title: Synthesis and anti-mycobacterial activities of triazoloquinolones.
abstract: A number of quinolone derivatives have been reported to possess anti-mycobacterial activity. Generally. Mycobacterium tuberculosis isolates expressing resistance to both isoniazid and rifampin are susceptible to fluoroquinolones. Benzotriazole is a hetero-bicyclic aromatic ring endowed with interesting chemical and biological properties and pharmacological activities. In a preliminary study we have recently reported the activity of triazolo[4,5-h]quinolone-carboxylic acids, a new class of benzotriazole derivatives active against multi-drug resistant M. tuberculosis (MDR-Mtb). In this study we confirm that this novel class of quinolones is endowed with a selective anti-mycobacterial activity, coupled with absence of cytotoxicity. The SAR analysis of the new derivatives in comparison with the previous series shows that the methyl group is the most effective substituent in both N-3 and N-9 positions of the ring system.
authors.affiliation: Department of Medicinal and Toxicological Chemistry, University of Sassari, Via Muroni 23/a, 07100 Sassari, Italy. acarta@uniss.it
authors.forename: Antonio
authors.initials: A
authors.lastname: Carta
authors.forename: Michele
authors.initials: M
authors.lastname: Palomba
authors.forename: Irene
authors.initials: I
authors.lastname: Briguglio
authors.forename: Paola
authors.initials: P
authors.lastname: Corona
authors.forename: Sandra
authors.initials: S
authors.lastname: Piras
authors.forename: Daniela
authors.initials: D
authors.lastname: Jabes
authors.forename: Paola
authors.initials: P
authors.lastname: Guglierame
authors.forename: Paola
authors.initials: P
authors.lastname: Molicotti
authors.forename: Stefania
authors.initials: S
authors.lastname: Zanetti
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002175:Candida / Q000187:drug effects; D045744:Cell Line, Tumor; D006801:Humans; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000900:Anti-Bacterial Agents; D015363:Quinolones