Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class.
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.
Biava
Mariangela
M
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
Porretta
Giulio Cesare
GC
Poce
Giovanna
G
Deidda
Delia
D
Pompei
Raffaello
R
Tafi
Andrea
A
Manetti
Fabrizio
F
D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*
D000995:Antitubercular Agents; D010879:Piperazines; D011758:Pyrroles; C115651:BM 212