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

[ Vol. 7 , Issue. 1 ]

Author(s):

M. Biava, G. C. Porretta and F. Manetti   Pages 65 - 78 ( 14 )

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

Affiliation:

Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita "La Sapienza", Piazzale Aldo Moro 5, I-00185 Roma, Italy.



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