Compounds > btz 043
Page last updated: 2024-11-13

btz 043

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Cross-References

ID SourceID
PubMed CID49769085
CHEMBL ID2419018
SCHEMBL ID1752396
MeSH IDM0584079
PubMed CID42609849
CHEMBL ID1822872
SCHEMBL ID2488829
MeSH IDM0584079

Synonyms (69)

Synonym
2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
btz044
btz038
btz043,btz038, btz044
957217-65-1
NCGC00346489-01
S1097
CHEMBL2419018
SCHEMBL1752396
2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-4h-benzo[e][1,3]thiazin-4-one
2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-4h-1,3-benzothiazin-4-one
DTXSID80678524
HMS3654O19
2-[2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4h-1,3 benzothiazin-4-one
btz10526038
btz043 racemate
benzothiazinone 10526038
NCGC00346489-03
CS-0019700
HY-13579A
btz043 (racemate)
SW219325-1
AKOS030626977
FT-0716638
BCP12744
BCP01786
SB22928
CCG-269019
MS-27672
btz043 racemic
SR-05000022484-1
sr-05000022484
NCGC00346489-02
gtuirornxiohqr-uhfffaoysa-n
btz-10526043
btz-043 ,
CHEMBL1822872
bzt043
BCP9000457
btz 043
2-[(3s)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
1161233-85-7
BCPP000312
BTZ043 ,
g55zh52p57 ,
pbtz 169
btz 10526043
unii-g55zh52p57
4h-1,3-benzothiazin-4-one, 2-((2s)-2-methyl-1,4-dioxa-8-azaspiro(4.5)dec-8-yl)-8-nitro-6-(trifluoromethyl)-
2-((2s)-2-methyl-1,4-dioxa-8-azaspiro(4.5)decan-8-yl)-8-nitro-6-trifluoromethyl-4h-1,3-benzothiazin-4-one
SCHEMBL2488829 ,
s1097_selleck
AC-35368
DTXSID80151286
HY-13579
EX-A1012
AKOS030526000
CS-5635
AS-74893
2-[(2s)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-4h-1,3-benzothiazin-4-one
(s)-2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-4h-benzo[e][1,3]thiazin-4-one
[2-[(3s)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-4-oxo-6-(trifluoromethyl)-1,3-benzothiazin-8-yl]azinic acid
mfcd17215196
mmv676603
gtuirornxiohqr-vifpvbqesa-n ,
btz043-racemate
4h-1,3-benzothiazin-4-one, 2-[(2s)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-
Q27278777
EN300-23853592

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In addition, compound 8o was nontoxic to Vero cells and orally bioavailable in a preliminary pharmacokinetics study."( Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
Gao, C; Peng, CT; Wang, NY; Wei, Y; Xia, Y; Xiong, Y; Xu, Y; Ye, TH; You, XY; Yu, LT; Zeng, XX; Zhang, LD; Zuo, WQ, 2013)		0.39
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.89990.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency3.01120.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (188)

Assay IDTitleYearJournalArticle
AID765962Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
AID765964Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 by microplate alamar blue assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
AID1192368Aqueous solubility of the compound by HPLC method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives.
AID1077009Antimycobacterial activity against Mycobacterium tuberculosis2014European journal of medicinal chemistry, Apr-09, Volume: 76Sulfur rich 2-mercaptobenzothiazole and 1,2,3-triazole conjugates as novel antitubercular agents.
AID1164281Antimicrobial activity against wild-type Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 5 days by microdilution method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID765963Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microdilution plate assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
AID1164297Inhibition of Mycobacterium tuberculosis DprE12014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1192367Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 by MABA method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives.
AID765956Antitubercular activity against Mycobacterium avium ATCC 25291 by microdilution plate assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
AID1164294Antimicrobial activity against Mycobacterium tuberculosis assessed as growth inhibition after 5 days by microdilution method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1192369Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives.
