A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 μg/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. © 2009 Elsevier Ltd. All rights reserved.
Gemma, S., Savini, L., Altarelli, M., Tripaldi, P., Chiasserini, L., Sanna Coccone, S., et al. (2009). Development of Antitubercular Compounds Based on a 4-Quinolylhydrazone Scaffold. Further Structure-activity Relationship Studies. BIOORGANIC & MEDICINAL CHEMISTRY, 17(16), 6063-6072 [10.1016/j.bmc.2009.06.051].
Development of Antitubercular Compounds Based on a 4-Quinolylhydrazone Scaffold. Further Structure-activity Relationship Studies
Gemma, Sandra;Savini, Luisa;Altarelli, Maria;Tripaldi, Pierangela;Chiasserini, Luisa;Sanna Coccone, Salvatore;Vinod, Kumar;Camodeca, Caterina;Campiani, Giuseppe;Butini, Stefania
2009-01-01
Abstract
A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 μg/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. © 2009 Elsevier Ltd. All rights reserved.File | Dimensione | Formato | |
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https://hdl.handle.net/11365/3827
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