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2009Gemma 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
Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies.
Bioorganic & medicinal chemistry 2009;17(16):6063-72.
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.

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