AID765957Antitubercular activity against Mycobacterium smegmatis MC2 155 by microplate alamar blue assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
AID765955Lipophilicity, log P of the compound by shake flask method2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
AID1164295Antimicrobial activity against Mycobacterium tuberculosis overexpressing DprE1 assessed as growth inhibition after 5 days by microdilution method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID765960Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
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.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1586245Ratio of MIC for Mycobacterium tuberculosis over expressing DprE1 to MIC for Mycobacterium tuberculosis H37Rv2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Identification and Profiling of Hydantoins-A Novel Class of Potent Antimycobacterial DprE1 Inhibitors.
AID1154353Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis clone 4.1 over expressing DprE1 mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1883703Potency index, ratio of SKLB-TB1001 to test compound CC50 for cytotoxicity against human A549 cells2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1191019Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet biomass reduction assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1154327Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1586244Antibacterial activity against Mycobacterium tuberculosis over expressing DprE1 after 6 days by resazurin dye-based fluorescence assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Identification and Profiling of Hydantoins-A Novel Class of Potent Antimycobacterial DprE1 Inhibitors.
AID706654Antimycobacterial activity against Mycobacterium aurum SB662012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID706656Therapeutic index, ratio of GI50 for human HUVEC cells to MIC for Mycobacterium smegmatis 7000842012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1162181Antimicrobial activity against Mycobacterium smegmatis assessed as intracellular bacterial killing2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID1154547Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 Rv1937/F426C mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1143277Antimycobacterial activity against 3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one-resistant Mycobacterium tuberculosis clone 8.3 assessed as growth inhibition by resazurin assay2014Journal 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.
AID1883686Antibacterial activity against Mycobacterium tuberculosis H37Rv in chronic Mtb infection BALB/c mouse model assessed as reduction in log10 CFU in lungs at 50 mg/kg/day, po via gavage upto 28 days2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID698823AUC in Mycobacterium tuberculosis H37Rv infected BALB/c mouse at 37.5 to 300 mg/kg, po administered 6 times per week for 4 weeks2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1566203Antimycobacterial activity against 1,4-azaindole resistant Mycobacterium tuberculosis H37Rv harbouring DprE1 Y314H mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1577416Inhibition of DprE1 in Mycolicibacterium smegmatis MC2 155 lysate assessed as reduction in epimerization of P[14C]RPP to DP[14C]A at 70 uM measured after 1.5 hrs in presence of NADH by TLC-based autoradiography2019Journal 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.
AID1679148Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAS media assessed as reduction in bacterial growth incubated for 7 days by resazurin dye fluorescence based assay2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID706652Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing GFP2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1570898Prodrug conversion in THF/MeOH solution assessed as (S)-2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-4-oxo-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-8(5H)-ylideneazinic acid formation at 1 mmol in presence of NABD4 measured immediately by LC/MS anal2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1883702Cytotoxicity against human A549 cells2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID760170Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing pCHERRY3 after 4 days by plate format assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Advancement of Imidazo[1,2-
AID1191015Antimycobacterial activity against Mycobacterium marinum ATCC 927 assessed as reduction in bacterial growth incubated for 5 days by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1577418Inhibition of DprE1 in Mycobacterium tuberculosis H37Rv assessed as accumulation of trehalose monomycolates at 10 times MIC measured after 24 hrs in presence of [14C]-acetate by TLC-based autoradiography2019Journal 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.
AID1607513Ratio of MIC for Mycobacterium tuberculosis H37Rv harboring DprE1 G248S mutant to MIC for wild type Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID1191016Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 assessed as reduction in bacterial growth incubated for 6 days by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1154542Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
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.
AID1585116Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay2018European journal of medicinal chemistry, Dec-05, Volume: 160Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
AID1577417Inhibition of DprE1 in Mycobacterium tuberculosis H37Rv assessed as accumulation of trehalose dimycolates at 10 times MIC measured after 24 hrs in presence of [14C]-acetate by TLC-based autoradiography2019Journal 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.
AID1191021Drug metabolism in mouse liver microsomes assessed as formation of 2-((S)-2-Methyl-1,4-dioxa-8-aza-spiro[4.5]dec-8-yl)-8-nitro-1-oxo-6-trifluoromethyl-benzo[e][1,3]thiazin-4-one by LC/MS method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1570902Prodrug conversion in THF/MeOH solution assessed as 5,7-dideuterio-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one formation at 1 mmol treated with NaBD4 for 10 mins followed by AcOH addition and su2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1705304Inhibition of Mycobacterium tuberculosis H37Rv DprE1 assessed as increase in trehalose monomycolates at 100 x MIC incubated for 24 hrs using [14C]acetate by TLC based metabolic labelling assay relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents.
AID1154349Antimycobacterial activity against Mycobacterium tuberculosis over expressing TopA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1570904Prodrug conversion in DMSO-d6 solution assessed as 5-dideuterio-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one formation at 1 mmol treated with NaBD4 for 10 mins in presence of NaBD4 followed by Ac2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID706663Metabolic stability in human liver microsomes2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1191012Antibacterial activity against Acinetobacter baumannii ATCC 17961 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID616779Antituberculosis activity against Mycobacterium tuberculosis H37Rv2011Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18
Current status and research strategies in tuberculosis drug development.
AID1290939Antibacterial activity against Bacillus subtilis ATCC 66332016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID1586237Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 6 days by resazurin dye-based fluorescence assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Identification and Profiling of Hydantoins-A Novel Class of Potent Antimycobacterial DprE1 Inhibitors.
AID1659815Antimycobacterial activity against Mycobacterium tuberculosis expressing DprE12020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Molecule Property Analyses of Active Compounds for
AID1143275Antimycobacterial activity against 3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one-resistant Mycobacterium tuberculosis clone 8.1 assessed as growth inhibition by resazurin assay2014Journal 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.
AID1155088Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Design and Syntheses of Anti-Tuberculosis Agents Inspired by BTZ043 Using a Scaffold Simplification Strategy.
AID1607516Ratio of MIC for Mycobacterium tuberculosis H37Rv harboring DprE1 G17C mutant to MIC for wild type Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID1679145Antitubercular activity against Mycobacterium vaccae assessed as reduction in bacterial growth incubated for 42 hrs by broth microdilution assay2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID1883704Absolute oral bioavailability in overnight fasted Sprague-Dawley rat at 5 mg/kg measured for 0.25 to 24 hrs2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1566194Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial cell growth by resazurin reduction method2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1290938Antimycobacterial activity against Mycobacterium tuberculosis H37Rv cultured in GAS medium after 4 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID1570900Prodrug conversion in THF/MeOH medium assessed as 5-deuterio-N-hydroxy-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-4-oxo-6-(trifluoromethyl)-5H-1,3-benzothiazin-8-imine oxide formation at 1 mmol treated with NaBD4 for 10 mins followed by AcOH ad2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1570906Prodrug conversion in THF/MeOH medium assessed as 5,7-dideuterio-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one formation at 0.05 mmol treated with NaBD4 followed by DIAD addition by LC/MS analysis2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1290940Antibacterial activity against Staphylococcus aureus SG5112016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID1154351Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis over expressing DprE1 C387S mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1570903Prodrug conversion in DMSO-d6 solution assessed as 7-dideuterio-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one formation at 1 mmol treated with NaBD4 for 10 mins in presence of NaBD4 followed by Ac2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1871982Antimycobacterial activity against Mycobacterium tuberculosis2022European journal of medicinal chemistry, Feb-05, Volume: 229Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.
