Details

Autor(en) / Beteiligte

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

Titel

Antimycobacterial compounds. New pyrrole derivatives of BM212

Ist Teil von

• Bioorganic & medicinal chemistry, 2004-03, Vol.12 (6), p.1453-1458

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2004

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• We have identified BM212 as a lead compound among a series of pyrrole derivatives with good in vitro activity against mycobacteria and candidae. First studies led us to synthesize some pyrrole compounds in which the thiomorpholine fragment was present. Some compounds revealed very active and these findings prompted us to prepare new pyrrole derivatives 2– 15 in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis and atypical mycobacteria. Previously we have identified BM212 and 1, two pyrrole derivatives with good in vitro activity against mycobacteria, on the base of a four-feature pharmacophore model individuated by us. These findings prompted us to prepare new pyrrole derivatives in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis.