) Wild type strain MT-12000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
AID301998Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase.
AID495198Antimicrobial activity against wild type Mycobacterium tuberculosis 8C6 after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID725969Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition by NCCLS agar dilution method2013Bioorganic & 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.
AID1435650Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 131 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1891920Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID421759Antibacterial activity against Mycobacterium phlei after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID765105Bacteriostatic activity against rifampicin, isoniazid, streptomycin, ethambutol and pyrazinamide-resistant Mycobacterium tuberculosis MS-115 assessed as growth inhibition at 2 to 200 ug/mL relative to control2013Bioorganic & 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.
AID658540Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 after 72 hrs by MTT assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antibacterial acylphloroglucinols from Hypericum olympicum.
AID540887Antibacterial activity against Mycobacterium tuberculosis B51 harboring embB ATG-ACG (M306T) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID425189Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2009Bioorganic & 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.
AID656229Antimycobacterial activity against isoniazid-, rifampin-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID495231Antimicrobial activity against Mycobacterium tuberculosis 32C5 harboring embB324 GGC-CGC(Gly-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID540911Antibacterial activity against HYG cassette-negative EMB-resistant Mycobacterium tuberculosis B54 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1188153Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID495236Antimicrobial activity against Mycobacterium tuberculosis NJT210GAC harboring embB406 GGC-GAC(Gly-Asp) mutation in embB gene after 4 weeks2010Antimicrobial 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.
AID1697865Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition at MIC of 15 uM
AID529532Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-ATC mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID444320Cytotoxicity against mouse J774 cells infected with Mycobacterium bovis BCG assessed as cell viability at 10 ug/ml by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID1667678Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 5 days by alamar blue based colorimetric assay2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from l-serine.
AID540894Antibacterial activity against Mycobacterium tuberculosis Rv21 harboring embB GAT-TAT (D328Y) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID540880Antibacterial activity against Mycobacterium tuberculosis B54 harboring embB ATG-ATA (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID370117Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 2 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID738688Antimicrobial activity against Mycobacterium tuberculosis H37Rv by BACTEC radiometric method2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
Synthesis and biological evaluation of trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxyalkylamine derivatives against drug susceptible, non-replicating M. tuberculosis H37Rv and clinical multidrug resistant strains.
AID445331Cytotoxicity against human MRC5 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID540879Antibacterial activity against Mycobacterium tuberculosis H37Rv by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID145136In vitro antibacterial activity against Mycobacterium tuberculosis MT ATCC H37Rv strain2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID405178AUC (0 to 24 hrs) in tuberculosis patient at 750 mg, po coadministered with 450 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID694231Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic condition by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID1201573Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294/XDR-TB incubated for 28 days by agar dilution method2015European journal of medicinal chemistry, May-05, Volume: 95Synthesis and biological evaluation of new imidazo[2,1-b][1,3,4]thiadiazole-benzimidazole derivatives.
AID1852583Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by MABA
AID495211Antimicrobial activity against Mycobacterium tuberculosis 16C6 harboring embB320 TTC-TTG(phe-Leu) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1406780Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition after 48 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.
AID1278841Inhibition of Mycobacterium tuberculosis pantothenate synthetase using pantoic acid as substrate and beta-alanine as reactant assessed as NAD+ formation by spectrophotmetry in presence of NADH2016Bioorganic & 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.
AID562261Antimicrobial activity against Mycobacterium smegmatis expressing EmbC M286V mutant gene at 32 ug/ml after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1132595Antitubercular against Mycobacterium smegmatis ATCC 607 by agar dilution method1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Antitubercular 2,8-bis(alkylaminomethyl)phenazines.
AID609928Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 30 days by agar microdilution method2011Bioorganic & 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.
AID1253867Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis FJ05195 after 3 to 4 weeks by microplate alamar blue assay2015Bioorganic & 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.
AID565644Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC gene after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID565645Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC M300L mutant gene after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1889500Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and molecular docking studies of imidazole and benzimidazole linked ethionamide derivatives as inhibitors of InhA and antituberculosis agents.
AID1192688Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse chronic TB model assessed as survival rate at 490 umol/kg administered via esophageal cannula 6 times a week for 4 weeks relative to untreated control2015Bioorganic & 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.
AID534425Antibacterial activity against Mycobacterium bovis BCG-Glaxo2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID444321Cytotoxicity against mouse J774 cells infected with Mycobacterium bovis BCG assessed as cell viability at 100 ug/ml by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID574798Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 obtained from sputum of patient at 5 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial 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.
AID1187834Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 as substrate after 30 mins by DNA supercoiling assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID665278Antitubercular activity against isoniazid, rifampicin and ethambutol-resistant Mycobacterium tuberculosis clinical isolate after 28 days by agar dilution method2012European journal of medicinal chemistry, Jul, Volume: 53A 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.
AID1266238Cytotoxicity against mouse RAW264.7 cells at 50 uM after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.
AID1163981Cytotoxicity against mouse RAW264.7 cells at 100 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1577335Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 234/2005 after 14 days2019Journal 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.
AID442657Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010European 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.
AID1889501Cytotoxicity in African green monkey Vero cells assessed as reduction in cell viability2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and molecular docking studies of imidazole and benzimidazole linked ethionamide derivatives as inhibitors of InhA and antituberculosis agents.
AID569259Antimycobacterial activity against Mycobacterium avium subsp. avium ATCC 2529I2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1891919Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID421762Antibacterial activity against Staphylococcus aureus EMRSA15 after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID1300864Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two fold serial dilution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis, biological evaluation and structure-activity relationship of 2-styrylquinazolones as anti-tubercular agents.
AID290253Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Hydroxythiosemicarbazones: synthesis and in vitro antitubercular activity.
AID495226Antimicrobial activity against Mycobacterium tuberculosis 32C1 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1138420Antimicrobial activity against Mycobacterium smegmatis after 10 hrs2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Multitarget drug discovery for tuberculosis and other infectious diseases.
AID1274537Antibacterial activity against Mycobacterium tuberculosis H37Rv2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and evaluation of antibacterial and antitumor activities of new galactopyranosylated amino alcohols.
AID510544Ratio of sAUC (0 to 24 hrs) for diabetic tuberculosis patient to sAUC (0 to 24 hrs) for tuberculosis patient at 15 mg/kg, po2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID442658Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method2010European 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.
AID562238Antimycobacterial activity against Mycobacterium smegmatis assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID495197Antimicrobial activity against Mycobacterium tuberculosis 8C7 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID574808Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 horboring rpoB S531L, katG R463L/E217G, gyrA D94N/S95T, rrs A1401G by CLSI method2010Antimicrobial 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.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID143713In Vitro antimicrobial activity against the Mycobacterium tuberculosis (MT) strain H-37-Rv ATCC2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
AID1687559Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 assessed as inhibition of microbial growth by classical test tube method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID429089Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates from tuberculosis patient assessed as percent resistant isolates at 2 ug/ml by absolute-concentration method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations.
AID1174112Antimycobacterial activity against isoniazid, rifampin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1854287Antitubercular 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 assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID1266236Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of supercoiling activity using relaxed pBR322 plasmid as substrate after 30 mins2016Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.
AID1594635Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of parasite growth incubated for 6 days by REMA method2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID1411649Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days by broth dilution method2017MedChemComm, 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.
AID495202Antimicrobial activity against Mycobacterium tuberculosis 8C5 harboring embC13 CGG-CTG(Arg-Leu) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1400024Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv harboring pFCA-luxAB preincubated for 10 days under anaerobic condition followed by incubation under ambient gaseous condition for 28 hrs by LORA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID145295Tested for antibacterial activity against Mycobacterium tuberculosis H37Rv isonicotinic acid hydrazide-resistant strain1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1433175Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Design of novel dispirooxindolopyrrolidine and dispirooxindolopyrrolothiazole derivatives as potential antitubercular agents.
AID1381931Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2018European journal of medicinal chemistry, Feb-25, Volume: 146New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity.
AID439072Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 7 days2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and evaluation of (S,S)-N,N'-bis-[3-(2,2',6,6'-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.
AID1590010Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Ultrasonication-ionic liquid synergy for the synthesis of new potent anti-tuberculosis 1,2,4-triazol-1-yl-pyrazole based spirooxindolopyrrolizidines.
AID529531Antimycobacterial 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 method2008Antimicrobial 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.
AID439076Antitubercular activity against isoniazid, rifampin-resistant Mycobacterium tuberculosis by radiometric BACTEC460 method2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and evaluation of (S,S)-N,N'-bis-[3-(2,2',6,6'-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.
AID529537Antimycobacterial 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 method2008Antimicrobial 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.
AID619608Antitubercular activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
A facile four-component sequential protocol in the expedient synthesis of novel 2-aryl-5-methyl-2,3-dihydro-1H-3-pyrazolones in water and their antitubercular evaluation.
AID540892Antibacterial activity against Mycobacterium tuberculosis Rv39 harboring embB GGC-CGC (G324R) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID559765Antimycobacterial activity against PknGMsm-deficient Mycobacterium smegmatis harboring PknG K181M mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID1058223Antimycobacterial activity against Mycobacterium avium2013Bioorganic & 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.
AID540904Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis Rv4400 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID540878Antibacterial activity against Mycobacterium tuberculosis Beijing by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1687561Antitubercular activity against Mycobacterium tuberculosis Spec.192 assessed as inhibition of microbial growth by classical test tube method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID145153Lowest concentration of compound against Mtb H37Ra strain required to inhibit the growth completely; activity range is 2-42004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Antimycobacterial agents. 1. Thio analogues of purine.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID370073Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35820 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID540916Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis RvAS1 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID540212Mean residence time in human after iv administration2008Drug 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.
AID1536933Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 1 week by microplate alamar blue assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Synthesis and evaluation of novel substituted 1,2,3-triazolyldihydroquinolines as promising antitubercular agents.
AID540913Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis B5401 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID306130Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents.
AID540211Fraction unbound in human after iv administration2008Drug 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.
AID618417Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and antitubercular evaluation of novel dibenzo[b,d]furan and 9-methyl-9H-carbazole derived hexahydro-2H-pyrano[3,2-c]quinolines via Povarov reaction.
AID495225Antimicrobial activity against Mycobacterium tuberculosis 32C1 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1174109Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID495204Antimicrobial activity against wild type Mycobacterium tuberculosis 8C2 after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1360819Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by Two-fold serial dilution assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Benzo[d]thiazole-2-carbanilides as new anti-TB chemotypes: Design, synthesis, biological evaluation, and structure-activity relationship.
AID370113Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 0.083 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1173785Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA assay2014Bioorganic & 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.
AID1623449Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by Alamar blue assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis of novel morpholine, thiomorpholine and N-substituted piperazine coupled 2-(thiophen-2-yl)dihydroquinolines as potent inhibitors of Mycobacterium tuberculosis.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID574806Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 horboring rpoB S531L/G566R/I569L, katG S315T/R463L, gyrA A90V/S95T, rrs A1401G by CLSI method2010Antimicrobial 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.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID429857Antibacterial activity against Mycobacterium phlei after 72 hrs2009Journal of natural products, Jun, Volume: 72, Issue:6
Antibacterial diterpenes from Plectranthus ernstii.
AID1864498Substrate activity at human OCT3 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1333153Induction 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 control2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID439074Ratio of MBC to MIC for Mycobacterium tuberculosis H37Rv2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and evaluation of (S,S)-N,N'-bis-[3-(2,2',6,6'-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.
AID765273fCmax/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1864499Substrate activity at human OCT2 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1187928Antitubercular activity against Mycobacterium tuberculosis H37Rv after 4 weeks2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
New class of methyl tetrazole based hybrid of (Z)-5-benzylidene-2-(piperazin-1-yl)thiazol-4(%H)-one as potent antitubercular agents.
AID540213Half life in human after iv administration2008Drug 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.
AID290254Cytotoxicity against Vero cells after 72 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Hydroxythiosemicarbazones: synthesis and in vitro antitubercular activity.
AID1188156Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 100 uM after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID1180390Inhibition of Mycobacterium tuberculosis pantothenate synthetase expressed in Escherichia coli BL21 (DE3) by spectrophotometry2014Bioorganic & 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.
AID495209Antimicrobial activity against Mycobacterium tuberculosis 8C7 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1263165Antituberculosis activity against Mycobacterium tuberculosis H37Rv MTCC 300 after 4 weeks by Lowenstein-Jensen medium method2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Pyrazole clubbed triazolo[1,5-a]pyrimidine hybrids as an anti-tubercular agents: Synthesis, in vitro screening and molecular docking study.
AID1854285Antitubercular activity against clinical isolate ethambutol-resistant Mycobacterium tuberculosis ATCC 35837 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID1501038Antitubercular activity against Mycobacterium tuberculosis H37Rv2017European journal of medicinal chemistry, Oct-20, Volume: 139Recent advances of pyrazole-containing derivatives as anti-tubercular agents.
AID1699965Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition by MABA relative to control2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and biological evaluation of anti-tubercular activity of Schiff bases of 2-Amino thiazoles.
AID658542Antimycobacterial activity against Mycobacterium phlei ATCC 11758 after 72 hrs by MTT assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antibacterial acylphloroglucinols from Hypericum olympicum.
AID405181Tmax in tuberculosis patient at 750 mg, po coadministered with 600 mg, po rifampin2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID529539Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 CTG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1383953Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 10 days by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID1891921Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1765356Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID559764Antimycobacterial activity against PknGMsm-deficient Mycobacterium smegmatis by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID564973Antimicrobial activity against Mycobacterium bovis BCG by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID540871Antibacterial activity against Mycobacterium tuberculosis Rv17 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID569260Antimicrobial activity against Staphylococcus aureus2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID606810Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks by agar plate assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Antitubercular chromones and flavonoids from Pisonia aculeata.
AID1071104Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate Alamar blue assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1174108Antimycobacterial activity against isoniazid, rifampin, ethambutol, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1864504Inhibition of human OCT3 mediated N-Ethyllidocaine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID1316977Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in po dosed Balb/c mouse assessed as bacterial burden in lungs administered daily through gavage starting on day 2 post infection for 4 days per week for 2 weeks each 4 days dosi2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification and optimization of a new series of anti-tubercular quinazolinones.
AID1577329Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis Praha 4 after 14 days2019Journal 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.
AID540867Antibacterial activity against Mycobacterium tuberculosis B64 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID540926Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis BAS10 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID495213Antimicrobial activity against Mycobacterium tuberculosis 16C9 harboring embB497 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1916592Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as bacterial growth inhibition measured after 5 days by MABA method2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1891914Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID144742Percent inhibitory activity against Mycobacterium tuberculosis (Mtb) H37Rv Strain at 6.25 ug/mL; No data2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Antimycobacterial agents. 1. Thio analogues of purine.
AID713902Antimycobacterial activity against Mycobacterium tuberculosis 90-2213872012European journal of medicinal chemistry, Mar, Volume: 49Recent advances in antitubercular natural products.
AID540210Clearance in human after iv administration2008Drug 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.
AID1372628Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week in presence of efflux pump inhibitor verapamil by MABA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1058224Antimycobacterial activity against Mycobacterium intracellulare2013Bioorganic & 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.
AID1127155Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 24 hrs by Lowenstein-Jensen agar dilution method2014European journal of medicinal chemistry, May-22, Volume: 79Facile synthesis of benzonitrile/nicotinonitrile based s-triazines as new potential antimycobacterial agents.
AID1173786Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by MTT assay2014Bioorganic & 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.
AID440894Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis by agar dilution method2009European 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.
AID495208Antimicrobial activity against wild type Mycobacterium tuberculosis 210 after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1173783Inhibition of purified Mycobacterium smegmatis GyrB at 50 to 100 uM after 100 mins by ATPase assay2014Bioorganic & 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.
AID562260Antimicrobial activity against Mycobacterium smegmatis expressing EmbC M286L mutant gene at 32 ug/ml after 48 hrs2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID540874Antibacterial activity against Mycobacterium tuberculosis B55 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID540921Antibacterial activity against HYG cassette-negative Mycobacterium tuberculosis Beijing by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID563698Antibacterial activity against pyrazinamide-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID609934Inhibition of Wistar rat liver glycogen phosphorylase at 100 uM after 30 mins2011Bioorganic & 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.
AID550046Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of colonies after 30 days by agar microdilution method2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Conventional and microwave assisted synthesis of 2-oxo-4-substituted aryl-azetidine derivatives of benzotriazole: a new class of biological compounds.
AID1071119Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 100 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1765354Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID1196883Inhibition of Mycobacterium tuberculosis AlaDH using L-alanine as substrate after 20 mins by spectrophotometry2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID694368Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis MS-115 under anaerobic condition assessed as growth inhibition at 5 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID299658Antimycobacterial activity against Mycobacterium tuberculosis H37Ra2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis of symmetrical C- and pseudo-symmetrical O-linked disaccharide analogs for arabinosyltransferase inhibitory activity in Mycobacterium tuberculosis.
AID265979Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID476043Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines.
AID145297Tested for antibacterial activity against Mycobacterium tuberculosis H37Rv streptomycin resistant strain1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID1406742Inhibition of replicating Mycobacterium tuberculosis H37Rv InhA assessed as cell growth inhibition after 7 days by MABA method2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis of carbohydrazides and carboxamides as anti-tubercular agents.
AID495201Antimicrobial activity against wild type Mycobacterium tuberculosis 8C3 after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID669488Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Design, synthesis, and structure-activity correlations of novel dibenzo[b,d]furan, dibenzo[b,d]thiophene, and N-methylcarbazole clubbed 1,2,3-triazoles as potent inhibitors of Mycobacterium tuberculosis.
AID495233Antimicrobial activity against Mycobacterium tuberculosis NJT210CGG harboring embB497 CAG-CGG(Gln-Arg) mutation in embB gene after 4 weeks2010Antimicrobial 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.
AID1557253Antitubercular activity against resistant Mycobacterium tuberculosis harboring embCAB Met306IIe/Val mutant2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID1687473Antitubercular activity against INH-resistant Mycobacterium tuberculosis Spec.800 harboring InhA promoter mutation assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID510543AUC (0 to 24 hrs) in tuberculosis patient at 15 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1126498Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis and evaluation of 1,2,3-triazole-adamantylacetamide hybrids as potent inhibitors of Mycobacterium tuberculosis.
AID370114Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 0.25 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1713723Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
A facile stereoselective synthesis of dispiro-indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids and evaluation of their antimycobacterial, anticancer and AchE inhibitory activities.
AID421761Antibacterial activity against tetracycline-effluxing Staphylococcus aureus XU212 after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID565648Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC M300I mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1187836Cytotoxicity against mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID1300865Cytotoxicity against HEK293T cells assessed as cell viability at 50 ug/ml after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis, biological evaluation and structure-activity relationship of 2-styrylquinazolones as anti-tubercular agents.
AID574810Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 horboring rpoB D516V, katG S315T/R463L, gyrA D94G/S95T/R128S/Y129C, rrs A1401G by CLSI method2010Antimicrobial 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.
AID1054037Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in Balb/c mouse model assessed as log CFU reduction at 100 mg/kg, po qd administered for 28 days relative to untreated control2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis, and biological evaluation of indole-2-carboxamides: a promising class of antituberculosis agents.
AID1278843Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 50 uM after 72 hrs by MTT assay2016Bioorganic & 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.
AID1627828Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
A convenient synthesis and screening of benzosuberone bearing 1,2,3-triazoles against Mycobacterium tuberculosis.
AID1400026Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID565643Antimicrobial activity against Mycobacterium tuberculosis expressing EmbC gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID529523Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis isolate NJT210EMB-R-C3 assessed as bacterial colony formation at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1765355Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID1183298Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives.
AID1188154Inhibition of Mycobacterium tuberculosis DNA gyrase supercoiling activity using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1296383Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 234/2005 after 14 days by microdilution method2016Journal 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.
AID664308Antituberculosis activity against Mycobacterium tuberculosis H37Rv by BACTEC MGIT method2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents.
AID495210Antimicrobial activity against Mycobacterium tuberculosis 16C6 harboring embB320 TTC-TTG(phe-Leu) mutation in embCAB gene after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID448534Cytotoxicity against Mycobacterium bovis Bacillus Calmette-Guerin infected mouse J774 macrophage assessed as cell viability at 100 ug/mL after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
AID1187838Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 as substrate at 0.97 uM after 30 mins by DNA supercoiling assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID143717In vitro antibacterial activity of compound against Mycobacterium avium MAC AN3 (wild type strain) isolated from infected patients.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID1891916Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID529529Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 30167 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1602937Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 5 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1187837Selectivity index, ratio of CC50 for mouse RAW264.7 cells to MIC for Mycobacterium tuberculosis H37Rv2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID574585Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 obtained from sputum of patient at 5 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial 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.
AID599273Antimycobacterial activity against Mycobacterium phlei ATCC 11758 after 3 days by MTT assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID547819Antitubercular activity against Mycobacterium tuberculosis by agar dilution method2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and antitubercular activities of substituted benzoic acid N'-(substituted benzylidene/furan-2-ylmethylene)-N-(pyridine-3-carbonyl)-hydrazides.
AID1187835Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID1782923Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as inhibition of bacterial growth incubated for 9 days by resazurin microtiter assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID522852Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as intracellular bacterial killing2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Ethambutol optimal clinical dose and susceptibility breakpoint identification by use of a novel pharmacokinetic-pharmacodynamic model of disseminated intracellular Mycobacterium avium.
AID725971Inhibition 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 control2013Bioorganic & 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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1180391Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 28 days by agar dilution method2014Bioorganic & 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.
AID1667679Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis G122 incubated for 5 days by alamar blue based colorimetric assay2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from l-serine.
AID429858Antibacterial activity against Mycobacterium smegmatis after 72 hrs2009Journal of natural products, Jun, Volume: 72, Issue:6
Antibacterial diterpenes from Plectranthus ernstii.
AID1076896Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method2014European journal of medicinal chemistry, Apr-09, Volume: 76Development of antimycobacterial tetrahydrothieno[2,3-c]pyridine-3-carboxamides and hexahydrocycloocta[b]thiophene-3-carboxamides: Molecular modification from known antimycobacterial lead.
AID1316914Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA2016Bioorganic & 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.
AID1127156Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay2014European journal of medicinal chemistry, May-22, Volume: 79Facile synthesis of benzonitrile/nicotinonitrile based s-triazines as new potential antimycobacterial agents.
AID1316917Inhibition of Mycobacterium tuberculosis ADH assessed as decrease in conversion of L-alanine to pyruvate by measuring NADH by spectrophotometry2016Bioorganic & 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.
AID444315Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID1602934Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 2 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID454541Antitubercular activity against Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
A highly atom economic, chemo-, regio- and stereoselective synthesis and evaluation of spiro-pyrrolothiazoles as antitubercular agents.
AID1687470Antitubercular activity against PAS/INH/EMB/RMP-resistant Mycobacterium tuberculosis Spec.210 assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID1262209Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of cell growth after 5 days by microplate alamar blue assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
New INH-pyrazole analogs: Design, synthesis and evaluation of antitubercular and antibacterial activity.
AID1224521Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-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.
AID765268T>MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID565994Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by twofold agar dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID534419Antibacterial activity against Mycobacterium bovis BCG-Connaught2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID656227Antimycobacterial activity against isoniazid-, rifampin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1272619Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days by broth microdilution method2016Bioorganic & 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.
AID529540Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 ATC mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial 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.
AID265978Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID1143266Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis 136570 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID495222Antimicrobial activity against Mycobacterium tuberculosis 16C15 harboring embB497 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1316919Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell proliferation at 50 ug/ml after 48 hrs by MTT assay2016Bioorganic & 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.
AID1706677Antitubercular activity against isoniazid/rifampicin multidrug-resistant Mycobacterium tuberculosis FJ05120 clinical isolates assessed as bacterial growth inhibition by MABA2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB.
AID1333272Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 2 times MIC measured after 3 hrs by luciferase reporter gene assay (Rvb = 158.3%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID370115Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 0.5 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID374075Antitubercular activity against Mycobacterium tuberculosis H37Rv after 24 hrs by agar microdilution method2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
A facile synthesis of alpha,alpha'-(EE)-bis(benzylidene)-cycloalkanones and their antitubercular evaluations.
AID670192Selectivity index, ratio of CC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Synthesis of Leubethanol derivatives and evaluation against Mycobacterium tuberculosis.
AID1435651Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID540902Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis Rv8102 harboring embB M306V mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID421760Antibacterial activity against Staphylococcus aureus SA1199B overexpressing NorA efflux pump after 72 hrs2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Bioactive pyridine-N-oxide disulfides from Allium stipitatum.
AID1403701Inhibition 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID406204Inhibition of Mycobacterium tuberculosis fatty acid synthase 1 expressed in Mycobacterium smegmatis mc2 2700 assessed as [2-14C]]malonyl-CoA incorporation into fatty acid at 6000 uM2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Inhibition of isolated Mycobacterium tuberculosis fatty acid synthase I by pyrazinamide analogs.
AID1593371Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID445287Antibacterial activity against Mycobacterium avium SmO by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID540881Antibacterial activity against Mycobacterium tuberculosis B85 harboring embB ATG-ATA (M306I) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1267219Antitubercular activity against multi drug resistant Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis, antimycobacterial screening and ligand-based molecular docking studies on novel pyrrole derivatives bearing pyrazoline, isoxazole and phenyl thiourea moieties.
AID1406779Antitubercular activity against Mycobacterium tuberculosis H37Rv after 1 week by microplate alamar blue assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.
AID563696Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID1602933Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 1 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1573723Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2019Bioorganic & 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.
AID562270Inhibition of Mycobacterium smegmatis EmbC D280G mutant assessed as effect on LAM production at 32ug/ml after 2 hrs by immunoblotting2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1602936Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 4 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1333172Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 after 5 days by broth dilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1311348Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold agar dilution method2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Click-based synthesis and antitubercular evaluation of dibenzofuran tethered thiazolyl-1,2,3-triazolyl acetamides.
AID1400028Inhibition of protein translation/transcription in Escherichia coli S30 cell extract at 0.1 ug/ml using circular DNA with pBESTluc after 60 mins by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID563690Antibacterial activity against Mycobacterium tuberculosis H37Ra by by 7H9 broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID294762Antibacterial activity against methicillin-resistant Staphylococcus aureus 873 after 2 weeks by broth dilution method2007Bioorganic & 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.
AID540895Antibacterial activity against Mycobacterium tuberculosis Rv31 harboring embB GAT-TAT (D328Y) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID529527Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 5041 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID448531Cytotoxicity against mouse J774 macrophage assessed as cell viability at 100 ug/mL after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
AID484649Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Selective one-pot multicomponent synthesis and anti-tubercular evaluation of 5-(aryl/cyclohexylsulfanyl)-2-alkoxy-4,6-diarylnicotinonitriles.
AID1624151Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID599247Antimycobacterial activity against Mycobacterium smegmatis mc2155 after 3 days by MTT assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID540901Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis Rv8101 by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1383954Antimycobacterial activity against MDR Mycobacterium tuberculosis isolate 591 after 15 days by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID1435653Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 7357/1998 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID559762Antimycobacterial activity against Mycobacterium smegmatis MAR4 harboring disrupted PknGMsm gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1594636Antimycobacterial activity against replicating Mycobacterium tuberculosis SS18b assessed as inhibition of parasite growth incubated for 6 days by REMA method2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID1423154Antitubercular activity against Mycobacterium tuberculosis H37Rv harboring dprE1-dprE2 mutant after 10 days in absence of anhydrotetracycline2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery and Structure-Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2'-Oxidase.
AID1573195Antimycobacterial activity against GFP-fused Mycobacterium tuberculosis H37Rv by resazurin dye-based micro-broth dilution method2018Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis.
AID422404Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks2009Journal of natural products, Feb-27, Volume: 72, Issue:2
seco-Abietane diterpenoids, a phenylethanoid derivative, and antitubercular constituents from Callicarpa pilosissima.
AID143707In Vitro antimicrobial activity against the Mycobacterium avium complex (MAC) Wild type strain AN22000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
AID1417198Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as lung mass index at 20 mg/kg, po administered via gavage over 42 days (excluding weekends) (Rvb = 2.28 +/- 0.1 No_unit)2018European journal of medicinal chemistry, Sep-05, Volume: 157Conjugation of a 5-nitrofuran-2-oyl moiety to aminoalkylimidazoles produces non-toxic nitrofurans that are efficacious in vitro and in vivo against multidrug-resistant Mycobacterium tuberculosis.
AID1174925Antitubercular activity against Mycobacterium tuberculosis isolate 756/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug 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.
AID1916624Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition by micro broth dilution assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID540925Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis BAS8 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID370070Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35838 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID437961Antitubercular activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
1,3-Dipolar cycloaddition of C-aryl-N-phenylnitrones to (R)-1-(1-phenylethyl)-3-[(E)-arylmethylidene]tetrahydro-4(1H)-pyridinones: synthesis and antimycobacterial evaluation of enantiomerically pure spiroisoxazolidines.
AID1174924Antitubercular activity against Mycobacterium tuberculosis isolate 439/11 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID245396Minimum inhibitory concentration against Mycobacterium tuberculosis H37Rv pFPCA1 in green fluorescent protein microplate assay2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Identification of heteroarylenamines as a new class of antituberculosis lead molecules.
AID574786Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2403 obtained from sputum of patient at 5 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial 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.
AID422517Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks by proportion method2009Journal of natural products, Jan, Volume: 72, Issue:1
Endiandric Acid Analogues from the Roots of Beilschmiedia erythrophloia.
AID1639085Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue method2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Expansion of a novel lead targeting M. tuberculosis DHFR as antitubercular agents.
AID540870Antibacterial activity against Mycobacterium tuberculosis Rv23 harboring embB ATG-GTG (M306V) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID617850Antitubercular activity against drug sensitive Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay2011Journal of natural products, Sep-23, Volume: 74, Issue:9
Stereochemical analysis of leubethanol, an anti-TB-active serrulatane, from Leucophyllum frutescens.
AID1076895Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method in presence of efflux pump inhibitor verapamil2014European journal of medicinal chemistry, Apr-09, Volume: 76Development of antimycobacterial tetrahydrothieno[2,3-c]pyridine-3-carboxamides and hexahydrocycloocta[b]thiophene-3-carboxamides: Molecular modification from known antimycobacterial lead.
AID613880Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 7 days by microbroth dilution method2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
The structure-activity relationship of urea derivatives as anti-tuberculosis agents.
AID294764Antibacterial activity against methicillin-resistant Staphylococcus aureus 908 after 2 weeks by broth dilution method2007Bioorganic & 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.
AID529530Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-GTG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1383958Ratio of MBC to MIC for MDR Mycobacterium tuberculosis isolate 5912018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID1372627Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week by MABA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID370254Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 20 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID355266Antitubercular activity against Mycobacterium tuberculosis H37Rv after 21 days by broth microdilution method1997Journal of natural products, Dec, Volume: 60, Issue:12
Norditerpenoids and diterpenoids from Salvia multicaulis with antituberculous activity.
AID1506729Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 28 days2017MedChemComm, Mar-01, Volume: 8, Issue:3
Design, synthesis, molecular-docking and antimycobacterial evaluation of some novel 1,2,3-triazolyl xanthenones.
AID564988Antimicrobial activity against Mycobacterium bovis BCG harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1072705Inhibition of Mycobacterium tuberculosis pantothenate synthetase expressed in Escherichia coli BL21 (DE3)2014Bioorganic & 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.
AID1224517Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 234/2005 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-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.
AID444316Cytotoxicity against mouse J774 cells assessed as cell viability at 1 ug/ml by MTT assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1163979Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay in presence of 8 mg/mL piperine efflux pump inhibitor2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID510542AUC (0 to 24 hrs) in diabetic tuberculosis patient at 15 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID564978Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring inactivated p55 gene by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1296384Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 9449/2007 after 14 days by microdilution method2016Journal 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.
AID441082Ratio of ethambutol MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 272942009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID574807Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 horboring rpoB S531L/Q510P, katG S315T/R463L, gyrA D94N/S95T, rrs G1484T by CLSI method2010Antimicrobial 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.
AID1138419Antimicrobial activity against Mycobacterium tuberculosis after 7 to 21 days by microdilution method2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Multitarget drug discovery for tuberculosis and other infectious diseases.
AID1854055Anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 5 days by alamar blue assay2022RSC medicinal chemistry, Mar-23, Volume: 13, Issue:3
Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-
AID143708In Vitro antimicrobial activity against the Mycobacterium avium complex (MAC) Wild type strain AN32000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
AID294760Antibacterial activity against Mycobacterium avium 724S after 2 weeks by broth dilution method2007Bioorganic & 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.
AID540906Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis Rv4402 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID445330Cytotoxicity against human A549 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1333139Induction of membrane disruption in Mycobacterium smegmatis MC2 155 assessed as increased cytoplasmic membrane permeability at 60 uM up to 3 hrs by Sytox green uptake assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID370119Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po after 8 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID495217Antimicrobial activity against Mycobacterium tuberculosis 16C11 harboring embB397 CCG-TCG(Pro-Ser) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1464092Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis G122 assessed as inhibition of mycobacterial growth incubated for 2 weeks by MABA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
meso-Dihydroguaiaretic acid derivatives with antibacterial and antimycobacterial activity.
AID1624149Antitubercular activity against isoniazid/ethionamide resistant Mycobacterium tuberculosis isolate 1 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID540893Antibacterial activity against Mycobacterium tuberculosis B79 harboring embB GGC-CGC (G324R) mutation in embB by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID495203Antimicrobial activity against wild type Mycobacterium tuberculosis 8C2 after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID562267Antimicrobial activity against Mycobacterium tuberculosis harboring Mycobacterium smegmatis embB M292I mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1174106Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1706678Antitubercular activity against isoniazid/rifampicin/streptomycin/capreomycin/ofloxacin extensively drug-resistant Mycobacterium tuberculosis FJ05195 clinical isolates assessed as bacterial growth inhibition by MABA2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB.
AID1383957Ratio of MBC to MIC for Mycobacterium tuberculosis H37Rv2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID495474Antimicrobial activity against Mycobacterium tuberculosis NJT210TCC harboring embB406 GGC-TCC(Gly-Ser) mutation in embB gene after 4 weeks2010Antimicrobial 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.
AID1143270Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis 12119 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID565656Antimicrobial activity against Mycobacterium smegmatis expressing EmbC gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID548358Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010European 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.
AID1782926Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID665277Antitubercular activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2012European journal of medicinal chemistry, Jul, Volume: 53A 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.
AID565230Antimicrobial activity against Mycobacterium chelonae 9917 by resazurine microtiter assay2009Antimicrobial 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.
AID529528Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT30167 expressing embB codon 306 ATG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial 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.
AID1143267Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis 912253 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal 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.
AID145272Minimum inhibitory concentration against Mycobacterium tuberculosis2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents.
AID1891907Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth measured after 7 days by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID445286Antibacterial activity against Mycobacterium avium 724S by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1609006Antimycobacterial activity against Mycobacterium smegmatis DSM 43465 after 120 hr by resazurin dye based microdilution method2019European journal of medicinal chemistry, Nov-01, Volume: 181Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.
AID445285Antibacterial activity against Mycobacterium bovis BCG str. Tokyo 172 by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID656233Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, ethambutol-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1390094Antimycobacterial activity against active form of Mycobacterium tuberculosis H37Rv measured after 7 days by alamar blue assay2018Bioorganic & 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.
AID658437Antibacterial activity against Mycobacterium smegmatis mc2 155 after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Compounds of Alpinia katsumadai as potential efflux inhibitors in Mycobacterium smegmatis.
AID1557254Antitubercular activity against resistant Mycobacterium tuberculosis harboring embCAB Gly406Asp/Ala mutant2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID565658Antimicrobial activity against Mycobacterium smegmatis expressing EmbC M286L mutant gene after 48 hrs by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis.
AID1590012Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 25 ug/ml incubated for 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Ultrasonication-ionic liquid synergy for the synthesis of new potent anti-tuberculosis 1,2,4-triazol-1-yl-pyrazole based spirooxindolopyrrolizidines.
AID1916597Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition measured after 5 days by MABA method2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1272621Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 14 days by broth microdilution method2016Bioorganic & 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.
AID1173784Inhibition of Mycobacterium tuberculosis DNA gyrase using relaxed pBR322 as substrate after 30 mins by supercoiling assay2014Bioorganic & 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.
AID580997Antimicrobial activity against Mycobacterium tuberculosis infected in patients with tuberculosis assessed as percentage of patients with negative culture after 4 weeks2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1464093Antimycobacterial activity against isoniazid/rifampicin/streptomycin-resistant Mycobacterium tuberculosis G133 assessed as inhibition of mycobacterial growth incubated for 2 weeks by MABA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
meso-Dihydroguaiaretic acid derivatives with antibacterial and antimycobacterial activity.
AID370243Cmax in Mycobacterium bovis BCG infected tuberculosis mouse model at 100 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1196885Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID646114Antitubercular activity against multi-drug-resistant Mycobacterium tuberculosis H37Rv clinical isolate after 28 days by 10 fold serial dilution method2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Camphorsulfonic acid catalysed facile tandem double Friedlander annulation protocol for the synthesis of phenoxy linked bisquinoline derivatives and discovery of antitubercular agents.
AID551505Cytotoxicity against human MRC5 cells assessed as metabolic active cells at 100 uM after 72 hrs by XTT assay relative to control2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.
AID294763Antibacterial activity against methicillin-resistant Staphylococcus aureus 906 after 2 weeks by broth dilution method2007Bioorganic & 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.
AID1782925Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID694236Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic condition assessed as growth inhibition at 5 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID445210Antituberculosis activity against Mycobacterium tuberculosis H37Rv by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1435649Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 4 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1691024Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis clinical isolate measured after 1 week by microplate alamar blue assay2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1331257Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by micro plate alamar blue assay2017Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
Synthesis, screening and docking analysis of hispolon analogs as potential antitubercular agents.
AID1296386Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 1 after 14 days by microdilution method2016Journal 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.
AID289157Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 days by colorimetric microassay2007Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17
Synthesis and biological evaluation of conformationally constrained analogues of the antitubercular agent ethambutol.
AID1403704Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 1 week in presence of piperine by MABA method2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID523296Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as assessed as lowest concentration to reduce bacterial burden in lungs to level of reduction achieved with higher doses orally treated in water-1% methylcel2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID551507Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 after 72 hrs by broth microtiter dilution method2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.
AID495215Antimicrobial activity against wild type Mycobacterium tuberculosis 16C10 after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID1167608Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis XDR-TB after 28 days by two-fold agar dilution method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.
AID442659Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010European 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.
AID1577339Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 8666/2010 after 14 days2019Journal 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.
AID143716In vitro antibacterial activity of compound against Mycobacterium avium MAC AN2 wild type strain) isolated from infected patients.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID540919Antibacterial activity against HYG cassette-positive Mycobacterium tuberculosis RvAS4 harboring embB M306I mutant gene by modified conventional agar proportion method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Mutations at embB codon 306 are an important molecular indicator of ethambutol resistance in Mycobacterium tuberculosis.
AID1437020Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis clinical isolate after 4 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
AID145137In vitro antibacterial activity against Mycobacterium tuberculosis MT-1 (wild type strain) isolated from infected patients.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics.
AID1378016Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by MABA2017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID495212Antimicrobial activity against Mycobacterium tuberculosis 16C7 harboring embB445 CAG-CGG(Gln-Arg) mutation in embCAB gene after 4 weeks by Bactec 460TB method2010Antimicrobial 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.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID738686Lipophilicity, log P of the compound2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
Synthesis and biological evaluation of trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxyalkylamine derivatives against drug susceptible, non-replicating M. tuberculosis H37Rv and clinical multidrug resistant strains.
AID445290Antibacterial activity against Escherichia coli by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID445332Selectivity for Mycobacterium tuberculosis H37Rv over human THP1 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1403702Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 1 week by MABA method2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID563695Antibacterial activity against rifampin-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID594787Antituberculosis activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
A green expedient synthesis of pyridopyrimidine-2-thiones and their antitubercular activity.
AID1333266Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 4 times MIC measured after 1 hr by luciferase reporter gene assay (Rvb = 90.6%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID495232Antimicrobial activity against wild type Mycobacterium tuberculosis 210 after 4 weeks2010Antimicrobial 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.
AID495218Antimicrobial activity against wild type Mycobacterium tuberculosis 16C12 after 4 weeks by 7H agar proportion method2010Antimicrobial 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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,121)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901749 (42.44)18.7374
1990's492 (11.94)18.2507
2000's649 (15.75)29.6817
2010's951 (23.08)24.3611
2020's280 (6.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 82.68

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.

MetricThis Compound (vs All)
Research Demand Index82.68 (24.57)
Research Supply Index8.48 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index151.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (82.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials366 (8.22%)5.53%
Reviews265 (5.95%)6.00%
Case Studies812 (18.23%)4.05%
Observational19 (0.43%)0.25%
Other2,992 (67.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (86)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 2/3, Multicenter, Randomized, Open-label, Active-controlled Study to Evaluate the Efficacy and Safety of Bedaquiline Administered as Part of a Treatment Regimen With Clarithromycin and Ethambutol in Adult Patients With Treatment-refractory Mycobac [NCT04630145]Phase 2/Phase 3124 participants (Anticipated)Interventional2021-01-08Recruiting
A Randomized, Double-Blind, Placebo-Controlled, Active Comparator, Multicenter Study to Evaluate the Efficacy and Safety of an Amikacin Liposome Inhalation Suspension (ALIS)-Based Regimen in Adult Subjects With Newly Diagnosed Nontuberculous Mycobact [NCT04677569]Phase 3250 participants (Anticipated)Interventional2021-04-01Recruiting
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 161 participants (Actual)Interventional2015-07-07Completed
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 116 participants (Anticipated)Interventional2022-01-04Recruiting
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 3394 participants (Actual)Interventional2002-04-08Completed
STREAM: The Evaluation of a Standard Treatment Regimen of Anti-tuberculosis Drugs for Patients With MDR-TB [NCT02409290]Phase 3588 participants (Actual)Interventional2016-03-31Completed
The Study of Standardized Preoperative Anti-tuberculosis Treatment of Surgical Treatment of Spinal Tuberculosis Patients [NCT02477852]Phase 4400 participants (Anticipated)Interventional2015-04-30Recruiting
Randomized, Open Label, Multiple Dose Phase 2a Study of the Early Bactericidal Activity of AZD5847 in Adults With Pulmonary Tuberculosis [NCT01516203]Phase 275 participants (Actual)Interventional2012-12-05Completed
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)Interventional2013-11-30Completed
Population Pharmacokinetics of Anti-tuberculosis Drugs in Children With Tuberculosis [NCT03625739]800 participants (Anticipated)Observational [Patient Registry]2018-07-01Recruiting
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 41,050 participants (Actual)Interventional2014-09-30Completed
A Seamless Phase 2B/C Platform Trial to Evaluate Multiple Regimens and Durations of Treatment in Pulmonary Tuberculosis [NCT06114628]Phase 22,500 participants (Anticipated)Interventional2023-12-08Not yet recruiting
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) [NCT04310930]Phase 2/Phase 3300 participants (Anticipated)Interventional2020-03-02Recruiting
Characterization of Immune Responses in Treatment-induced Latency in Pulmonary Tuberculosis [NCT01154959]Phase 3120 participants (Actual)Interventional2010-02-28Completed
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 360 participants (Anticipated)Interventional2016-05-30Recruiting
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 3672 participants (Actual)Interventional2017-02-01Completed
Rosuvastatin Evaluation as a Tuberculosis Treatment Adjunct [NCT04504851]Phase 2154 participants (Anticipated)Interventional2020-08-12Not yet recruiting
A Phase 1 Study to Evaluate the Effect of Co-administration on the Pharmacokinetics of SPR720, Azithromycin, and Ethambutol in Healthy Volunteers [NCT05966688]Phase 133 participants (Actual)Interventional2023-08-04Completed
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 2112 participants (Anticipated)Interventional2021-08-03Recruiting
Multicenter, Randomized Study Evaluating the Value of Antitubercular Treatment During Recurent Anterior Uveitis (URBA) [NCT04117698]Phase 3116 participants (Anticipated)Interventional2019-11-01Not yet recruiting
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)Observational2017-03-03Terminated(stopped due to According to Sponsor decision.)
A Randomized Controlled Clinical Trial Comparing Daily Vs. Intermittent 6 - Month Short Course Chemotherapy in Reducing Failures & Emergence of Acquired Rifampicin Resistance (ARR) in Patients With HIV and Pulmonary Tuberculosis [NCT00933790]Phase 3331 participants (Actual)Interventional2009-09-14Completed
Phase I/II Study of the Effects of Antibiotics on Sarcoidosis Pathogenesis [NCT01074554]Phase 1/Phase 230 participants (Actual)Interventional2010-02-28Completed
An Open-Label, Randomized Trial of Four Treatment Regimens for Patients With Disseminated Mycobacterium Avium Complex Disease and Acquired Immunodeficiency Syndrome (AIDS) [NCT00001047]Phase 3400 participants InterventionalCompleted
Substitution of Ethambutol With Linezolid During the Intensive Phase of Treatment of Pulmonary Tuberculosis: A Prospective, Multicenter, Randomized, Open-label Phase II Trial [NCT01994460]Phase 2429 participants (Anticipated)Interventional2014-01-31Recruiting
Investigation of the Efficacy of Antimycobacterial Therapy on Pulmonary Sarcoidosis Phase II Randomized, Double-blind, Placebo-controlled Trial [NCT02024555]Phase 297 participants (Actual)Interventional2014-03-31Completed
The Treatment of Pulmonary Mycobacterium Tuberculosis in HIV Infection [NCT00001033]Phase 3650 participants InterventionalCompleted
A Phase IIc Trial of Clofazimine- and Rifapentine-Containing Treatment Shortening Regimens in Drug-Susceptible Tuberculosis: The CLO-FAST Study [NCT04311502]Phase 2104 participants (Actual)Interventional2021-06-16Active, not recruiting
Reducing Early Mortality and Early Morbidity by Empiric Tuberculosis Treatment Regimens (REMEMBER) [NCT01380080]Phase 4851 participants (Actual)Interventional2011-10-31Completed
Investigation of the Efficacy of Antibiotics on Pulmonary Sarcoidosis [NCT01169038]Phase 115 participants (Actual)Interventional2010-07-31Completed
Efficacy of Thrice Weekly Intermittent Short Course Antituberculosis Chemotherapy in Tuberculosis Patients With and Without HIV Infection [NCT00698334]Phase 3150 participants (Anticipated)Interventional2006-04-30Completed
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)Interventional2020-03-01Not yet recruiting
CLArithromycin Versus AZIthromycin in the Treatment of Mycobacterium Avium Complex (MAC) Lung Infections [NCT03236987]Phase 3424 participants (Anticipated)Interventional2018-02-05Recruiting
Shortened Regimens for First Diagnosed Smear Positive Drug Susceptible Pulmonary Tuberculosis: a Randomised Controlled Non-inferiority Trial [NCT02901288]Phase 43,900 participants (Anticipated)Interventional2016-08-31Recruiting
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 3570 participants (Actual)Interventional2007-12-31Completed
Testing New Strategies for Patients Hospitalised With HIV-associated Disseminated Tuberculosis [NCT04951986]Phase 3732 participants (Anticipated)Interventional2021-08-11Recruiting
A Randomized Open-Label Study of the Tolerability and Efficacy of Clarithromycin and Ethambutol in Combination With or Without Clofazimine for the Treatment of Disseminated MAC (dMAC) in Patients With AIDS [NCT00002331]0 participants Interventional1994-01-31Completed
TBTC Study 28: Evaluation of a Moxifloxacin-based, Isoniazid-sparing Regimen for Tuberculosis Treatment [NCT00144417]Phase 2433 participants (Actual)Interventional2006-02-28Completed
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 3288 participants (Anticipated)Interventional2023-03-01Not yet recruiting
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)Observational2014-11-30Completed
Pharmacokinetics of Antituberculosis Agents in HIV-Infected Persons With Tuberculosis [NCT00000950]50 participants InterventionalCompleted
Tolerance, Safety, and Activity of Rifapentine Alone and in Combination Therapy in AIDS Patients With Mycobacterium Avium Complex Bacteremia. [NCT00002192]Phase 20 participants InterventionalCompleted
TBTC Study 24: A Non-Comparative Study of the Efficacy of a Largely-Intermittent, Six-Month Tuberculosis Treatment Regimen Among Patients Who Will Not Receive Isoniazid Due to Initial Isoniazid Resistance or Intolerance [NCT00023374]98 participants (Actual)Interventional2000-08-31Completed
A Phase II/III Trial of Rifampin, Ciprofloxacin, Clofazimine, Ethambutol, and Amikacin in the Treatment of Disseminated Mycobacterium Avium Infection in HIV-Infected Individuals. [NCT00000641]Phase 290 participants InterventionalCompleted
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 2121 participants (Actual)Interventional2009-11-30Terminated(stopped due to Funding withdrawn)
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 31,931 participants (Actual)Interventional2008-01-31Completed
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 2365 participants (Actual)Interventional2013-04-30Completed
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 3284 participants (Actual)Interventional2015-02-28Completed
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 2113 participants (Actual)Interventional2014-11-30Completed
Hypertonic Saline for Treatment of Pulmonary Mycobacterium Avium Complex (MAC) Disease [NCT04921943]Phase 450 participants (Anticipated)Interventional2021-05-18Recruiting
Comparison of Two- Versus Three-antibiotic Therapy for Pulmonary Mycobacterium Avium Complex Disease [NCT03672630]Phase 2/Phase 3500 participants (Anticipated)Interventional2019-02-22Recruiting
Evaluation of the Pharmacokinetics of Antituberculosis Drugs and Tuberculosis Treatment Outcomes in HIV-tuberculosis Co-infected Ugandan Adults [NCT01782950]Phase 4400 participants (Anticipated)Interventional2013-02-28Recruiting
A Randomized Controlled Non-Inferiority Study for Shortening Tuberculosis Treatment With Sitafloxacin-Containing Regimens [NCT05454345]Phase 3620 participants (Anticipated)Interventional2022-10-01Not 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 2240 participants (Actual)Interventional2014-10-23Completed
An Open-Label Randomized Pharmacokinetic/Pharmacodynamic Study of Mycobutin (Rifabutin) or Rifabutin in Combination With Myambutol (Ethambutol) for Prophylaxis of Mycobacterium Avium Complex (MAC) Bacteremia in AIDS Patients With CD4 Counts <= 100 Cells/m [NCT00002343]Phase 4200 participants InterventionalCompleted
Using Biomarkers to Predict TB Treatment Duration [NCT02821832]Phase 2946 participants (Actual)Interventional2017-06-21Active, not recruiting
Randomized Clinical Trial to Assess the Efficacy of Short Course Intermittent Regimens for the Treatment of HIV-Associated Tuberculosis [NCT00376012]Phase 3300 participants (Actual)Interventional2001-02-28Active, 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 240 participants (Anticipated)Interventional2022-11-30Recruiting
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 InterventionalCompleted
New Super-short Course Regimen for Retreatment Pulmonary Tuberculosis [NCT02331823]Phase 4864 participants (Anticipated)Interventional2013-06-30Recruiting
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 271 participants (Actual)Interventional2013-07-13Terminated(stopped due to The study was stopped early due to feasibility concerns.)
A Randomized, Double-Blind, Comparative Study of Azithromycin Versus Clarithromycin in Combination With Ethambutol for the Treatment of Disseminated Mycobacterium Avium Complex (MAC) Infection in AIDs Patients [NCT00002140]Phase 30 participants InterventionalCompleted
Pharmacokinetic Evaluation of Nontuberculous Mycobacterial Antibiotics in Cystic Fibrosis Versus Controls [NCT02372383]31 participants (Actual)Interventional2014-10-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Active Comparator, Multicenter Study to Validate Patient-Reported Outcome Instruments in Adult Subjects With Newly Diagnosed Nontuberculous Mycobacterial (NTM) Lung Infection Caused by Mycobacterium Avi [NCT04677543]Phase 399 participants (Actual)Interventional2020-12-22Completed
Evaluation of Two Different Preventive Therapy Regimens for Tuberculosis in HIV Infected Persons [NCT00351702]Phase 3650 participants (Actual)Interventional2001-02-28Completed
A Phase II/III Prospective, Multicenter, Randomized, Controlled Trial Comparing the Safety and Efficacy of Three Clarithromycin-Containing Combination Drug Regimens for the Treatment of Disseminated Mycobacterium Avium Complex (MAC) Disease in Persons Wit [NCT00001058]Phase 2246 participants InterventionalCompleted
The Effect of Therapy on the Tissue Burden of Disseminated MAC Infection as Measured by Quantitative Bone Marrow Culture and Correlation With Quantitative Blood Culture in HIV-Infected Patients [NCT00001039]Phase 224 participants InterventionalCompleted
A Three-Arm Comparative Trial for the Treatment of MAC Bacteremia in AIDS: A Clarithromycin/Ethambutol Regimen Containing Rifabutin (450 Mg) or Rifabutin (300 Mg) or Placebo [NCT00002101]Phase 3450 participants InterventionalCompleted
Viral and Immune Dynamics in HIV-Infected Patients With Tuberculosis [NCT00004736]Phase 144 participants InterventionalCompleted
Treatment of Pulmonary Disease Caused by MAIS, M.Xenopi or M.Malmoense: A Comparison of Two Triple Drug Regimens and an Assessment of the Value of Immunotherapy With M.Vaccae [NCT00367913]Phase 4400 participants Interventional1995-03-31Completed
Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis [NCT03474198]Phase 2/Phase 3675 participants (Actual)Interventional2018-03-21Completed
[NCT00004689]Phase 250 participants Interventional1991-01-31Completed
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 3402 participants (Actual)Interventional2019-08-22Active, not recruiting