AID706664Metabolic stability in mouse liver microsomes2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1154348Antimycobacterial activity against Mycobacterium tuberculosis over expressing InhA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1191008Antimycobacterial activity against Mycobacterium aurum SB66 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1679144Antitubercular activity against Mycobacterium aurum assessed as reduction in bacterial growth incubated for 42 hrs by broth microdilution assay2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID706657Therapeutic index, ratio of CC50 for human HeLa cells to MIC for Mycobacterium smegmatis 7000842012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID706666Metabolic stability in mouse plasma2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID706661Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1155085Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in GAS medium by microplate alamar blue assay2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Design and Syntheses of Anti-Tuberculosis Agents Inspired by BTZ043 Using a Scaffold Simplification Strategy.
AID1143273Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis harboring DprE1 C-G mutant assessed as growth inhibition by resazurin assay2014Journal 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.
AID1607517Ratio of MIC for Mycobacterium tuberculosis H37Rv harboring DprE1 C387S mutant to MIC for wild type Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID1296443Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as growth inhibition at 0.2 ug/ml preincubated for 24 hrs followed by radiolabeling with [14C]-acetate for 24 hrs2016Journal 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.
AID1154544Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 C387S mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1290941Antibacterial activity against Micrococcus luteus ATCC 102402016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID698825Antimycobacterial activity against Mycobacterium smegmatis2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID706453Ratio of isoniazid MIC to compound MIC for Mycobacterium tuberculosis H37Rv2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1154350Antimycobacterial activity against Mycobacterium tuberculosis over expressing PimA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1155084Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in 7H12 medium by microplate alamar blue assay2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Design and Syntheses of Anti-Tuberculosis Agents Inspired by BTZ043 Using a Scaffold Simplification Strategy.
AID706653Kinetic solubility of the compound at pH 7.42012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1290937Antimycobacterial activity against Mycobacterium tuberculosis H37Rv cultured in 7H12 medium after 4 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID1191013Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 7 days under 7H12 medium by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1607515Ratio of MIC for Mycobacterium tuberculosis H37Rv harboring DprE1 L368P mutant to MIC for wild type Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID698976Antimycobacterial activity against Mycobacterium tuberculosis2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1883705Half life in overnight fasted Sprague-Dawley rat at 5 mg/kg measured for 0.25 to 24 hrs2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1299956Antibacterial activity against Mycobacterium tuberculosis H37Rv in 7H12 medium by microplate alamar blue assay2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
AID1143276Antimycobacterial activity against 3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one-resistant Mycobacterium tuberculosis clone 8.2 assessed as growth inhibition by resazurin assay2014Journal 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.
AID1191018Cytotoxicity against human PC3 cells after 72 hrs by crystal violet biomass reduction assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID698824Cmax in Mycobacterium tuberculosis H37Rv infected BALB/c mouse at 37.5 to 300 mg/kg, po administered 6 times per week for 4 weeks2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1566231Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis H37Rv harbouring DprE1 C387S mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1585123Inhibition of Mycobacterium tuberculosis DprE1 expressed in Escherichia coli BL21(DE3) by fluorescence based assay2018European journal of medicinal chemistry, Dec-05, Volume: 160Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
AID1191017Antimycobacterial activity against Mycobacterium kansasii ATCC 12478 assessed as reduction in bacterial growth incubated for 6 days by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1296444Inhibition of DprE1 in Mycobacterium tuberculosis H37Ra assessed as accumulation of trehalose dimycolate at 0.2 ug/ml preincubated for 24 hrs followed by radiolabeling with [14C]-acetate for 24 hrs by TLC/autoradiographic 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.
AID1191007Antimycobacterial activity against Mycobacterium vaccae IMET10670 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID706667Chemical stability in buffer2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1162180Antimicrobial activity against Mycobacterium smegmatis2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID1299955Antibacterial activity against Mycobacterium tuberculosis H37Rv in GAS medium by microplate alamar blue assay2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
AID1143259Inhibition of Mycobacterium smegmatis DprE1 expressed in Escherichia coli Rosetta cells using farnesyl-phosphoryl-beta-D-ribofuranose as substrate by fluorescence analysis2014Journal 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.
