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BioAssay: AID 408874

Cytotoxicity against african green monkey Vero cells after 5 days

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: 408874
Data Source: ChEMBL (556903)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-14

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: 80583
Target Type: CELL-LINE
Cell Line: Vero
Tissue: Kidney cells
Pref Name: Vero
Organism: Chlorocebus aethiops
Tax ID: 9534
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: Vero

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Maximal non-toxic dose 50 activity commentMaximal non-toxic dose 50 activity commentString
2Maximal non-toxic dose 50 standard flagMaximal non-toxic dose 50 standard flagInteger
3Maximal non-toxic dose 50 qualifierMaximal non-toxic dose 50 qualifierString
4Maximal non-toxic dose 50 published valueMaximal non-toxic dose 50 published valueFloatug ml-1
5Maximal non-toxic dose 50 standard valueMaximal non-toxic dose 50 standard valueFloatug ml-1

Data Table (Concise)
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