A Multicenter, Randomized, Open-Label Study To Evaluate The Efficacy And Safety Of A Contezolid, Delamanid and Bedaquiline-Containing Short Regimen For The Treatment Of Rifampicin-Resistant Pulmonary Tuberculosis [NCT06081361]Phase 3186 participants (Anticipated)Interventional2023-11-01Not yet 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)Observational2021-10-01Not yet recruiting
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 277 participants (Actual)Interventional2019-11-15Completed
Population Pharmacokinetics Analysis of Ethambutol in Overweight and Obese Volunteers [NCT01048697]Phase 418 participants (Actual)Interventional2010-01-31Completed
Essentiality of Isoniazid in Tuberculosis Therapy [NCT01589497]Phase 269 participants (Actual)Interventional2015-06-30Completed
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 2514 participants (Anticipated)Interventional2023-07-26Recruiting
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 2157 participants (Actual)Interventional2015-04-29Completed
Novel Triple-dose Tuberculosis Retreatment Regimen: How to Overcome Resistance Without Creating More in Niger [NCT04260477]Phase 3370 participants (Anticipated)Interventional2021-03-01Recruiting
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 2330 participants (Anticipated)Interventional2024-01-02Not 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 3455 participants (Actual)Interventional2018-07-30Completed
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 2156 participants (Anticipated)Interventional2023-10-31Not 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 3926 participants (Anticipated)Interventional2020-09-30Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00042289 (26) [back to overview]Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00130247 (6) [back to overview]Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-TB Treatment - Per-protocol
NCT00130247 (6) [back to overview]Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-tuberculosis (TB) Treatment - Intention-to-treat
NCT00130247 (6) [back to overview]Relapses at 1 and 2 Years
NCT00130247 (6) [back to overview]Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Intention to Treat
NCT00130247 (6) [back to overview]Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Per Protocol
NCT00130247 (6) [back to overview]Acquired Drug Resistance in Patients Who Relapsed
NCT00728507 (1) [back to overview]To Compare, by Treatment Group, the Percentage of Patients With a Negative Sputum Culture at the End of Intensive Phase Therapy.
NCT00864383 (9) [back to overview]Combined Failure of Bacteriological Cure and Relapse as Defined by Culture Using Liquid Media (Mycobacteria Growth Indicator Tube-MGIT).
NCT00864383 (9) [back to overview]Combined Failure of Bacteriological Cure and Relapse Within One Year of Completion of Therapy as Defined by Culture Using Solid Media (Lowenstein-Jensen - LJ).
NCT00864383 (9) [back to overview]Number of Patients Who Are Culture Negative (Liquid MGIT Culture)
NCT00864383 (9) [back to overview]Number of Patients Who Are Culture Negative (Solid LJ Culture)
NCT00864383 (9) [back to overview]Number of Patients With Grade 3 or 4 Adverse Events (Using a Modified Division of Acquired Immunodeficiency Syndrome National Institute of Allergy and Infectious Diseases [DAIDS] Scale of Adverse Event Reporting)
NCT00864383 (9) [back to overview]Sensitivity Analyses Assuming All Losses to Follow-up and Non-tuberculous Deaths Have a Favourable Outcome Using Solid (L-J) Media.
NCT00864383 (9) [back to overview]Sensitivity Analysis Assuming All Losses to Follow-up and Non-tuberculous Deaths Have an Unfavorable Outcome Using Solid (L-J) Media.
NCT00864383 (9) [back to overview]Time to First Culture Negative Sputum Sample (LJ Solid Media)
NCT00864383 (9) [back to overview]Time to First Culture Negative Sputum Sample (MGIT Liquid Media)
NCT01048697 (1) [back to overview]Total Clearance of Ethambutol
NCT01074554 (3) [back to overview]Change in Lesion Size at the Completion of Antibiotic Therapy, Measured on a Continuous Scale; Change Will be Determined by Change in Diameter of the Lesions
NCT01074554 (3) [back to overview]Change in Modified Sarcoidosis Activity and Severity Index (SASI) at Completion of Therapy.
NCT01074554 (3) [back to overview]Granuloma Burden
NCT01169038 (1) [back to overview]Change in Absolute FVC From Baseline to Post Completion of 8 Weeks of Antibiotic Therapy.
NCT01380080 (16) [back to overview]Proportion of Participants With Reportable Hospitalization by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With HIV-1 RNA Level <400 Copies/mL
NCT01380080 (16) [back to overview]CD4+ T-cell Count Change From Baseline
NCT01380080 (16) [back to overview]CD4+ T-cell Count
NCT01380080 (16) [back to overview]Time to Initiation of TB Treatment by Week 96
NCT01380080 (16) [back to overview]Proportion of Participants With TB Diagnosis by Week 96
NCT01380080 (16) [back to overview]Proportion of Participants With Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48
NCT01380080 (16) [back to overview]Cumulative Probability of Death by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of Death or AIDS Progression by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of Death or AIDS Progression by Week 48
NCT01380080 (16) [back to overview]Cumulative Probability of Death or Unknown Vital Status by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of First AIDS Progression by Week 96
NCT01380080 (16) [back to overview]Proportion of Participants Who Prematurely Discontinued Antiretroviral Therapy by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants Who Prematurely Discontinued Any Component of TB Treatment by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With at Least One New Grade 3 or 4 Adverse Event That is at Least a One-grade Increase From Baseline by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With at Least One New Grade 3 or 4 Targeted Laboratory Value That is at Least a One-grade Increase From Baseline by Week 48
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CL/F at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CLast at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CLast at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter Cmax at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter Cmax at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter CL/F at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter CLast at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter Cmax at Day 14
NCT01589497 (32) [back to overview]AUC0-24hour for Ethambutol (EMB)
NCT01589497 (32) [back to overview]AUC0-24hour for Pyrazinamide (PZA)
NCT01589497 (32) [back to overview]Ethambutol PK Parameter CLast
NCT01589497 (32) [back to overview]Ethambutol PK Parameter Cmax
NCT01589497 (32) [back to overview]Log10 Transformed Colony-forming Unit (CFU) Count Per mL From Sputum Samples at Baseline and Day 14
NCT01589497 (32) [back to overview]Pharmacokinetic Parameter (PK) Area Under the Concentration-time Curve (AUC0-24hour) for Rifampicin (RIF)
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter CL/F
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter CLast
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter Cmax
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Clearance (CL/F)
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Last Concentration (CLast)
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Maximum Plasma Concentration (Cmax)
NCT01589497 (32) [back to overview]Ethambutol PK Parameter CL/F
NCT01589497 (32) [back to overview]AUC0-24hour for Isoniazid (INH) at Day 1
NCT01589497 (32) [back to overview]AUC0-24hour for Isoniazid at Day 14
NCT01589497 (32) [back to overview]AUC0-24hour for Moxifloxacin (Mox) at Day 14
NCT01589497 (32) [back to overview]Correlation Between Time to Positivity (TTP) and log10 Transformed Colony-forming Unit (CFU) Counts Per mL
NCT01589497 (32) [back to overview]Daily Change in log10 Colony-forming Unit (CFU) Counts Per mL Sputum From Day 2 to Day 14
NCT01589497 (32) [back to overview]Daily Change in log10 Transformed Colony-forming Unit (CFU) Counts Per mL Sputum From Baseline (Study Treatment Initiation) to Day 2
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 14
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 2
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Day 2 to Day 14
NCT01589497 (32) [back to overview]Daily Decrease in log10 Transformed Colony-forming Unit (CFU) Counts Per ml Sputum From Baseline (Study Treatment Initiation) to Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CL/F at Day 1
NCT01601626 (26) [back to overview]RBT Cmax and Cmin in Participants Enrolled in Arms A and C
NCT01601626 (26) [back to overview]RAL AUC in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Treatment Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced HIV Virologic Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness or Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence
NCT01601626 (26) [back to overview]LPV AUC in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Sign or Symptom
NCT01601626 (26) [back to overview]Number of Participants Who Experienced MTB IRIS
NCT01601626 (26) [back to overview]Percent of Participants Who Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced Sputum Conversion at Week 8.
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 8
NCT01601626 (26) [back to overview]Cumulative Probability of HIV Virologic Failure at Week 72
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 24
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 48
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 72
NCT01601626 (26) [back to overview]RBT AUC in Participants Enrolled in Arms A and C
NCT01601626 (26) [back to overview]LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]RAL Cmax and Cmin in Participants Enrolled in Arm C
NCT01785186 (3) [back to overview]Frequency of Adverse Events
NCT01785186 (3) [back to overview]Sputum Culture Conversion (2 Negative Cultures) Using Liquid Media
NCT01785186 (3) [back to overview]Pharmacokinetics Including AUC, Cl, t1/2, Vd, and Protein Binding
NCT02024555 (8) [back to overview]Adverse Events
NCT02024555 (8) [back to overview]Abnormal Lab Values
NCT02024555 (8) [back to overview]Failure of Standard Therapy
NCT02024555 (8) [back to overview]Change in the Saint George's Respiratory Questionnaire (SGRQ)
NCT02024555 (8) [back to overview]Change in Percent Predicted Absolute Forced Vital Capacity (FVC) in Participants With Pulmonary Sarcoidosis, Comparing Baseline With Performance After Completion of 16 Weeks of Therapy.
NCT02024555 (8) [back to overview]Six Minute Walk, Distance in Meters
NCT02024555 (8) [back to overview]FEV1%
NCT02024555 (8) [back to overview]Change in Oxygen Saturation
NCT02193776 (2) [back to overview]Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System
NCT02193776 (2) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02256696 (8) [back to overview]Number of Participants With Permanent Discontinuation of Assigned Study Regimen
NCT02256696 (8) [back to overview]Number of Participants With Grade 3 or Higher Adverse Events
NCT02256696 (8) [back to overview]PK (Cmax) of PA-824 at 200 mg Once Daily With Rifampin or Rifabutin-containing Treatment
NCT02256696 (8) [back to overview]Relationship Between PA-824 Exposure (AUC) and Rate of Change in Time to Positivity (TTP) Over 12 Weeks
NCT02256696 (8) [back to overview]Steady State Pharmacokinetics (PK) (AUC) of PA-824 When Given With Rifampin or Rifabutin
NCT02256696 (8) [back to overview]Percentage of Participants With Sputum Culture Conversion by 8 Weeks of Treatment
NCT02256696 (8) [back to overview]Time to Culture Conversion on Solid Medium
NCT02256696 (8) [back to overview]Time to Sputum Culture Conversion on Liquid Medium
NCT02372383 (10) [back to overview]Other PK Measures: Median Time to Maximal Drug Concentration (Tmax)
NCT02372383 (10) [back to overview]Other PK Measures: Half-life (t1/2)
NCT02372383 (10) [back to overview]Other PK Measures: Drug Clearance
NCT02372383 (10) [back to overview]Covariates of PK Measures: Body Mass Index
NCT02372383 (10) [back to overview]Covariates of PK Measures: C-reactive Protein (CRP)
NCT02372383 (10) [back to overview]Median Maximal Drug Concentration (Cmax)
NCT02372383 (10) [back to overview]Area Under the Curve (AUC)
NCT02372383 (10) [back to overview]Covariates of PK Measures: Creatinine
NCT02372383 (10) [back to overview]Other PK Measures: Volume of Distribution (Vd)
NCT02372383 (10) [back to overview]Covariates of PK Measures: Circulating Neutrophil Count
NCT02409290 (5) [back to overview]STREAM Stage 2 Primary Outcome Measure (the Proportion of Patients With a Favourable Outcome at Week 76)
NCT02409290 (5) [back to overview]Proportion of Patients With Acquired Drug Resistance
NCT02409290 (5) [back to overview]Favourable Outcome After Long-term Follow-up (132 Weeks)
NCT02409290 (5) [back to overview]Failure or Recurrence (FoR)
NCT02409290 (5) [back to overview]Failure or Recurrence (FoR)
NCT02554318 (6) [back to overview]Caloric Intake on 24-hour Dietary Recall Method at the 2nd and 6th.
NCT02554318 (6) [back to overview]Change in Distance on 6-minute Walk Test (6MWT) From Baseline at 2 Months
NCT02554318 (6) [back to overview]Change in Bodyweight on a Digital Weight Scale From Baseline at 2 Months
NCT02554318 (6) [back to overview]Change in Body Mass Index (BMI) From Baseline at 2 Months
NCT02554318 (6) [back to overview]Change in Hand-grip Strength on a Digital Dynamometer Scale From Baseline at 2 Months
NCT02554318 (6) [back to overview]Protein Intake on 24-hour Dietary Recall Method.
NCT02821832 (1) [back to overview]Comparison of the Rate of Treatment Success at 18 Months (After Treatment Initiation) Between Arms B and C
NCT03338621 (2) [back to overview]Number of Participants With Culture Negative Status by 8 Weeks
NCT03338621 (2) [back to overview]Time to Culture Negative Status

Plasma Concentration for Contraceptives

Serum concentrations of the contraceptives. Note that no historical controls were provided by team pharmacologists and thus no comparisons were done for contraceptive concentrations in women using hormonal contraceptives and selected ARV drugs as compared to historical controls not using those ARV drugs. (NCT00042289)
Timeframe: Measured at 6-7 weeks after contraceptive initiation postpartum

Interventionpg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG604
LPV/RTV 400/100 b.i.d. With ENG428
EFV 600mg q.d. With ENG125

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.1.602.05

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.1.9691.6692.387

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PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.360.480.38
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.130.130.28
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.3.75.17.2
RAL 400mg b.i.d.0.06210.0640.0797

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PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.2.842.524.51
DRV/RTV 600/100mg b.i.d.2.122.222.51
FPV/RTV 700/100mg b.i.d.2.121.642.87
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA0.470.52

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PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

Interventionng/mL (Geometric Mean)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.108128

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionng/mL (Median)
2nd Trimester3rd TrimesterPostpartum
EVG/COBI 150/150mg q.d.1447.11432.81713.1
TAF 10mg q.d. w/COBI80.491.298.2
TAF 25mg q.d.69.796133
TAF 25mg q.d. w/COBI or RTV Boosting87.8107141

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionng/mL (Median)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.448647

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.701.010.63
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.8.410.714.6
RAL 400mg b.i.d.2.2501.7703.035
RPV 25mg q.d.0.1450.1340.134

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.2.822.203.90
ATV/RTV Arm 1: 300/100mg q.d.NA3.64.1
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.3.114.514.52
DRV/COBI 800/150 mg q.d.4.593.677.04
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.6.226.558.96
DRV/RTV 600/100mg b.i.d.5.645.537.78
DRV/RTV 800/100mg q.d.6.775.788.11
DTG 50mg q.d.3.623.544.85
EFV 600 mg q.d. (Outside THA)3.875.134.41
FPV/RTV 700/100mg b.i.d.5.615.126.75
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)3.893.625.37
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA5.15.0
TFV 300mg q.d.0.2500.2450.298
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.1.22.54.1
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.2.733.565.43

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.5.445.10

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. Half-life is defined as 0.693/k, where k, the elimination rate constant, is the slope of the decline in concentrations. (NCT00042289)
Timeframe: Infant plasma samples at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

Interventionhour (Median)
DTG 50mg q.d.32.8
EVG/COBI 150/150mg q.d.7.6
DRV/COBI 800/150 mg q.d.NA
EFV 600 mg q.d. (Outside THA)65.6

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.0.15
DTG 50mg q.d.1.25
EVG/COBI 150/150mg q.d.0.91
DRV/COBI 800/150 mg q.d.0.07
ATV/COBI 300/150 mg q.d.0.07
TFV 300mg q.d.0.88

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. For arms with zero overall participants analyzed, samples were below the limit of quantification and ratios could not be calculated. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
TAF 10mg q.d. w/COBI0.97
EFV 600 mg q.d. (Outside THA)0.67
EFV 600mg q.d.0.49
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.0.2
RAL 400mg b.i.d.1.5
ETR 200mg b.i.d.0.52
MVC 150 or 300mg b.i.d.0.33
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.14
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.16
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.0.19
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.12
RPV 25mg q.d.0.55
ATV/RTV 300/100mg q.d. or TFV/ATV/RTV 300/300/100mg q.d.0.18
DRV/RTV 800/100mg q.d. or DRV/RTV 600/100mg b.i.d.0.18

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PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

"Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose.~For the TAF 25 mg q.d., 10 mg q.d. w/COBI, and 25 mg q.d. w/COBI or RTV boosting arms, samples were all below the limit of quantification and statistical analyses were not conducted." (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.0.210.210.61
ATV/RTV Arm 1: 300/100mg q.d.2.00.71.2
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.490.710.90
DRV/COBI 800/150 mg q.d.0.330.271.43
DRV/RTV 800/100mg q.d.0.991.172.78
DTG 50mg q.d.0.730.931.28
EFV 600 mg q.d. (Outside THA)1.491.481.94
EVG/COBI 150/150mg q.d.0.02580.04870.3771
TAF 10mg q.d. w/COBI0.001950.001950.00195
TAF 25mg q.d.0.001950.001950.00195
TAF 25mg q.d. w/COBI or RTV Boosting0.001950.001950.00195
TFV 300mg q.d.0.0390.0540.061
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.0.30.50.8
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.440.571.26

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Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12h (area-under-the-curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8 and 12 hours post dosing.

Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG115.97100.20

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Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8, 12, and 24 hours post dosing.

,
Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
ATV/RTV/TFV 300/100/300mg q.d. With ENG53.9655.25
EFV 600mg q.d. With ENG53.6456.65

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,
InterventionParticipants (Count of Participants)
3rd TrimesterPostpartum
EFV 600mg q.d.2021
MVC 150 or 300mg b.i.d.87

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,,,,,,,,,,,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
2nd Trimester3rd TrimesterPostpartum
ATV/RTV Arm 1: 300/100mg q.d.11212
DRV/COBI 800/150 mg q.d.3414
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.71622
DRV/RTV 600/100mg b.i.d.71922
DRV/RTV 800/100mg q.d.91922
DTG 50mg q.d.92023
EFV 600 mg q.d. (Outside THA)123334
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.82927
ETR 200mg b.i.d.5137
EVG/COBI 150/150mg q.d.81018
FPV/RTV 700/100mg b.i.d.82622
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)101926
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.93027
ATV/COBI 300/150 mg q.d.125
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA1514
RAL 400mg b.i.d.113330
RPV 25mg q.d.142625
TAF 10mg q.d. w/COBI152322
TAF 25mg q.d.132324
TAF 25mg q.d. w/COBI or RTV Boosting102418
TFV 300mg q.d.22727
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.11112
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.72332

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. (NCT00042289)
Timeframe: Blood samples were collected at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

,,,
Interventionmcg/mL (Median)
2-10 hours after birth18-28 hours after birth36-72 hours after birth5-9 days after birth
DRV/COBI 800/150 mg q.d.0.351.431.871.72
DTG 50mg q.d.1.731.531.000.06
EFV 600 mg q.d. (Outside THA)1.11.00.90.4
EVG/COBI 150/150mg q.d.0.1320.0320.0050.005

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

Interventionng*hour/mL (Geometric Mean)
2nd Trimester3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.NA27173645

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.55.151.879.6
DRV/RTV 600/100mg b.i.d.45.845.961.7
FPV/RTV 700/100mg b.i.d.43.5032.1551.60
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA34.233.5

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.4.58.35.3
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)14.916.127.1
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.7296133
RAL 400mg b.i.d.6.65.411.6

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24 (area under the curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

,,,,,,,,,,,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.25.3318.8536.20
ATV/RTV Arm 1: 300/100mg q.d.88.241.957.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.30.645.748.8
DRV/COBI 800/150 mg q.d.50.0042.0595.55
DRV/RTV 800/100mg q.d.64.663.5103.9
DTG 50mg q.d.47.649.265.0
EFV 600 mg q.d. (Outside THA)47.3060.0262.70
EVG/COBI 150/150mg q.d.15.314.021.0
TAF 10mg q.d. w/COBI0.1970.2060.216
TAF 25mg q.d.0.1710.2120.271
TAF 25mg q.d. w/COBI or RTV Boosting0.1810.2570.283
TFV 300mg q.d.1.92.43.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.14.528.839.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.26.237.758.7

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.55.458.3

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.0.0630.0560.081

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Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-TB Treatment - Per-protocol

Patients who presented with TB after completion of study phase treatment but before the end of follow-up were classified as relapses. A bacteriologic relapse was defined as a patient who became consistently culture-positive [defined as at least 1 of the following]: (a) at least 1 sputum mycobacterial culture growing at least 10 colonies of MTB on solid medium; (b) 2 or more respiratory secretion cultures that are positive for MTB in liquid media; or (c) any culture from an extrapulmonary site that is positive for MTB during follow-up after successful completion of initial anti-TB treatment. (NCT00130247)
Timeframe: 30 months

InterventionParticipants (Number)
4-Month Arm13
6-Month Arm3

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Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-tuberculosis (TB) Treatment - Intention-to-treat

Patients who presented with TB after completion of study phase treatment but before the end of follow-up were classified as relapses. A bacteriologic relapse was defined as a patient who became consistently culture-positive [defined as at least 1 of the following]: (a) at least 1 sputum mycobacterial culture growing at least 10 colonies of MTB on solid medium; (b) 2 or more respiratory secretion cultures that are positive for MTB in liquid media; or (c) any culture from an extrapulmonary site that is positive for MTB during follow-up after successful completion of initial anti-TB treatment. (NCT00130247)
Timeframe: 30 months

InterventionParticipants (Number)
4-Month Arm13
6-Month Arm3

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Relapses at 1 and 2 Years

(NCT00130247)
Timeframe: 1 and 2 years after successful completion of initial anti-TB treatment

,
InterventionParticipants (Number)
Relapses at 1 yearRelapses at 2 years
4-Month Arm1013
6-Month Arm33

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Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Intention to Treat

A culture-positive treatment failure was defined as initial culture conversion but subsequent reversion to culture positivity. A clinical treatment failure was defined as a patient with clinical and/or radiographic evidence of progressive tuberculosis not confirmed by a positive culture after 4 or more months of anti-TB treatment while still receiving treatment. Patients who defaulted before completing study treatment and returned later with culture-positive tuberculosis were termed failures after non-adherence. (NCT00130247)
Timeframe: 2 years

,
InterventionParticipants (Number)
Treatment FailuresRelapses
4-Month Arm013
6-Month Arm03

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Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Per Protocol

A culture-positive treatment failure was defined as initial culture conversion but subsequent reversion to culture positivity. A clinical treatment failure was defined as a patient with clinical and/or radiographic evidence of progressive tuberculosis not confirmed by a positive culture after 4 or more months of anti-TB treatment while still receiving treatment. Patients who defaulted before completing study treatment and returned later with culture-positive tuberculosis were termed failures after non-adherence. (NCT00130247)
Timeframe: 2 years

,
InterventionParticipants (Number)
Treatment FailuresRelapses
4-Month Arm013
6-Month Arm03

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Acquired Drug Resistance in Patients Who Relapsed

(NCT00130247)
Timeframe: 2 years

InterventionParticipants (Number)
4-Month Arm0
6-Month Arm0

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To Compare, by Treatment Group, the Percentage of Patients With a Negative Sputum Culture at the End of Intensive Phase Therapy.

LJ culture conversion (NCT00728507)
Timeframe: Week 8

Interventionpercentage of participants (Number)
HPZM78.3
HRZE84.3

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Combined Failure of Bacteriological Cure and Relapse as Defined by Culture Using Liquid Media (Mycobacteria Growth Indicator Tube-MGIT).

The secondary analysis of efficacy outcome was the proportion of patients who had bacteriologically or clinically defined failure or relapse within 18 months after randomization (a composite unfavorable outcome) based on MGIT. Culture-negative status was defined as two negative-culture results at different visits without an intervening positive result. The date of culture-negative status was defined as the date of the first negative-culture result. This status continued until there were two positive cultures, without an intervening negative culture, or until there was a single positive culture that was not followed by two negative cultures. Relapse strains were those shown to be identical on 24-locus Mycobacterial interspersed repetitive units (MIRU) analysis. (NCT00864383)
Timeframe: 18 months (within one year of completion of therapy)

Interventionparticipants with failure or relapse (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)65
Regimen 2 - 2MHRZ/2MHR98
Regimen 3 - 2EMRZ/2MR131

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Combined Failure of Bacteriological Cure and Relapse Within One Year of Completion of Therapy as Defined by Culture Using Solid Media (Lowenstein-Jensen - LJ).

The primary efficacy outcome was the proportion of patients who had bacteriologically or clinically defined failure or relapse within 18 months after randomization (a composite unfavorable outcome). Culture-negative status was defined as two negative-culture results at different visits without an intervening positive result. The date of culture-negative status was defined as the date of the first negative-culture result. This status continued until there were two positive cultures, without an intervening negative culture, or until there was a single positive culture that was not followed by two negative cultures. Relapse strains were those shown to be identical on 24-locus Mycobacterial interspersed repetitive units (MIRU) analysis. For the final 18 month study visit when both L-J samples were contaminated or missing, if the subject could not be brought back, liquid medium culture results were used in place of solid medium culture results. (NCT00864383)
Timeframe: 18 months (within one year of completion of therapy)

Interventionparticipants with failure or relapse (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)43
Regimen 2 - 2MHRZ/2MHR78
Regimen 3 - 2EMRZ/2MR105

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Number of Patients Who Are Culture Negative (Liquid MGIT Culture)

Number of patients who are TB MGIT culture negative at 8 weeks. (NCT00864383)
Timeframe: 8 weeks

Interventionparticipants who are culture negative (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)235
Regimen 2 - 2MHRZ/2MHR274
Regimen 3 - 2EMRZ/2MR260

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Number of Patients Who Are Culture Negative (Solid LJ Culture)

Number of patients who are TB LJ culture negative at 8 weeks. (NCT00864383)
Timeframe: 8 weeks

Interventionparticipants who are culture negative (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)352
Regimen 2 - 2MHRZ/2MHR394
Regimen 3 - 2EMRZ/2MR401

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Number of Patients With Grade 3 or 4 Adverse Events (Using a Modified Division of Acquired Immunodeficiency Syndrome National Institute of Allergy and Infectious Diseases [DAIDS] Scale of Adverse Event Reporting)

The number of participants includes all patients who had at least one grade 3 or 4 adverse event. (NCT00864383)
Timeframe: 18 months (within one year of completion of therapy)

Interventionparticipants with Grade 3 or 4 AEs (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)123
Regimen 2 - 2MHRZ/2MHR127
Regimen 3 - 2EMRZ/2MR111

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Sensitivity Analyses Assuming All Losses to Follow-up and Non-tuberculous Deaths Have a Favourable Outcome Using Solid (L-J) Media.

"Sensitivity Analysis of Primary Efficacy Results of All Randomized Subjects Imputing Favorable for Missing Outcomes. Analysis is the number of subjects with an unfavorable outcome. Favorable outcome is defined as the number of subjects with a negative TB culture status at 18 months (at or after 72 weeks), who had not already been classified as having an unfavorable outcome, and whose last positive TB culture result (isolated positive culture) was followed by at least two negative culture results." (NCT00864383)
Timeframe: 18 months

Interventionparticipants with unfavorable outcome (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)87
Regimen 2 - 2MHRZ/2MHR132
Regimen 3 - 2EMRZ/2MR132

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Sensitivity Analysis Assuming All Losses to Follow-up and Non-tuberculous Deaths Have an Unfavorable Outcome Using Solid (L-J) Media.

"Sensitivity Analysis of Primary Efficacy Results of All Randomized Subjects Imputing Unfavorable for Missing Outcomes. Analysis is the number of subjects with an unfavorable outcome. Favorable outcome is defined as the number of subjects with a negative TB culture status at 18 months (at or after 72 weeks), who had not already been classified as having an unfavorable outcome, and whose last positive TB culture result (isolated positive culture) was followed by at least two negative culture results." (NCT00864383)
Timeframe: 18 months

Interventionparticipants with unfavorable outcome (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)172
Regimen 2 - 2MHRZ/2MHR219
Regimen 3 - 2EMRZ/2MR217

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Time to First Culture Negative Sputum Sample (LJ Solid Media)

Culture negative for TB using LJ cultures. (NCT00864383)
Timeframe: 18 months

InterventionTime to culture negative status / weeks (Median)
Regimen 1 - 2EHRZ/4HR (Control Regimen)6.0
Regimen 2 - 2MHRZ/2MHR6.0
Regimen 3 - 2EMRZ/2MR6.0

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Time to First Culture Negative Sputum Sample (MGIT Liquid Media)

(NCT00864383)
Timeframe: 18 months

InterventionTime to culture negative status / weeks (Median)
Regimen 1 - 2EHRZ/4HR (Control Regimen)11.9
Regimen 2 - 2MHRZ/2MHR8.0
Regimen 3 - 2EMRZ/2MR8.0

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Total Clearance of Ethambutol

(NCT01048697)
Timeframe: Blood samples will be collected over a 24 hour period (0, 2, 6, 11, 18, and 24 hours)

InterventionL/h (Mean)
Ethambutol80.8

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Change in Lesion Size at the Completion of Antibiotic Therapy, Measured on a Continuous Scale; Change Will be Determined by Change in Diameter of the Lesions

(NCT01074554)
Timeframe: Baseline to 8 weeks

Interventionmm (Median)
Antibiotic Regimen-8.4
Placebo Regimen0.07

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Change in Modified Sarcoidosis Activity and Severity Index (SASI) at Completion of Therapy.

Characterization of lesion severity was conducted using Modified Sarcoidosis Activity and Severity Index (SASI), measuring erythema, induration and desquamation. The modification was that the same scale was applied to any part of the body, instead of the face alone. The scale range is 0 (no problem) to 72 (very severe). (NCT01074554)
Timeframe: Baseline to 8 weeks

Interventionunits on a scale (Mean)
Antibiotic Regimen-2.9
Placebo Regimen-0.6

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Granuloma Burden

Number of patients with a decrease in Granuloma Burden (only in those patients having granulomas present at baseline biopsy) (NCT01074554)
Timeframe: Baseline to 8 weeks

Interventionparticipants (Number)
Antibiotic Regimen7
Placebo Regimen0

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Change in Absolute FVC From Baseline to Post Completion of 8 Weeks of Antibiotic Therapy.

The primary endpoint was improvement in absolute FVC from baseline to completion of therapy. Spirometry testing was performed using a standardized calibrated laptop spirometer, Flowscreen II USA Spirometer (VIASYS Healthcare Inc., Yorba Linda, CA). The volume accuracy of the spirometer was checked daily using a three liter calibration syringe. Each subject was given at least three attempts and the greatest measurement for absolute FVC and Forced Expiratory Volume (FEV1) at baseline, four week, and eight week assessments was recorded. (NCT01169038)
Timeframe: 8 weeks

Interventionliters (Mean)
Antibiotics2.61

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Proportion of Participants With Reportable Hospitalization by Week 48

Proportion of participants with reportable hospitalization reported by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.10
Arm B: IPT0.12

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Proportion of Participants With HIV-1 RNA Level <400 Copies/mL

Proportion of participants with HIV-1 RNA level <400 copies/mL. (NCT01380080)
Timeframe: At weeks 0, 4, 24, and 48

,
InterventionProportion of participants (Number)
Week 0Week 4Week 24Week 48
Arm A: Empiric00.460.840.87
Arm B: IPT0.010.490.850.89

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CD4+ T-cell Count Change From Baseline

Change was calculated as the CD4+ T-cell count at the later weeks (4, 24 and 48) minus the baseline (week 0) CD4+ T-cell count. (NCT01380080)
Timeframe: Weeks 0, 4, 24 and 48

,
Interventioncells/ mm^3 (Median)
Week 4Week 24Week 48
Arm A: Empiric4996158
Arm B: IPT54102146

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CD4+ T-cell Count

The absolute levels of CD4+ T-cell counts (cells/mm^3) (NCT01380080)
Timeframe: At weeks 0, 4, 24, and 48

,
Interventioncells/ mm^3 (Median)
Week 0Week 4Week 24Week 48
Arm A: Empiric1874121176
Arm B: IPT1976121172

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Time to Initiation of TB Treatment by Week 96

Median time to TB treatment initiation since study entry (NCT01380080)
Timeframe: From study entry to week 96

InterventionDays (Median)
Arm A: Empiric0
Arm B: IPT0

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Proportion of Participants With TB Diagnosis by Week 96

Proportion of participants with TB diagnosis per current ACTG Diagnosis Appendix 60 by week 96 (NCT01380080)
Timeframe: From study entry to week 96

InterventionProportion of participants (Number)
Arm A: Empiric0.08
Arm B: IPT0.05

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Proportion of Participants With Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48

Proportion of participants with IRIS (using current ACTG definition Appendix 60, see References) by Week 48. IRIS in participants with TB and other opportunistic infections may occur shortly after the initiation of potent combination ART, particularly in participants with advanced HIV disease. (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.04
Arm B: IPT0.05

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Cumulative Probability of Death by Week 24

The Kaplan-Meier estimate of cumulative probability of death by week 24 (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric4.8
Arm B: IPT5.2

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Cumulative Probability of Death or AIDS Progression by Week 24

The Kaplan-Meier estimate of the cumulative probability of death or AIDS progression by week 24. AIDS progression was defined as new WHO stage 3 or 4 conditions occurred after study entry. (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric17.1
Arm B: IPT12.5

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Cumulative Probability of Death or AIDS Progression by Week 48

The Kaplan-Meier estimate of the cumulative probability of death or AIDS progression by week 48. AIDS progression was defined as new WHO stage 3 or 4 conditions occurred after study entry. (NCT01380080)
Timeframe: From study entry to week 48

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric19.3
Arm B: IPT15.3

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Cumulative Probability of Death or Unknown Vital Status by Week 24

"The Kaplan-Meier estimate of the cumulative probability of death or unknown vital status by week 24.~The vital status was considered unknown at week 24 if a participant prematurely discontinued from the study before week 24 and no vital status was obtained at week 48." (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric5.2
Arm B: IPT5.2

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Cumulative Probability of First AIDS Progression by Week 96

The Kaplan-Meier estimate of the cumulative probability of first AIDS progression which was defined as the identification of a new World Health Organization (WHO) stage 3 or 4 condition (NCT01380080)
Timeframe: From study entry to week 96

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric16.6
Arm B: IPT11.3

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Proportion of Participants Who Prematurely Discontinued Antiretroviral Therapy by Week 48

Proportion of participants with premature discontinuation of antiretroviral therapy (ART) by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.19
Arm B: IPT0.21

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Proportion of Participants Who Prematurely Discontinued Any Component of TB Treatment by Week 48

Proportion of participants with premature discontinuation of any component of TB treatment by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.13
Arm B: IPT0.05

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Proportion of Participants With at Least One New Grade 3 or 4 Adverse Event That is at Least a One-grade Increase From Baseline by Week 48

Proportion of participants with at least one new Grade 3 or 4 laboratory or sign or symptom that is at least a one-grade increase from baseline by Week 48. Grade 3=Severe, Grade 4=Life-Threatening according to DAIDS AE Grading Table (see references). (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.32
Arm B: IPT0.30

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Proportion of Participants With at Least One New Grade 3 or 4 Targeted Laboratory Value That is at Least a One-grade Increase From Baseline by Week 48

"Proportion of participants with at least one new Grade 3 or 4 that is at least a one-grade increase from baseline for the following targeted laboratory values by Week 48~The targeted laboratory events include hemoglobin, serum creatinine, ALT and AST" (NCT01380080)
Timeframe: From study entry to week 48. The lab events were collected at study entry, weeks 2, 4, 8, 12, 16, 20, 24, and 48.

InterventionProportion of participants (Number)
Arm A: Empiric0.11
Arm B: IPT0.13

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Isoniazid PK Parameter CL/F at Day 14

Isoniazid PK parameter CL/F obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

InterventionL/hour (Median)
RHZE-RHZE30.6

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Isoniazid PK Parameter CLast at Day 1

Isoniazid (INH) PK parameter CLast obtained Day 1. The lower limit of quantification of the assay (LLOQ) for INH was 100 ng/mL. The results below the lower limit of quantification were assigned as one-half the value of the LLOQ, which was 50 ng/mL. (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

Interventionng/mL (Median)
RHZE-RHZE50
RHZE-RZE50
RHZE-RMZE50

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Isoniazid PK Parameter CLast at Day 14

Isoniazid (INH) PK parameter CLast obtained Day 14. The lower limit of quantification of the assay (LLOQ) for INH was 100 ng/mL. The results below the lower limit of quantification were assigned as one-half the value of the LLOQ, which was 50 ng/mL. (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

Interventionng/mL (Median)
RHZE-RHZE50

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Isoniazid PK Parameter Cmax at Day 1

Isoniazid PK parameter Cmax obtained Day 1 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

Interventionng/mL (Median)
RHZE-RHZE3165
RHZE-RZE2920
RHZE-RMZE2760

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Isoniazid PK Parameter Cmax at Day 14

Isoniazid PK parameter Cmax obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

Interventionng/mL (Median)
RHZE-RHZE3130

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Moxifloxacin PK Parameter CL/F at Day 14

Moxifloxacin PK parameter CL/F obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

InterventionL/hour (Median)
RHZE-RMZE17.8

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Moxifloxacin PK Parameter CLast at Day 14

Moxifloxacin PK parameter CLast obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

Interventionng/mL (Median)
RHZE-RMZE178

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Moxifloxacin PK Parameter Cmax at Day 14

Moxifloxacin PK parameter Cmax obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

Interventionng/mL (Median)
RHZE-RMZE3010

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AUC0-24hour for Ethambutol (EMB)

PK AUCs of Ethambutol (EMB) from 0 to 24 hours obtained at Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
Interventionh*ng/mL (Median)
EMB AUC0-24hour at Day 1EMB AUC0-24hour at Day 14
RHZE-RHZE11918.816414.9
RHZE-RMZE11322.415181.2
RHZE-RZE11145.816675.9
RZE-RZE10716.816574.6

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AUC0-24hour for Pyrazinamide (PZA)

PK AUCs of Pyrazinamide (PZA) from 0 to 24 hours obtained at Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
Interventionh*ng/mL (Median)
PZA AUC0-24hour at Day 1PZA AUC0-24hour at Day 14
RHZE-RHZE301214.5249879.1
RHZE-RMZE292078.2280071.0
RHZE-RZE255283.0201389.7
RZE-RZE272853.9252276.8

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Ethambutol PK Parameter CLast

Ethambutol PK parameter CLast obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
EMB CLast at Day 1EMB CLast at Day 14
RHZE-RHZE86.5205.0
RHZE-RMZE40164
RHZE-RZE85176
RZE-RZE86159

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Ethambutol PK Parameter Cmax

Ethambutol PK parameter Cmax obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
EMB Cmax at Day 1EMB Cmax at Day 14
RHZE-RHZE26502980
RHZE-RMZE24702780
RHZE-RZE20403090
RZE-RZE22202920

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Log10 Transformed Colony-forming Unit (CFU) Count Per mL From Sputum Samples at Baseline and Day 14

The log10 CFU count per mL from sputum samples processed by standard method or decontaminated method. (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 14

,
Interventionlog10 CFU/ mL (Median)
Pre-entryDay 0Day 14
Decontaminated Processing Method5.895.583.74
Standard Processing Method5.805.684.01

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Pharmacokinetic Parameter (PK) Area Under the Concentration-time Curve (AUC0-24hour) for Rifampicin (RIF)

Pharmacokinetic Parameter Area Under the Concentration-time Curve (AUCs) of Rifampicin from 0 to 24 hours obtained at Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
Interventionh*ng/mL (Median)
RIF AUC0-24hour at Day 1RIF AUC0-24hour at Day 14
RHZE-RHZE37358.831361.4
RHZE-RMZE51434.126751.2
RHZE-RZE42062.627161.7
RZE-RZE39294.030521.0

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Pyrazinamide PK Parameter CL/F

Pyrazinamide PK parameter CL/F obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
InterventionL/hour (Median)
PZA CL/F Day 1PZA CL/F Day 14
RHZE-RHZE4.14.5
RHZE-RMZE4.74.7
RHZE-RZE4.85.4
RZE-RZE4.24.7

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Pyrazinamide PK Parameter CLast

Pyrazinamide PK parameter CLast obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
PZA CLast at Day 1PZA CLast at Day 14
RHZE-RHZE33701955.0
RHZE-RMZE31301790
RHZE-RZE28501280
RZE-RZE27101770

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Pyrazinamide PK Parameter Cmax

Pyrazinamide PK parameter Cmax obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
PZA Cmax at Day 1PZA Cmax at Day 14
RHZE-RHZE2765029300
RHZE-RMZE2880029300
RHZE-RZE2700027000
RZE-RZE2580028000

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Rifampicin PK Parameter Clearance (CL/F)

Rifampicin PK parameter Clearance (CL/F) obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
InterventionL/hour (Median)
RIF CL/F Day 1RIF CL/F Day 14
RHZE-RHZE14.018.0
RHZE-RMZE10.521.5
RHZE-RZE12.522.1
RZE-RZE14.317.0

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Rifampicin PK Parameter Last Concentration (CLast)

Rifampicin (RIF) PK parameter Last Concentration (CLast) obtained Day 1 and Day 14. The lower limit of quantification of the assay (LLOQ) for RIF was 40 ng/mL. The results below the lower limit of quantification were assigned as one-half the value of the LLOQ, which was 20 ng/mL. (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
RIF CLast at Day 1RIF CLast at Day 14
RHZE-RHZE74.520
RHZE-RMZE13320
RHZE-RZE2020
RZE-RZE2020

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Rifampicin PK Parameter Maximum Plasma Concentration (Cmax)

Rifampicin PK parameter Parameter Maximum Plasma Concentration (Cmax) obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
RIF Cmax at Day 1RIF Cmax at Day 14
RHZE-RHZE55657145
RHZE-RMZE86607370
RHZE-RZE60606960
RZE-RZE48808350

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Ethambutol PK Parameter CL/F

Ethambutol PK parameter CL/F obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
InterventionL/hour (Median)
EMB CL/F Day 1EMB CL/F Day 14
RHZE-RHZE93.657.9
RHZE-RMZE83.856.8
RHZE-RZE85.463.5
RZE-RZE76.560.1

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AUC0-24hour for Isoniazid (INH) at Day 1

PK AUCs of Isoniazid (INH) from 0 to 24 hours obtained at Day 1 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

Interventionh*ng/mL (Median)
RHZE-RHZE10725.8
RHZE-RZE7970.6
RHZE-RMZE7165.1

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AUC0-24hour for Isoniazid at Day 14

PK AUCs of Isoniazid from 0 to 24 hours obtained at Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

Interventionh*ng/mL (Median)
RHZE-RHZE9797.2

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AUC0-24hour for Moxifloxacin (Mox) at Day 14

PK AUCs of Moxiflozacin (Mox) from 0 to 24 hours obtained at Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

Interventionh*ng/mL (Median)
RHZE-RMZE22498.4

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Correlation Between Time to Positivity (TTP) and log10 Transformed Colony-forming Unit (CFU) Counts Per mL

Pearson correlation coefficient was used to examine the correlation between TTP and log10 CFU among all qualified samples obtained on study (NCT01589497)
Timeframe: Pre-entry, Day 0, Day 1, Day 2, Day 3, Day 5, Day 7, Day 9, Day 11 and Day 14

Interventioncorrelation coefficient (Number)
Overall-0.75

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Daily Change in log10 Colony-forming Unit (CFU) Counts Per mL Sputum From Day 2 to Day 14

"The daily change in log10 CFU/mL sputum was calculated as follows:~EBA2-14(CFU) = (log10 CFU/mL at day 2 - log10 CFU/mL at day 14)/12.~For a CFU/mL count of 0, the log10 CFU/mL was set to 0." (NCT01589497)
Timeframe: Day 2 and day 14

Interventionlog10 CFU/ mL (Median)
RHZE-RHZE0.143
RHZE-RZE0.093
RHZE-RMZE0.123
RZE-RZE0.104

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Daily Change in log10 Transformed Colony-forming Unit (CFU) Counts Per mL Sputum From Baseline (Study Treatment Initiation) to Day 2

"The daily change in log10 CFU/mL sputum was calculated as follows:~EBA0-2(CFU) = (baseline log10 CFU/mL sputum (mean of log10 CFU/mL at pre-entry and day 0) - log10 CFU/mL at day 2)/2.~For a CFU/mL count of 0, the log10 CFU/mL was set to 0." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 2

Interventionlog10 CFU/ mL (Median)
RHZE-RHZE0.255
RHZE-RZE0.385
RHZE-RMZE0.111
RZE-RZE0.034

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Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 14

"The daily change in TTP was calculated as follows:~EBA0-14(TTP) = [baseline TTP (mean of TTP at pre-entry and day 0) - TTP at day 14]/14." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 14

Interventionhours (Median)
RHZE-RHZE-12
RHZE-RZE-12
RHZE-RMZE-13
RZE-RZE-11

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Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 2

"The daily change in TTP was calculated as follows:~EBA0-2(TTP) = (baseline TTP (mean of TTP at pre-entry and day 0) - TTP at day 2)/2." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 2

Interventionhours (Median)
RHZE-RHZE-31
RHZE-RZE-30
RHZE-RMZE-29
RZE-RZE-25

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Daily Change in Time to Positivity (TTP) From Day 2 to Day 14

"The daily change in TTP was calculated as follows:~EBA2-14(TTP) = (TTP at day 2 - TTP at day 14)/12." (NCT01589497)
Timeframe: Day 2 and Day 14

Interventionhours (Median)
RHZE-RHZE-9
RHZE-RZE-9
RHZE-RMZE-12
RZE-RZE-9

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Daily Decrease in log10 Transformed Colony-forming Unit (CFU) Counts Per ml Sputum From Baseline (Study Treatment Initiation) to Day 14

"The daily decrease was calculated as follows:~EBA0-14(CFU)= [baseline log10 CFU/mL sputum (mean of log10 CFU/mL at pre-entry and day 0) - log10 CFU/mL at day 14]/14. For a CFU/ml count of 0, the log10 CFU/mL was set to 0.~No formal statistical testing was conducted to compare the arms. Please refer to the explanation in the Protocol Section." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 14

Interventionlog10 CFU/ mL (Median)
RHZE-RHZE0.134
RHZE-RZE0.096
RHZE-RMZE0.136
RZE-RZE0.119

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Isoniazid PK Parameter CL/F at Day 1

Isoniazid PK parameter CL/F obtained Day 1 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

InterventionL/hour (Median)
RHZE-RHZE28.0
RHZE-RZE37.6
RHZE-RMZE41.9

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RBT Cmax and Cmin in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT461161
C: Standard-Dose LPV/r + RAL w/RBT349115

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RAL AUC in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
C: Standard-Dose LPV/r + RAL w/RBT11338

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Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48

The percent of participants whose HIV viral load was less than 50 copies/mL at week 48 was calculated with an associated standard error. Participants who were lost-to-follow-up or dead by week 48 or had missing RNA at week 48 were coded as having HIV viral load greater than 50 copies/mL. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT45.8
B: Double-dose LPV/r w/RIF54.2
C: Standard-Dose LPV/r + RAL w/RBT56.5

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Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.

The percent of participants whose HIV viral load was less than 400 copies/mL at week 48 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. Participants who were lost-to-follow-up or dead by week 48 or had missing results at week 48 were coded as having HIV viral load greater than 400 copies/mL. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT58.3
B: Double-dose LPV/r w/RIF66.7
C: Standard-Dose LPV/r + RAL w/RBT60.9

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Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one TB drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through to the discontinuation of the last TB drug

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT13.0

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Percent of Participants Who Experienced TB Treatment Failure

TB treatment failure was defined as having a MTB-positive culture after 16 weeks of TB treatment for a participant who was documented to be taking TB medications. The percent of participants who experienced TB treatment failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After 16 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF0.0
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one HIV drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF16.7
C: Standard-Dose LPV/r + RAL w/RBT21.7

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Percent of Participants Who Experienced HIV Virologic Failure

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. Participants who were missing data due to being lost-to-follow-up or dead were coded as virologic failures. The percent of participants who experienced HIV virologic failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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Percent of Participants Who Experienced a New AIDS-defining Illness or Died

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness or died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The drug resistance was determined based on phenotypic methods. The percent of participants who experienced TB relapse/recurrence and who had TB drug resistance was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionparticipants (Number)
B: Double-dose LPV/r w/RIF0
C: Standard-Dose LPV/r + RAL w/RBT0

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Percent of Participants Who Experienced TB Relapse/Recurrence

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The percent of participants who experienced TB relapse/recurrence was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT4.3

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LPV AUC in Participants Enrolled in Arms A, B, and C

Describe LPV plasma PK characteristics (area under the curve [AUC] between 0 and 12 hours) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT159796
B: Double-dose LPV/r w/RIF161772
C: Standard-Dose LPV/r + RAL w/RBT149247

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Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) laboratory abnormality were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT6
B: Double-dose LPV/r w/RIF3
C: Standard-Dose LPV/r + RAL w/RBT5

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Number of Participants Reporting a Grade 3 or 4 Sign or Symptom

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) sign or symptom were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF5
C: Standard-Dose LPV/r + RAL w/RBT5

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Number of Participants Who Experienced MTB IRIS

The number of participants who experienced MTB immune reconstitution inflammatory syndrome (IRIS) was summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT1
B: Double-dose LPV/r w/RIF2
C: Standard-Dose LPV/r + RAL w/RBT3

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Percent of Participants Who Died

The percent of participants who died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF4.7
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced Sputum Conversion at Week 8.

Sputum conversion was defined as culture MTB-negative at week 8 or AFB smear negative at week 8 (and culture contaminated or missing at week 8); there were no Xpert MTB/RIF results at week 8. The percent of participants experienced sputum conversion at week 8 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 8 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT87.5
B: Double-dose LPV/r w/RIF81.8
C: Standard-Dose LPV/r + RAL w/RBT70.0

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Percent of Participants Who Experienced a New AIDS-defining Illness

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT0.0

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CD4 Count Change From Baseline to Week 8

The difference in CD4 count from baseline to week 8 was calculated as the CD4 count at week 8 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 8 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF26
C: Standard-Dose LPV/r + RAL w/RBT37

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Cumulative Probability of HIV Virologic Failure at Week 72

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. The percent of participants with HIV virologic failure at week 72 was calculated using a Kaplan-Meier estimator with an associated standard error. The confidence interval was calculated using a log-log transformation. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventioncumulative events per 100 participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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CD4 Count Change From Baseline to Week 24

The difference in CD4 count from baseline to week 24 was calculated as the CD4 count at week 24 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 24 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT20
B: Double-dose LPV/r w/RIF56
C: Standard-Dose LPV/r + RAL w/RBT13

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CD4 Count Change From Baseline to Week 48

The difference in CD4 count from baseline to week 48 was calculated as the CD4 count at week 48 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 48 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT99
B: Double-dose LPV/r w/RIF119
C: Standard-Dose LPV/r + RAL w/RBT74

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CD4 Count Change From Baseline to Week 72

The difference in CD4 count from baseline to week 72 was calculated as the CD4 count at week 72 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 72 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT126
B: Double-dose LPV/r w/RIF212
C: Standard-Dose LPV/r + RAL w/RBT54

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RBT AUC in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT7374
C: Standard-Dose LPV/r + RAL w/RBT5516

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LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C

Describe LPV plasma pharmacokinetic (PK) characteristics (maximum concentration [Cmax] and minimum concentration [Cmin]) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

,,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT185319920
B: Double-dose LPV/r w/RIF181388033
C: Standard-Dose LPV/r + RAL w/RBT168028548

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RAL Cmax and Cmin in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
C: Standard-Dose LPV/r + RAL w/RBT2830166

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Frequency of Adverse Events

All Adverse Events (AE), and AEs considered to be drug-related will coded using standard AE dictionaries. (NCT01785186)
Timeframe: 0 - 12 weeks

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Interventionparticipants (Number)
Number of Patients with at least 1 AENumber of patients with at least 1 SAE
Arm 1 (R35)534
HR20ZM494
HR20ZQ425
HRZE926
HRZQ494

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Sputum Culture Conversion (2 Negative Cultures) Using Liquid Media

From enrollment, the time to stable culture conversion (2 consecutive negative weekly cultures) in liquid media. (NCT01785186)
Timeframe: 0 - 12 weeks

Interventiondays (Median)
Arm 1 (R35)48
HRZQ63
HR20ZQ66
HR20ZM55
HRZE62

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Pharmacokinetics Including AUC, Cl, t1/2, Vd, and Protein Binding

"Pharmacokinetic parameters will be assessed for rifampicin, moxifloxacin and SQ109:~area under the plasma concentration curve from dosing to the end of the dosing interval (AUC 0-24) (in h*ng/mL)~the observed maximum concentration (Cmax( (in ng/mL)~time to reach Cmax (Tmax)(in hours)~the minimum observed plasma concentration 24 hours following the last dose (Cmin) (in hours),~clearance (Cl) (in mL/minute),~volume of distribution (Vd) (in L),~elimination half-life (T1/2,) (in hours)~free (protein-unbound) fraction (for rifampicin only) (in percent)." (NCT01785186)
Timeframe: 0 - 12 weeks

InterventionRifampicin AUC(mg*h/l) (Geometric Mean)
HRZQ17.4
Arm 1 (R35)170
HR20ZQ68.3
HR20ZM57.8
HRZE24.2

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Adverse Events

Safety profile of regimen as evidenced by the number of adverse events (NCT02024555)
Timeframe: 24 weeks

,
Interventionnumber of events (Number)
Serious Adverse EventsNon-Serious Adverse Events
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin424
Placebo316

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Abnormal Lab Values

Safety profile of regimen as evidenced by the number of abnormal lab values classified as Adverse Events (NCT02024555)
Timeframe: baseline to 16 weeks

,
Interventionparticipants (Number)
low platelet countlow WBC countelevated glucoselow glucose
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin1531
Placebo0021

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Failure of Standard Therapy

We will assess how many subjects in either arm need escalation of their standard regimen (ie increase in prednisone) during the 16 weeks. (NCT02024555)
Timeframe: Baseline to 16 weeks

InterventionParticipants (Count of Participants)
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin3
Placebo2

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Change in the Saint George's Respiratory Questionnaire (SGRQ)

"The SGRQ is a 50-item questionnaire developed to measure health status (quality of life) in patients with diseases of airways obstruction.~Scores range from 0 to 100, with higher scores indicating more limitations.~A minimum change in score of 4 units was established as clinically relevant after patient and clinician testing." (NCT02024555)
Timeframe: Baseline and 16 weeks

Interventionscore on a scale (Mean)
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin-2.23
Placebo-6.30

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Change in Percent Predicted Absolute Forced Vital Capacity (FVC) in Participants With Pulmonary Sarcoidosis, Comparing Baseline With Performance After Completion of 16 Weeks of Therapy.

