Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure–activity relationship studies
作者:Sandra Gemma、Luisa Savini、Maria Altarelli、Pierangela Tripaldi、Luisa Chiasserini、Salvatore Sanna Coccone、Vinod Kumar、Caterina Camodeca、Giuseppe Campiani、Ettore Novellino、Sandra Clarizio、Giovanni Delogu、Stefania Butini
DOI:10.1016/j.bmc.2009.06.051
日期:2009.8
A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 mu g/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. (C) 2009 Elsevier Ltd. All rights reserved.