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

作者：Gemma Sandra; Savini Luisa^*; Altarelli Maria; Tripaldi Pierangela; Chiasserini Luisa; Coccone Salvatore Sanna; Kumar Vinod; Camodeca Caterina; Campiani Giuseppe; Novellino Ettore; Clarizio Sandra; Delogu Giovanni; Butini Stefania

来源：Bioorganic & Medicinal Chemistry, 2009, 17(16): 6063-6072.

DOI：10.1016/j.bmc.2009.06.051

• Mycobacterium tuberculosis
• Hydrazone
• Quinoline

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.

• 出版日期2009-8-15