AID1191010Antibacterial activity against Micrococcus luteus ATCC 10240 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1570907Prodrug conversion in THF/MeOH medium assessed as 5,7-dideuterio-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one formation at 0.05 mmol treated with NaBD4 followed by DIAD addition by 1H-NMR analysi2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1154543Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 OE mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1294076Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra after 12 days by XTT-Menadione assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis and docking studies of pyrazine-thiazolidinone hybrid scaffold targeting dormant tuberculosis.
AID706658Cytotoxicity against human HeLa cells after 72 hrs by methylene blue staining2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID706668Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 2745/092012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1191020Cytotoxicity against human HeLa cells after 72 hrs by crystal violet biomass reduction assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1191014Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 7 days under GAS medium by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1224565Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2014European 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.
AID1570899Prodrug conversion in THF/MeOH solution assessed as 7-deuterio-N-hydroxy-2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-4-oxo-6-(trifluoromethyl)-7H-1,3-benzothiazin-8-imine oxide formation at 1 mmol treated with NaBD4 for 10 mins followed by AcOH 2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID698821Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as log reduction of CFU in spleen at 300 mg/kg, po administered 6 times per week for 4 weeks2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1566204Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harbouring DprE1 Y314S mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1679146Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID706665Metabolic stability in human plasma2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1191006Antimycobacterial activity against Mycobacterium smegmatis str. MC2 155 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1154545Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 C387G mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1566201Antimycobacterial activity against Mycobacterium tuberculosis H37Rv overexpressing DprE1 assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1143272Antimycobacterial activity against Mycobacterium tuberculosis overexpressing DprE1 assessed as growth inhibition by resazurin assay2014Journal 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.
AID1288637Antituberculosis activity against Mycobacterium tuberculosis H37Rv in glycerol-alanine salts medium incubated for 4 days by Microplate Alamar Blue assay2016MedChemComm, Jan-01, Volume: 7, Issue:1
Syntheses and Biological Evaluations of Highly Functionalized Hydroxamate Containing and
AID1299962Irreversible inhibition of recombinant Mycobacterium tuberculosis H37Rv DprE1 using FPR as substrate assessed as residual enzymatic activity preincubated for 10 mins followed by substrate addition by fluorescence assay2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
AID1679143Inhibition of Mycobacterium tuberculosis H37Rv DprE1 at 100 times of MIC incubated for 24 hrs by [14C]-acetate radioligand based thin layer chromatography2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
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.
AID706669Antimycobacterial activity against Mycobacterium smegmatis 700084 after 48 hrs by broth microdilution assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID706655Therapeutic index, ratio of GI50 for human K562 cells to MIC for Mycobacterium smegmatis 7000842012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1154352Antimycobacterial activity against TMC207R-resistant Mycobacterium tuberculosis clone 8.1 over expressing DprE1 mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1607512Ratio of MIC for Mycobacterium tuberculosis H37Rv harboring DprE1 E221Q mutant to MIC for wild type Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID1154347Antimycobacterial activity against Mycobacterium tuberculosis over expressing DprE1 after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1607514Ratio of MIC for Mycobacterium tuberculosis H37Rv harboring DprE1 Y314H mutant to MIC for wild type Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID1290942Antibacterial activity against Mycobacterium vaccae IMET 106702016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID706662Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1288636Antituberculosis activity against Mycobacterium tuberculosis H37Rv in 7H12 medium incubated for 4 days by Microplate Alamar Blue assay2016MedChemComm, Jan-01, Volume: 7, Issue:1
Syntheses and Biological Evaluations of Highly Functionalized Hydroxamate Containing and
AID1191011Antibacterial activity against Pseudomonas aeruginosa KW799/61 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1570914Inhibition of DprE1 in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth at <0.004 uM measured in MABA media2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1570911Prodrug conversion in THF/MeOH solution assessed as first order rate constant for protonated metabolite (6H2) formation at 0.01 mmol treated with NaBH4 by UV-visible spectroscopic analysis2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID706659Antiproliferative activity against human K562 cells after 72 hrs by electronic cell analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1143274Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis harboring DprE1 C-S mutant assessed as growth inhibition by resazurin assay2014Journal 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.
AID1154546Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 Y314H mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1679147Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in 7H12 media assessed as reduction in bacterial growth incubated for 7 days by resazurin dye fluorescence based assay2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID1705303Inhibition of Mycobacterium tuberculosis H37Rv DprE1 assessed as increase in trehalose dimycolates at 100 x MIC incubated for 24 hrs using [14C]acetate by TLC based metabolic labelling assay relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents.
AID1883706AUC in overnight fasted Sprague-Dawley rat at 5 mg/kg measured for 0.25 to 24 hrs2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID706670Antimycobacterial activity against Mycobacterium fortuitum B2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1143271Antimycobacterial activity against wild type Mycobacterium tuberculosis H37Rv assessed as growth inhibition by resazurin assay2014Journal 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.
AID1570901Inhibition of DprE1 in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth at 0.02 to 0.03 uM measured in GAS medium2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID1162166Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID1191009Antibacterial activity against Staphylococcus aureus SG511 assessed as reduction in bacterial growth incubated for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1585115Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA2018European journal of medicinal chemistry, Dec-05, Volume: 160Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
AID706660Antiproliferative activity against human HUVEC cells after 72 hrs by methylene blue staining2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of antitubercular benzothiazinone compounds by ligand-based design.
AID1435710Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by broth microdilution method2017European 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.
AID1566202Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis H37Rv harbouring DprE1 C387G mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1191022Drug metabolism in mouse liver microsomes assessed as formation of 2-((S)-2-Methyl-1,4-dioxa-8-aza-spiro[4.5]dec-8-yl)-8-nitro-1,1-dioxo-6-trifluoromethyl-1H-1lambda*6*-benzo[e][1,3]thiazin-4-one by LC/MS method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1299959Inhibition of DprE1 in P-14C-RPP-labelled Mycobacterium smegmatis MC2 155 cell membranes assessed as supression of conversion of decaprenylphosphoryl ribose to decaprenylphosphoryl arabinose after 1 hr by TLC analysis2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
AID1570897Prodrug conversion in THF/MeOH solution assessed as (S)-2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-4-oxo-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-8(7H)-ylideneazinic acid formation at 1 mmol in presence of NABD4 measured immediately by LC/MS anal2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Deuteration of BTZ043 Extends the Lifetime of Meisenheimer Intermediates to the Antituberculosis Nitroso Oxidation State.
AID698820Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as log reduction of CFU in lung at 300 mg/kg, po administered 6 times per week for 4 weeks2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (42)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's30 (71.43)24.3611
2020's12 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.30

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.30 (24.57)
Research Supply Index3.43 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews6 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
Other24 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
isoniazid
hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).. Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.		2.7830carbohydrazideantitubercular agent;
drug allergen
triclosan
[no description available]		2.110aromatic ether;
dichlorobenzene;
monochlorobenzenes;
phenols		antibacterial agent;
antimalarial;
drug allergen;
EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
fungicide;
persistent organic pollutant;
xenobiotic
chloramphenicol
Amphenicol: Chloramphenicol and its derivatives.		2.110C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.110delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
sparfloxacin
[no description available]		2.110fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		2.110aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
bedaquiline
bedaquiline: a diarylquinoline Antitubercular Agent. bedaquiline : A quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria.		2.110aromatic ether;
naphthalenes;
organobromine compound;
quinolines;
tertiary alcohol;
tertiary amino compound		antitubercular agent;
ATP synthase inhibitor
novobiocin
novobiocin : A coumarin-derived antibiotic obtained from Streptomyces niveus.. Novobiocin: An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189)		2.110carbamate ester;
ether;
hexoside;
hydroxycoumarin;
monocarboxylic acid amide;
monosaccharide derivative;
phenols		antibacterial agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Escherichia coli metabolite;
hepatoprotective agent
pbtz169
macozinone: an antitubercular agent; structure in first source		2.1110
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.520cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		2.1310monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
arotinolol
arotinolol: structure given in first source; arotinolol is the (+-)-isomer		3.5110aromatic amide;
thiophenes
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		3.5110aromatic ether;
nitrile;
polyether;
tertiary amino compound
ciprofloxacin
ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.. Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.		2.5220aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
clofazimine
Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.		5.4970monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		2.5220conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
isoniazid
hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).. Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.		6.27170carbohydrazideantitubercular agent;
drug allergen
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		3.23503-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
ono 1078
pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist		3.5110chromones
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		3.1710N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		3.5110phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
kanamycin a
Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components.		2.1310kanamycinsbacterial metabolite
cycloserine
Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).		3.51104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
2-nitrofluorene
2-nitrofluorene: RN given refers to cpd with locant with nitro moiety in 2 position. 2-nitrofluorene : A nitroarene that is fluorene substituted by a nitro group at position 2.		2.5720nitroarenecarcinogenic agent;
mutagen
2-anthramine
2-anthramine: structure		2.2110anthracenamine
ethambutol
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.. 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)		3.5370ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
vancomycin
vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.. Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.		2.5220glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite
streptomycin
[no description available]		3.2350antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor
sodium azide
Sodium Azide: A cytochrome oxidase inhibitor which is a nitridizing agent and an inhibitor of terminal oxidation. (From Merck Index, 12th ed). sodium azide : The sodium salt of hydrogen azide (hydrazoic acid).		2.5720inorganic sodium saltantibacterial agent;
explosive;
mitochondrial respiratory-chain inhibitor;
mutagen
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		3.1910penicillin allergen;
penicillin		antibacterial drug
amikacin
Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group.		3.0540alpha-D-glucoside;
amino cyclitol glycoside;
aminoglycoside;
carboxamide		antibacterial drug;
antimicrobial agent;
nephrotoxin
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		3.5110[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
nitazoxanide
nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug		3.5110benzamides;
carboxylic ester
dup 105
4-methylsulfinylphenyloxooxazolidinylmethylacetamide: structure given in first source		3.1710
fropenem
[no description available]		3.5110faropenem
4(5)-phenylimidazole
4(5)-phenylimidazole: tautomeric cpd; cytochrome P450 14alpha-sterol demethylase, CYP51 antagonist		3.3510
ljc 10627
biapenem: structure given in first source. biapenem : A carbapenem antibiotic in which the azetidine and pyrroline rings carry 1-hydroxymethyl and pyrazolo[1,2-a][1,2,4]triazolium-6-ylthio substituents respectively.		3.5110carbapenems;
organic sulfide;
pyrazolotriazole		antibacterial drug
gentamicin c1a
[no description available]		2.8530gentamycin C
5-nitro-1,10-phenanthroline
5-nitro-1,10-phenanthroline: structure in first source		3.5110
2-(3,4-dichlorophenoxy)-5-nitrobenzonitrile
[no description available]		2.3110
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		4.8450aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
azd2563
posizolid: an antitubercular agent; structure in first source		4.120
nu 6027
[no description available]		3.5110
meropenem
Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.		3.5110alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen
linezolid
[no description available]		5.2640acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
pa 824
