A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.

Gemma, S., Savini, L., Altarelli, M., Tripaldi, P., Chiasserini, L., Coccone, S., Kumar, V., Camodeca, C., Campiani, G., Novellino, E., Clarizio, S., Delogu, G., Butini, S., Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies, <<BIOORGANIC & MEDICINAL CHEMISTRY>>, 2009; 17 (16): 6063-6072. [doi:10.1016/j.bmc.2009.06.051] [http://hdl.handle.net/10807/6591]

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Clarizio, Sandra;Delogu, Giovanni;
2009

Abstract

A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.
2009
Inglese
Gemma, S., Savini, L., Altarelli, M., Tripaldi, P., Chiasserini, L., Coccone, S., Kumar, V., Camodeca, C., Campiani, G., Novellino, E., Clarizio, S., Delogu, G., Butini, S., Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies, <<BIOORGANIC & MEDICINAL CHEMISTRY>>, 2009; 17 (16): 6063-6072. [doi:10.1016/j.bmc.2009.06.051] [http://hdl.handle.net/10807/6591]
File in questo prodotto:
Non ci sono file associati a questo prodotto.

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/10807/6591
Citazioni
  • ???jsp.display-item.citation.pmc??? 5
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact