Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies.
Gemma S, Savini L, Altarelli M, Tripaldi P, Chiasserini L, Coccone SS, Kumar V, Camodeca C, Campiani G, Novellino E, Clarizio S, Delogu G, Butini S.
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.