Compounds > bm 212
Page last updated: 2024-12-08

bm 212

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

BM 212: anti-mycobacterial agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID456926
CHEMBL ID321077
SCHEMBL ID1452627
MeSH IDM0297688

Synonyms (23)

Synonym
bm 212
bm212
1-[[1,5-bis(4-chlorophenyl)-2-methyl-pyrrol-3-yl]methyl]-4-methyl-piperazine
bm-212
1-{[1,5-bis(4-chlorophenyl)-2-methylpyrrol-3-yl]methyl}-4-methylpiperazine
1-[[1,5-bis(4-chlorophenyl)-2-methylpyrrol-3-yl]methyl]-4-methylpiperazine
CHEMBL321077
SCHEMBL1452627
1,5-di(4-chlorophenyl)-2-methyl-3-(4-methylpiperazin-1-yl)methylpyrrole
u9hsu4gzwl ,
146204-42-4
piperazine, 1-((1,5-bis(4-chlorophenyl)-2-methyl-1h-pyrrol-3-yl)methyl)-4-methyl-
unii-u9hsu4gzwl
bm212 cpd
AC-35388
HY-100725
CS-5953
AKOS032944899
BCP24821
BS-15436
Q27290962
1-((1,5-bis(4-chlorophenyl)-2-methyl-1h-pyrrol-3-yl)methyl)-4-methylpiperazine
1-{[1,5-bis(4-chlorophenyl)-2-methyl-1h-pyrrol-3-yl]methyl}-4-methylpiperazine

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The focus was on the pharmacokinetics, the metabolism, the dose dependency and gender differences of the pharmacokinetic parameters of BM 113 and its main desacetylated metabolite, BM 212."( Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part III: Pharmacokinetics, metabolism, dose dependency and gender effect after single or repeated administration to human healthy volunteers.
Buzas, A; Duchêne, P; Houin, G; Ladure, P; Laneury, JP; Merour, JY; Ollivier, R; Tran, G, 1999)		0.5

