title: [1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
abstract: In this preliminary study we report the activity of 3-methyl-9-substituted-6-oxo-6,9-dihydro-3H-[1,2,3]-triazolo[4,5-h]quinolone-carboxylic acids and their esters as a new class of antiinfective agents against MDR Mycobacterium tuberculosis. In antitubercular screening against H37Rv and 11 clinically isolated strains of M. tuberculosis several derivatives (1o,3a,c,i,j,p) showed MIC(90) in the range 0.5-3.2 microg/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC(90)=0.5 microg/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested.
authors.affiliation: Dipartimento Farmaco Chimico Tossicologico, Università degli Studi di 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: Giuseppe
authors.initials: G
authors.lastname: Paglietti
authors.forename: Paola
authors.initials: P
authors.lastname: Molicotti
authors.forename: Bianca
authors.initials: B
authors.lastname: Paglietti
authors.forename: Sara
authors.initials: S
authors.lastname: Cannas
authors.forename: Stefania
authors.initials: S
authors.lastname: Zanetti
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D024881:Drug Resistance, Bacterial; D018432:Drug Resistance, Multiple; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D009169:Mycobacterium tuberculosis / Q000378:metabolism*; D015363:Quinolones / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy*
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D015363:Quinolones; D014230:Triazoles