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

Authors :
Salvatore Sanna Coccone
Luisa Chiasserini
Ettore Novellino
Maria Altarelli
Sandra Gemma
Caterina Camodeca
Stefania Butini
Giuseppe Campiani
Vinod Kumar
Giovanni Delogu
Luisa Savini
Pierangela Tripaldi
Sandra Clarizio
Gemma, S.
Savini, L.
Altarelli, M.
Tripaldi, P.
Chiasserini, L.
Coccone, S. S.
Kumar, V.
Camodeca, C.
Campiani, G.
Novellino, Ettore
Clarizio, S.
Delogu, G.
Butini, S.
Source :
Bioorganic & Medicinal Chemistry. 17:6063-6072
Publication Year :
2009
Publisher :
Elsevier BV, 2009.

Abstract

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.

Details

ISSN :
09680896
Volume :
17
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry
Accession number :
edsair.doi.dedup.....4cb01c3620d271a31a8fda5941618c7d
Full Text :
https://doi.org/10.1016/j.bmc.2009.06.051