New Derivatives of BM212: A Class of Antimycobacterial Compounds Based on the Pyrrole Ring as a Scaffold

Author(s): M. Biava , G. C. Porretta , F. Manetti .

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 7 , Issue 1 , 2007

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Abstract:

During our investigation in the area of antimycobacterial agents, we have identified the 1,5-(4-chlorophenyl)-2- methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM212) as the lead compound for a new class of antimycobacterial pyrrole derivatives with potent in vitro activity against mycobacteria and with low cytotoxicity. We have also identified the salient structural features of BM212, while structure-activity relationships (SAR) and molecular modeling studies on pyrrole compounds allowed us to design and synthesize additional analogues. Among them, seven compounds revealed a very high activity (better than that of BM212 toward mycobacteria) and a very interesting protection index, comparable to that of reference compounds, such as isoniazid, streptomycin and rifampin.

Keywords: BM212, lead compound, mycobacterium tuberculosis, atypical mycobacteria, in vitro activity, intramacrophagic activity, pyrroles, pharmacophore, cytotoxicity, protection index

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Article Details

VOLUME: 7
ISSUE: 1
Year: 2007
Page: [65 - 78]
Pages: 14
DOI: 10.2174/138955707779317786

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