New derivatives of BM212: A class of antimycobacterial compounds based on the pyrrole ring as a scaffold.
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.
Biava
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Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, Piazzale Aldo Moro 5, I-00185 Roma, Italy. Mariangela.Biava@uniroma1.it
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D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology
D000995:Antitubercular Agents; D010879:Piperazines; D011758:Pyrroles; C115651:BM 212