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]
Autori: | ||
Titolo: | Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies | |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.bmc.2009.06.051 | |
Data di pubblicazione: | 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. | |
Lingua: | Inglese | |
Rivista: | ||
Citazione: | 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] | |
Appare nelle tipologie: | Articolo in rivista, Nota a sentenza |