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BioAssay: AID 408869

Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates by agar dilution method

Synthesis and biological evaluation of new derivatives of 1,5-bis(4-chlorophenyl)-2-methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM 212, 16) are reported. Variously substituted phenyl rings with different substitution pattern and lipophilicity were added to the pyrrole nucleus to evaluate their influence on the activity toward Mycobacterium tuberculosis (MTB) and atypical mycobacteria. The most active derivatives showed activity between 0.125-0.5 microg/mL (better than 16 and streptomycin) and protection index (64-256) higher than 16 (4) and similar to isoniazid and streptomycin (128). ..more
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 Tested Compounds
 Tested Compounds
All(4)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(4)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 408869
Data Source: ChEMBL (556898)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-14

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: 1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.

Abstract: Synthesis and biological evaluation of new derivatives of 1,5-bis(4-chlorophenyl)-2-methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM 212, 16) are reported. Variously substituted phenyl rings with different substitution pattern and lipophilicity were added to the pyrrole nucleus to evaluate their influence on the activity toward Mycobacterium tuberculosis (MTB) and atypical mycobacteria. The most active derivatives showed activity between 0.125-0.5 microg/mL (better than 16 and streptomycin) and protection index (64-256) higher than 16 (4) and similar to isoniazid and streptomycin (128).
(PMID: 18494459)
Comment
Putative Target:
ChEMBL Target ID: 50309
Target Type: ORGANISM
Pref Name: Mycobacterium tuberculosis
Organism: Mycobacterium tuberculosis
Tax ID: 1773
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
BAO: Assay Format: organism-based format
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1MIC activity commentMIC activity commentString
2MIC standard flagMIC standard flagInteger
3MIC qualifierMIC qualifierString
4MIC published valueMIC published valueFloatug ml-1
5MIC standard valueMIC standard valueFloatug.mL-1
6MIC50 activity commentMIC50 activity commentString
7MIC50 standard flagMIC50 standard flagInteger
8MIC50 qualifierMIC50 qualifierString
9MIC50 published valueMIC50 published valueFloatug ml-1
10MIC50 standard valueMIC50 standard valueFloatug.mL-1
11MIC90 activity commentMIC90 activity commentString
12MIC90 standard flagMIC90 standard flagInteger
13MIC90 qualifierMIC90 qualifierString
14MIC90 published valueMIC90 published valueFloatug ml-1
15MIC90 standard valueMIC90 standard valueFloatug.mL-1

Data Table (Concise)
Data Table ( Complete ):     View All Data
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