title: Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies.
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.
authors.affiliation: European Research Centre for Drug Discovery & Development, Università di Siena, Italy.
authors.forename: Sandra
authors.initials: S
authors.lastname: Gemma
authors.forename: Luisa
authors.initials: L
authors.lastname: Savini
authors.forename: Maria
authors.initials: M
authors.lastname: Altarelli
authors.forename: Pierangela
authors.initials: P
authors.lastname: Tripaldi
authors.forename: Luisa
authors.initials: L
authors.lastname: Chiasserini
authors.forename: Salvatore Sanna
authors.initials: SS
authors.lastname: Coccone
authors.forename: Vinod
authors.initials: V
authors.lastname: Kumar
authors.forename: Caterina
authors.initials: C
authors.lastname: Camodeca
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Campiani
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Sandra
authors.initials: S
authors.lastname: Clarizio
authors.forename: Giovanni
authors.initials: G
authors.lastname: Delogu
authors.forename: Stefania
authors.initials: S
authors.lastname: Butini
mesh_terms: 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
chemical_list: D000995:Antitubercular Agents; D006835:Hydrazones