Dosage Studied

ExcerptRelevanceReference
" HPLC dosage of BM 212, using a specific method, showed that BM 212 represented 62% of the urine radioactivity."( Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part III: Pharmacokinetics, metabolism, dose dependency and gender effect after single or repeated administration to human healthy volunteers.
Buzas, A; Duchêne, P; Houin, G; Ladure, P; Laneury, JP; Merour, JY; Ollivier, R; Tran, G, 1999)		0.65
" The best compound identified to date was progressed to dose-response studies in an acute murine TB infection model."( Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection.
Agus, E; Alfonso, S; Ballell, L; Bates, RH; Biava, M; Botta, M; Cocozza, M; De Logu, A; De Rossi, E; Franzblau, SG; La Rosa, V; Manetti, F; Ortega, F; Pasca, MR; Poce, G; Porretta, GC; Rullas, J; Wae, B, 2013)		0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID1330712Cytotoxicity against mouse RAW cells assessed as reduction in cell viability at =>3 uM measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID1296092Inhibition of multidrug resistance efflux pump in Mycobacterium aurum ATCC 23366 assessed as inhibition of ethidium bromide efflux by measuring relative fluorescence units for ethidium bromide accumulation at 1/4 times MIC incubated for 60 mins by fluorim2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID449211Cytotoxicity against african green monkey Vero cells after 72 hrs2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID1296077Antimycobacterial activity against Mycobacterium bovis BCG Pasteur ATCC 35734 assessed as inhibition of mycobacterial growth incubated for 24 hrs by MABA method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID145132In vitro antibacterial activity against Mycobacterium tuberculosis 1034711999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID1462357Protection index, ratio of IC50 for HepG2 cells to MIC for Mycobacterium tuberculosis H37Rv
AID1296090Selectivity index, ratio of GIC50 for cytotoxicity against mouse RAW264.7 cells to MIC for Mycobacterium tuberculosis H37Rv ATTC 272942016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID1296078Antimycobacterial activity against Mycobacterium aurum ATCC 23366 assessed as inhibition of mycobacterial growth incubated for 4 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID1296080Antimycobacterial activity against Mycobacterium tuberculosis mc'2-7000x assessed as inhibition of mycobacterial growth2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID1296081Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATTC 27294 assessed as inhibition of mycobacterial growth incubated for 7 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID408874Cytotoxicity against african green monkey Vero cells after 5 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1296083Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis isolate MDR2 assessed as inhibition of mycobacterial growth incubated for 9 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID218066In vitro cytotoxicity against vero cells1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID1330705Solubility of the compound at pH 4.5 by HPLC method2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID408872Antimycobacterial activity against Mycobacterium avium CIP 1033172008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID144022In vitro antibacterial activity agains Mycobacterium gordonae 64271999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID143714In vitro antibacterial activity against Mycobacterium avium 1033171999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID268910Protection index, cytotoxicity against Vero cell line/antibacterial activity against Mycobacterium tuberculosis 1034712006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID449210Antimycobacterial activity against Mycobacterium avium CIP 103317 by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID1462340Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 6 days by resazurin dye based assay
AID1462343Half life in mouse microsomes
AID1659811Antitubercular activity against Mycobacterium tuberculosis harboring mmpL32020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Molecule Property Analyses of Active Compounds for
AID1296076Antimycobacterial activity against Mycobacterium smegmatis str. MC2 155 ATCC 700084 assessed as inhibition of mycobacterial growth incubated for 24 hrs by MABA method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID1330700Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID144296In vitro antibacterial activity against Mycobacterium marinum 64231999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID1330707Solubility of the compound at pH 10.2 by HPLC method2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID268908Antibacterial activity against Mycobacterium tuberculosis 1034712006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID408870Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID268911Antibacterial activity against Mycobacterium avium2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID1330702Selectivity index, ratio of IC50 for human HepG2 cells to MIC for Mycobacterium tuberculosis H37Rv2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID449208Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID268912Antibacterial activity against Mycobacterium marinum2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID370061Selectivity index, ratio of MIC for Mycobacterium tuberculosis to cytotoxicity to african green monkey Vero cells2005Antimicrobial agents and chemotherapy, Jun, Volume: 49, Issue:6
New small-molecule synthetic antimycobacterials.
AID1330697Cytotoxicity against human THP1 cells assessed as reduction in cell viability at =>3 uM measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID1330703Solubility of the compound at pH 1.2 by HPLC method2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID449207Antimycobacterial activity against Mycobacterium tuberculosis CIP 103471 by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID408875Antimycobacterial activity against Mycobacterium tuberculosis 1034712008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1330711Protein binding human plasma at 150 uM measured after 30 mins by equilibrium dialysis method2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID1330709Metabolic stability in mouse liver microsomes at 1 or 50 uM measured after 30 to 60 mins in presence of cofactor by LC-MS/MS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID408877Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1296082Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis isolate MDR1 assessed as inhibition of mycobacterial growth incubated for 9 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID1330701Selectivity index, ratio of IC50 for human A549 cells to MIC for Mycobacterium tuberculosis H37Rv2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID408878Antimycobacterial activity against Mycobacterium smegmatis CIP 1035992008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1296091Selectivity index, ratio of GIC50 for cytotoxicity against human THP1 cells to MIC for Mycobacterium tuberculosis H37Rv ATTC 272942016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID408873Protection index, ratio of MNTD50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis 1034712008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1330708Metabolic stability in human plasma at 50 uM measured after 60 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID1330699Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID268909Cytotoxicity against Vero cell line2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID1330696Antimycobacterial activity against Mycobacterium tuberculosis by broth microdilution assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID1330704Solubility of the compound at pH 2.2 by HPLC method2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID449209Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis ATCC 35838 by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID1462358Protection index, ratio of IC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv
AID1330710Metabolic stability in human liver microsomes at 1 or 50 uM measured after 30 to 60 mins in presence of cofactor by LC-MS/MS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID1462342Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
AID1296088Cytotoxic activity against human THP1 cells assessed as reduction in cell viability incubated for 48 hrs by trypan blue based assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID370056Antimycobacterial activity against Mycobacterium tuberculosis2005Antimicrobial agents and chemotherapy, Jun, Volume: 49, Issue:6
New small-molecule synthetic antimycobacterials.
AID408879Antimycobacterial activity against Mycobacterium marinum CIP 64232008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1462359Antitubercular activity against clinical isolates of Mycobacterium tuberculosis by broth microdilution assay
AID1296089Cytotoxic activity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by trypan blue based assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID1330698Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition by Alamar-Blue assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID449212Protection index, ratio of MNTD for african green monkey Vero cells to MIC for Mycobacterium tuberculosis CIP 1034712009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID1297708Antitubercular activity against Mycobacterium tuberculosis clinical isolate by BACTEC 460 TB 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.
AID1330706Solubility of the compound at pH 7.4 by HPLC method2016European journal of medicinal chemistry, Oct-21, Volume: 122Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.
AID268913Antibacterial activity against Mycobacterium smegmatis2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID144445In vitro antibacterial activity against Mycobacterium smegmatis 1035991999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID408871Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (13.64)18.2507
2000's9 (40.91)29.6817
2010's8 (36.36)24.3611
2020's2 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.52

