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, M., Porretta, G.C., Poce, G., Deidda, D., Pompei, R., Tafi, A., et al. (2005). Antimycobacterial compounds. Optimization of the BM212 structure, the lead compound for a new pyrrole derivative class. BIOORGANIC & MEDICINAL CHEMISTRY, 13(4), 1221-1230 [10.1016/j.bmc.2004.11.018].

Antimycobacterial compounds. Optimization of the BM212 structure, the lead compound for a new pyrrole derivative class

Tafi, Andrea;Manetti, Fabrizio
2005-01-01

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 Mycobacterium tuberculosis and atypical mycobacteria.
2005
Biava, M., Porretta, G.C., Poce, G., Deidda, D., Pompei, R., Tafi, A., et al. (2005). Antimycobacterial compounds. Optimization of the BM212 structure, the lead compound for a new pyrrole derivative class. BIOORGANIC & MEDICINAL CHEMISTRY, 13(4), 1221-1230 [10.1016/j.bmc.2004.11.018].
File in questo prodotto:
File Dimensione Formato  
2005BioorgMedChemAntiTBpirroli.pdf

non disponibili

Tipologia: Post-print
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 389.41 kB
Formato Adobe PDF
389.41 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/22367
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo