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|Title:||New derivatives of BM212. a class of antimycobacterial compounds based on the pyrrole ring as a scaffold||Authors:||Biava, M
PORRETTA G., C
|Keywords:||Atypical mycobacteria; BM212; Cytotoxicity; In vitro activity; Intramacrophagic activity; Lead compound; Mycobacterium tuberculosis; Pharmacophore; Protection index; Pyrroles||Issue Date:||2007||Project:||None||Journal:||MINI-REVIEWS IN MEDICINAL CHEMISTRY||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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