Details

Autor(en) / Beteiligte

• Biava, M
• Porretta, G C
• Manetti, F

Titel

New derivatives of BM212: A class of antimycobacterial compounds based on the pyrrole ring as a scaffold

Ist Teil von

• Mini reviews in medicinal chemistry, 2007-01, Vol.7 (1), p.65-78

Ort / Verlag

Netherlands

Erscheinungsjahr

2007

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.