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
Mini-Reviews in Medicinal Chemistry
Title: New Derivatives of BM212: A Class of Antimycobacterial Compounds Based on the Pyrrole Ring as a Scaffold
Volume: 7 Issue: 1
Author(s): M. Biava, G. C. Porretta and F. Manetti
Affiliation:
Keywords: BM212, lead compound, mycobacterium tuberculosis, atypical mycobacteria, in vitro activity, intramacrophagic activity, pyrroles, pharmacophore, cytotoxicity, protection index
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.
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Cite this article as:
Biava M., Porretta C. G. and Manetti F., New Derivatives of BM212: A Class of Antimycobacterial Compounds Based on the Pyrrole Ring as a Scaffold, Mini-Reviews in Medicinal Chemistry 2007; 7 (1) . https://dx.doi.org/10.2174/138955707779317786
DOI https://dx.doi.org/10.2174/138955707779317786 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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