pretomanid: nitroimidazopyran derived from 5-nitroimidazoles; a prodrug that requires activation by a bacterial F420-depedent glucose-6-phosphate dehydrogenase (Fgd) and nitroreductase to activate components that then inhibit bacterial mycolic acid and protein synthesis; structure in first source		5.8580
bm 212
BM 212: anti-mycobacterial agent; structure in first source		3.3510
u 100480
U 100480: structure given in first source		5.6750
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		3.5110pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
sq 109
N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine: has antitubercular activity		5.6750
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		2.5220antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
bedaquiline
bedaquiline: a diarylquinoline Antitubercular Agent. bedaquiline : A quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria.		6.0880aromatic ether;
naphthalenes;
organobromine compound;
quinolines;
tertiary alcohol;
tertiary amino compound		antitubercular agent;
ATP synthase inhibitor
ceftazidime
[no description available]		2.1710cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
rifamycin sv
rifamycin SV: RN given refers to parent cpd; structure in Merck Index, 9th ed, #8009. rifamycin SV : A member of the class of rifamycins that exhibits antibiotic and antitubercular properties.		2.110acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterotetracyclic compound;
polyphenol;
rifamycins		antimicrobial agent;
antitubercular agent;
bacterial metabolite
sri 286
[no description available]		3.3510
opc-67683
OPC-67683: an antitubercular agent		5.3560piperidines
sri 224
[no description available]		3.3510
thioacetazone
Thioacetazone: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217). thiosemicarbazone : A hydrazone resulting from the formal condensation of an aldehyde or ketone with the non-thioacylated nitrogen of thiosemicarbazide or its substituted derivatives.		3.3510
tebipenem
tebipenem: an oral carbapenem antibiotic, against penicillin-nonsusceptible Streptococcus pneumoniae; structure in first source		3.5110
dup 721
[no description available]		3.1710
gentamicin sulfate
[no description available]		2.110
lymecycline
Lymecycline: A semisynthetic antibiotic related to TETRACYCLINE. It is more readily absorbed than TETRACYCLINE and can be used in lower doses.. lymecycline : A tetracycline-based broad-spectrum antibiotic. It is approximately 5000 times more soluble than tetracycline base and is unique amongst tetracyclines in that it is absorbed by the "active transport" process across the intestinal wall.		3.5110
pbtz169
macozinone: an antitubercular agent; structure in first source		5.6680
ceritinib
ceritinib: an anaplastic lymphoma kinase inhibitor. ceritinib : A member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(piperidin-4-yl)-5-methylphenyl and 2-(isopropylsulfonyl)phenyl substituents. Used for the treatment of ALK-positive metastatic non-small cell lung cancer.		3.5110aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
4,6-dichloro-n-(4,4-dimethylcyclohexyl)-1h-indole-2-carboxamide
4,6-dichloro-N-(4,4-dimethylcyclohexyl)-1H-indole-2-carboxamide: structure in first source		3.5110
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		5.87160cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
rifabutin
[no description available]		3.1910
amg531
[no description available]		3.5110
ConditionIndicatedRelationship StrengthStudiesTrials
Koch's Disease
[description not available]		05.79100
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		05.79100
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5520
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Pulmonary Consumption
[description not available]		02.9810
Tuberculosis, Pulmonary
MYCOBACTERIUM infections of the lung.		02.9810
Tuberculosis, Drug-Resistant
[description not available]		03.0110
Tuberculosis, Multidrug-Resistant
Tuberculosis resistant to chemotherapy with two or more ANTITUBERCULAR AGENTS, including at least ISONIAZID and RIFAMPICIN. The problem of resistance is particularly troublesome in tuberculous OPPORTUNISTIC INFECTIONS associated with HIV INFECTIONS. It requires the use of second line drugs which are more toxic than the first line regimens. TB with isolates that have developed further resistance to at least three of the six classes of second line drugs is defined as EXTENSIVELY DRUG-RESISTANT TUBERCULOSIS.		03.0110
Latent Tuberculosis
The dormant form of TUBERCULOSIS where the person shows no obvious symptoms and no sign of the causative agent (Mycobacterium tuberculosis) in the SPUTUM despite being positive for tuberculosis infection skin test.		02.1310
Extensively Drug-Resistant Tuberculosis
Tuberculosis resistant to ISONIAZID and RIFAMPIN and at least three of the six main classes of second-line drugs (AMINOGLYCOSIDES; polypeptide agents; FLUOROQUINOLONES; THIOAMIDES; CYCLOSERINE; and PARA-AMINOSALICYLIC ACID) as defined by the CDC.		03.3310