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BioAssay: AID 408873

Protection index, ratio of MNTD50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis 103471

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(19)
 
 
Unspecified(19)
 
 
 Tested Substances
 Tested Substances
All(19)
 
 
Unspecified(19)
 
 
 Related BioAssays
 Related BioAssays
AID: 408873
Data Source: ChEMBL (556902)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-07-02

Data Table ( Complete ):           All
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: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
ChEMBL Assay Type: Unassigned

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Assay Cell Type: Vero

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ratio activity commentRatio activity commentString
2Ratio standard flagRatio standard flagInteger
3Ratio qualifierRatio qualifierString
4Ratio published valueRatio published valueFloat
5Ratio standard valueRatio standard valueFloat

Data Table (Concise)
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