Change in percent predicted absolute forced vital capacity (FVC) in participants with pulmonary sarcoidosis, comparing baseline with performance after completion of 16 weeks of therapy. This will involve comparing sarcoidosis and placebo after 16 weeks of therapy. (NCT02024555)
Timeframe: Baseline to 16 weeks

Interventionpercentage predicted absolute FVC (Mean)
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin0.35
Placebo0.17

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Six Minute Walk, Distance in Meters

The 6-min walk test (6 MWT) is a submaximal exercise test that entails measurement of distance walked over a span of 6 minutes. (NCT02024555)
Timeframe: Baseline, 4, 8, and 16 and 24 weeks

,
Interventionmeters (Mean)
BaselineWeek 4Week 8Week 16Week 24
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin416.25432.65451.59440.37444.68
Placebo416.41428.35420.21430.85425.18

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FEV1%

FEV1% was measure pre and post 6 minute walk test (NCT02024555)
Timeframe: Baseline, 4, 8, and 16 and 24 weeks

,
InterventionPercentage of predicted FEV1 (Mean)
Baseline preBaseline post4 weeks pre4 weeks post8 weeks pre8 weeks post16 weeks pre16 weeks post24 weeks pre24 weeks post
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin69.1169.9771.5771.9669.3070.3669.8871.3972.2273.09
Placebo67.4573.8169.5673.8173.7174.368.2770.4163.2766.27

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Change in Oxygen Saturation

measured using pulse oximetry (NCT02024555)
Timeframe: Baseline, 4, 8, and 16 and 24 weeks

,
Interventionpercentage of oxygen saturation (Mean)
Baseline to week 4Baseline to week 8Baseline to week 16
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin0.39-0.122.54
Placebo-0.85-0.43-0.46

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Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System

The bactericidal activity (BA) was determined by the rate of change in TTP collected from overnight sputum samples over 8 weeks of treatment in the liquid culture media MGIT system, represented by the model-fitted log(TTP) results as calculated by the regression of the observed log(TTP) results over time. The bactericidal activity of log(TTP) over Day 0 to Day 56 (BATTP[0-56]) was presented and expressed as the daily percentage change in TTP from Day 0 to Day 56. The mean BATTP (0-56) was calculated from Bayesian non-linear mixed effects regression models fitted to log(TTP) collected from sputum samples (observed from Day 0 to Day 56). (NCT02193776)
Timeframe: Day 0 to Day 56 (8 weeks)

Interventionpercentage change in TTP/day (Mean)
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide4.878
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide5.182
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)4.046
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide5.194

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

A TEAE was defined as any AE which started or worsened on or after first study drug administration up to and including the Day 70 follow-up visit (or up to and including 14 days after last study drug administration for participants not having Day 70 follow-up visit). Drug-related TEAEs were defined as TEAEs for which relationship to study drug was indicated as 'possible', 'probable', 'certain' or missing. TEAEs leading to death were defined as TEAEs resulted 'fatal' outcome. Serious TEAEs were defined as TEAEs for which serious was indicated as 'yes'. TEAEs leading to discontinuation of study drug were defined as TEAEs for which action taken with study drug was indicated as 'study drug stopped'. TEAEs leading to early withdrawal from study were defined as TEAEs resulted study discontinuation. Grade III and IV TEAEs were defined as TEAEs for which severity (DMID grade) was indicated as 'Grade 3 (severe)' and 'Grade 4 (potentially life-threatening)' or missing, respectively. (NCT02193776)
Timeframe: First study drug administration (Day 1) up to and including the Day 70 follow-up visit (or up to and including 14 days after last study drug administration for participants not having the Day 70 follow-up visit) (70 days)

,,,
InterventionParticipants (Count of Participants)
Any TEAEDrug-related TEAETEAE leading to deathAny serious TEAEDrug-related serious TEAETEAE leading to discontinuation of study drugTEAE leading to early withdrawal from studyGrade III TEAEGrade IV TEAE
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide452913055177
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide503814265198
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)442914122142
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide574604222131

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Number of Participants With Permanent Discontinuation of Assigned Study Regimen

If it is in the best interest of a participant to stop the study regimen for any reason (NCT02256696)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm 12
Arm 27
Arm 30

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Number of Participants With Grade 3 or Higher Adverse Events

Any Grade 3 event according to the Division of AIDS (DAIDS) toxicity table (NCT02256696)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm 13
Arm 26
Arm 32

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PK (Cmax) of PA-824 at 200 mg Once Daily With Rifampin or Rifabutin-containing Treatment

The Pharmacokinetic results (Cmax) of the study drug when given with a rifampin or a rifabutin. (NCT02256696)
Timeframe: pre-dose and 1, 2, 5, 8, and 24 hours post-dose on Day 14

Interventionmg/L (Mean)
Arm 12.03
Arm 22.69

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Relationship Between PA-824 Exposure (AUC) and Rate of Change in Time to Positivity (TTP) Over 12 Weeks

Relationship between PA-824 exposure (AUC) and rate of change in TTP over 12 weeks, using non-linear mixed effects modeling. The data is reported as percentage increase in TTP per 10 unit increase in PA-824 AUC (% increase/10 unit increase PA-824 AUC). (NCT02256696)
Timeframe: 12 weeks

Intervention% increase/10 unit increase PA-824 AUC (Number)
Arms 1 and 2 (Pretomanid-containing Arms)9.4

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Steady State Pharmacokinetics (PK) (AUC) of PA-824 When Given With Rifampin or Rifabutin

AUC of PA-824 when given with either rifampicin or rifabutin to determine steady state Pharmacokinetics (PK) of PA-824. (NCT02256696)
Timeframe: pre-dose and 1, 2, 5, 8, and 24 hours post-dose on Day 14

Interventionmg*h/L (Mean)
Arm 131.91
Arm 259.05

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Percentage of Participants With Sputum Culture Conversion by 8 Weeks of Treatment

Percentage of participants whose sputum converts from positive to negative at Week 8 time point, on solid and liquid media. (NCT02256696)
Timeframe: 8 weeks

,,
Interventionpercentage of participants (Number)
Liquid mediaSolid media
Arm 17998
Arm 289100
Arm 36996

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Time to Culture Conversion on Solid Medium

The time (days) it takes for the sputum to convert form positive to negative on solid medium (NCT02256696)
Timeframe: 12 weeks

,,
Interventiondays (Median)
Time to conversion on solid culture (mITT)Time to conversion on solid culture (per protocol)
Arm 12828
Arm 22121
Arm 34242

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Time to Sputum Culture Conversion on Liquid Medium

The time (days) it takes for the sputum to convert from positive to negative. (NCT02256696)
Timeframe: 12 weeks

,,
Interventiondays (Median)
Time to culture conversion (mITT)Time to culture conversion (per protocol)
Arm 14242
Arm 22828
Arm 35656

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Other PK Measures: Median Time to Maximal Drug Concentration (Tmax)

Tmax of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionhours (Median)
RifampinEthambutolAzithromycin
CF Patients, Fasting1.52.32.0
CF Patients, Food2.52.02.0
Healthy Controls1.52.32.0

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Other PK Measures: Half-life (t1/2)

t1/2 of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionhours (Median)
RifampinEthambutolAzithromycin
CF Fasting3.44.35.2
CF Food3.44.76.6
Healthy Controls3.85.36.2

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Other PK Measures: Drug Clearance

"drug clearance of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls~Reported here are the Median (range) CL in the CF fasting state compared to HC for Rifampin." (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
InterventionL/h (Median)
RifampinEthambutolAzithromycin
CF Fasting7.942.473.6
CF Food7.637.382.8
Healthy Controls5.145.388.6

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Covariates of PK Measures: Body Mass Index

Body mass index (BMI). Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs (NCT02372383)
Timeframe: baseline

Interventionkg/m^2 (Median)
Healthy Controls23.0
CF Fasting21.9

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Covariates of PK Measures: C-reactive Protein (CRP)

Median Concentration of C-reactive Protein. Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs. (NCT02372383)
Timeframe: baseline

Interventionmg/dL (Median)
Healthy Controls0.2
CF Fasting0.8

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Median Maximal Drug Concentration (Cmax)

Cmax of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls. (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionmg/L (Median)
RifampinEthambutolAzithromycin
CF Fasting12.54.22.0
CF Food11.24.32.2
Healthy Controls16.563.01.1

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Area Under the Curve (AUC)

AUC of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls. (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionmg*h/L (Median)
RifampinEthambutolAzithromycin
CF Fasting7621.86.8
CF Food79.223.66
Healthy Controls118.321.45.6

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Covariates of PK Measures: Creatinine

Creatinine. Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs (NCT02372383)
Timeframe: baseline

Interventionmg/dL (Median)
Healthy Controls1.0
CF Fasting0.9

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Other PK Measures: Volume of Distribution (Vd)

Vd of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
InterventionL (Median)
RifampinEthambutolAzithromycin
CF Fasting39.7274.6549.2
CF Food37.4354.3621.3
Healthy Controls31.3352.8717.0

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Covariates of PK Measures: Circulating Neutrophil Count

Circulating neutrophil count. Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs (NCT02372383)
Timeframe: baseline

Intervention10^3 cells/uL (Median)
Healthy Controls3.0
CF Fasting3.8

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STREAM Stage 2 Primary Outcome Measure (the Proportion of Patients With a Favourable Outcome at Week 76)

The primary efficacy outcome of the STREAM Stage 2 comparison is status at Week 76 i.e. the proportion of patients with a favourable outcome at Week 76 (NCT02409290)
Timeframe: 76 weeks

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)0
Regimen B (Control Regimen)133
Regimen C (Oral Regimen)162
Regimen D (6-month Regimen)122

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Proportion of Patients With Acquired Drug Resistance

The proportion of patients with acquired drug resistance (any drug) (NCT02409290)
Timeframe: 132 weeks

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)0
Regimen B (Control Regimen)5
Regimen C (Oral Regimen)5
Regimen D (6-month Regimen)3

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Favourable Outcome After Long-term Follow-up (132 Weeks)

The proportion of patients with a favourable outcome at their last efficacy visit (NCT02409290)
Timeframe: Last efficacy visit, between 96 and 132 weeks

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)17
Regimen B (Control Regimen)126
Regimen C (Oral Regimen)152
Regimen D (6-month Regimen)115

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Failure or Recurrence (FoR)

The proportion of patients with failure or recurrence (FoR) (NCT02409290)
Timeframe: 132 weeks, control regimen (arm B) using concurrent controls only

InterventionParticipants (Count of Participants)
Regimen B (Control Regimen)14
Regimen D (6-month Regimen)2

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Failure or Recurrence (FoR)

probable or definite failure or recurrence (FoR) (NCT02409290)
Timeframe: final efficacy week (between 96 and 132 weeks)

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)0
Regimen B (Control Regimen)17
Regimen C (Oral Regimen)4
Regimen D (6-month Regimen)0

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Caloric Intake on 24-hour Dietary Recall Method at the 2nd and 6th.

The average calorie intake (in kcal/day) was assessed by the 24-hour dietary recall questionnaire and calculated by NutriSurvey software version 2005, with the country-specific food database for Indonesia. (NCT02554318)
Timeframe: In the course of the 8 week intervention, two interviews were conducted; at the 2nd and 6th week.

,
InterventionKcal/day (Mean)
2nd week6th weekAverage
Control1844.642059.271972.12
Intervention1980.102227.982113.16

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Change in Distance on 6-minute Walk Test (6MWT) From Baseline at 2 Months

The change distance in meters scale as assessed by 6MWT according to American Thoracic Society (ATS) 2002 guidelines. The 6MWT was carried out on a track along the 30-meter corridor marked by two colored cones placed at both ends of the track alignment. The participants were asked using the standard instruction to walk at their self-selected pace back and forth between the cones as far as they could for 6 minutes. The distance taken by each participant was measured and then recorded. Instructions were given to every patient by reading a guideline with the same intonations to every patient before performing the test. The result of the 6MWT was expressed in meters. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Higher scores reflected better physical function outcomes. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionMeter (Mean)
Intervention49.67
Control25.75

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Change in Bodyweight on a Digital Weight Scale From Baseline at 2 Months

Change of body weight of the participants over the two months intervention period as measured on a kilograms scale. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Positive numbers represent increases and negative numbers represent decreases. A higher value score in change means a better outcome on nutritional status for the patients after the study. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionKilogram (Mean)
Intervention2.80
Control1.44

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Change in Body Mass Index (BMI) From Baseline at 2 Months

The change in BMI was assessed by a digital weight scale and height scale (kg/m²). The formula for BMI is weight in kilograms divided by height in meters squared. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Higher scores reflected the better nutritional status results of the patients. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionKg/m² (Mean)
Intervention1.13
Control0.54

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Change in Hand-grip Strength on a Digital Dynamometer Scale From Baseline at 2 Months

The change of hand-grip strength of the participants over the two months intervention period was measured on a kilograms scale. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Positive numbers represent increases and negative numbers represent decreases. The higher scores reflected the better physical function outcomes of the patients. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionKilogram (Mean)
Intervention3.90
Control0.84

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Protein Intake on 24-hour Dietary Recall Method.

The average protein intake (in Gram/day) was assessed by the 24-hour dietary recall questionnaire and calculated using NutriSurvey software version 2005, with the country specific food database for Indonesia. (NCT02554318)
Timeframe: In the course of the 8 week intervention, two interviews were conducted; at the 2nd and 6th week.

,
InterventionGram/day (Mean)
2nd week6th weekAverage
Control69.4973.3571.42
Intervention77.3477.7077.52

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Comparison of the Rate of Treatment Success at 18 Months (After Treatment Initiation) Between Arms B and C

Estimation of the lower bound of a one-sided 95% confidence interval of the difference in success rates between arms B and C. If the lower bound is greater than -7%, this will be evidence that the treatment-shortening arm is not inferior to the standard duration arm. (NCT02821832)
Timeframe: 18 months

,,
InterventionParticipants (Count of Participants)
CuredConfirmed relapsesLate withdrawal, lost to follow-upProbable relapsesTreatment Failure
Arm A21751311
Arm B1211910
Arm C1179634

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Number of Participants With Culture Negative Status by 8 Weeks

Culture negative status is achieved when a participant produces at least two negative culture results at different visits (at least 7 days apart) without an intervening positive culture result for M.tb. (NCT03338621)
Timeframe: Days 0-56 (8 weeks)

InterventionParticipants (Count of Participants)
Drug Sensitive-TB 2HRZE/4HR70
Drug Sensitive-TB 4BPaMZ122

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Time to Culture Negative Status

Culture conversion is a diagnostic criteria indicating the point at which samples taken from a patient infected with a tuberculosis can no longer produce tuberculosis cell cultures, that point is considered culture negativity (NCT03338621)
Timeframe: During treatment (17 or 26 weeks)

Interventionweeks (Median)
Drug Sensitive-TB BPaMZ6
Drug Sensitive-TB 2HRZE/4HR11
Drug Resistant-TB BPaMZ5

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