Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies.
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.
Gemma
Sandra
S
European Research Centre for Drug Discovery & Development, Università di Siena, Italy.
Savini
Luisa
L
Altarelli
Maria
M
Tripaldi
Pierangela
P
Chiasserini
Luisa
L
Coccone
Salvatore Sanna
SS
Kumar
Vinod
V
Camodeca
Caterina
C
Campiani
Giuseppe
G
Novellino
Ettore
E
Clarizio
Sandra
S
Delogu
Giovanni
G
Butini
Stefania
S
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D002522:Chlorocebus aethiops; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013329:Structure-Activity Relationship; D014709:Vero Cells
D000995:Antitubercular Agents; D006835:Hydrazones