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

MetricThis Compound (vs All)
Research Demand Index37.52 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.80 (4.65)
Search Engine Demand Index34.82 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (4.55%)5.53%
Reviews4 (18.18%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (77.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
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
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.		2.520aromatic ether;
nitrile;
polyether;
tertiary amino compound
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		2.4920hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. 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.		2.1310aminoquinoline;
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.		3.3510monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
isoniazid
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.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		3.4370carbohydrazideantitubercular agent;
drug allergen
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		2.0710alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		7.17161pyrrole;
secondary amine
adamantane
Adamantane: A tricyclo bridged hydrocarbon.		2.5220adamantanes;
polycyclic alkane
ethambutol
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). 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.		2.1310ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
streptomycin
[no description available]		3.1250antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor
sulfometuron methyl
sulfometuron methyl: structure given in first source. sulfometuron methyl : A benzoate ester that is the methyl ester of 2-{[(4,6-dimethylpyrimidin-2-yl)carbamoyl]sulfamoyl}benzoic acid.		3.1210benzoate ester;
N-sulfonylurea;
pyrimidines		EC 2.2.1.6 (acetolactate synthase) inhibitor;
herbicide
4(5)-phenylimidazole
4(5)-phenylimidazole: tautomeric cpd; cytochrome P450 14alpha-sterol demethylase, CYP51 antagonist		3.3510
sr141716
[no description available]		2.1310amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
linezolid
[no description available]		3.3510acetamides;
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		4.0920
u 100480
U 100480: structure given in first source		4.0920
1,3-benzothiazol-2-yl(thiomorpholin-4-yl)methanone
[no description available]		2.1310benzothiazoles
valinomycin
Valinomycin: A cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins. It is composed of 3 moles each of L-valine, D-alpha-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring. (From Merck Index, 11th ed) Valinomycin is a potassium selective ionophore and is commonly used as a tool in biochemical studies.. valinomycin : A twelve-membered cyclodepsipeptide composed of three repeating D-alpha-hydroxyisovaleryl-D-valyl-L-lactoyl-L-valyl units joined in sequence. An antibiotic found in several Streptomyces strains.		2.110cyclodepsipeptide;
macrocycle		antimicrobial agent;
antiviral agent;
bacterial metabolite;
potassium ionophore
sq 109
N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine: has antitubercular activity		3.9330
menaquinone 6
menaquinone 6: RN given refers to (all-E)-isomer		2.110
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.		4.0920aromatic ether;
naphthalenes;
organobromine compound;
quinolines;
tertiary alcohol;
tertiary amino compound		antitubercular agent;
ATP synthase inhibitor
sri 286
[no description available]		3.3510
opc-67683
OPC-67683: an antitubercular agent		3.3510piperidines
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
btz 043
[no description available]		3.3510
piperidines
Piperidines: A family of hexahydropyridines.		3.3811
cord factors
Cord Factors: Toxic glycolipids composed of trehalose dimycolate derivatives. They are produced by MYCOBACTERIUM TUBERCULOSIS and other species of MYCOBACTERIUM. They induce cellular dysfunction in animals.		2.5220
trehalose monomycolate
trehalose monomycolate : Any trehalose bearing a single O-mycolate substituent; obtained via extraction of the cell wall of Mycobacterium bovis.		2.5220
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)		3.2860cyclic 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
ConditionIndicatedRelationship StrengthStudiesTrials
Koch's Disease
[description not available]		03.7130
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		03.7130
Tuberculosis, Drug-Resistant
[description not available]		02.110
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.		02.110
Atypical Mycobacterial Infection, Disseminated
[description not available]		02.0710