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 Myeobacterium tuberculosis and atypical mycobacteria. (C) 2004 Elsevier Ltd. All rights reserved.
Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class / Biava, Mariangela; Porretta, Giulio Cesare; Poce, Giovanna; Delia, Deidda; Raffaello, Pompei; Andrea, Tafi; Fabrizio, Manetti. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 13:4(2005), pp. 1221-1230. [10.1016/j.bmc.2004.11.018]
Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class
BIAVA, Mariangela;PORRETTA, Giulio Cesare;POCE, Giovanna;
2005
Abstract
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 Myeobacterium tuberculosis and atypical mycobacteria. (C) 2004 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
