Details

Autor(en) / Beteiligte

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

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry, 2005-02, Vol.13 (4), p.1221-1230

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2005

Quelle

MEDLINE

Beschreibungen/Notizen

• Previously we have identified BM 212, a pyrrole derivative with good in vitro activity against mycobacteria and a four-feature pharmacophore model derived from it and many other antimycobacterial compounds synthesized by us. On SAR and molecular modeling considerations, we prepared new pyrrole derivatives in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis. 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.