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

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.

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