Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class.

Mariangela Biava, Giulio Cesare Porretta, Giovanna Poce, Delia Deidda, Raffaello Pompei, Andrea Tafi, Fabrizio Manetti

Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, P.le A. Moro 5, 00185 Rome, Italy. mariangela.biava@uniroma1.it

Bioorganic & medicinal chemistry 2005 Feb 15

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Our work on antitubercular agents led to the identification of BM 212 as a lead compound among a series of pyrrole derivatives with good in vitro activity against mycobacteria and candidae. Further studies led us to synthesize additional pyrroles bearing the thiomorpholinomethyl moiety and different aryl substituents at N1 and C5. Some of them revealed very active, prompting us to design the new pyrrole derivatives 5-20 in the hope of increasing the activity and better understanding the influence of ortho halogens on the antimycobacterial activity. Microbiological data showed interesting in vitro activity toward Mycobacterium tuberculosis and atypical mycobacteria.

Citation

Mariangela Biava, Giulio Cesare Porretta, Giovanna Poce, Delia Deidda, Raffaello Pompei, Andrea Tafi, Fabrizio Manetti. Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class. Bioorganic & medicinal chemistry. 2005 Feb 15;13(4):1221-30