Carta, Antonio and Palomba, Michele Francesco Luigi and Paglietti, Giuseppe and Molicotti, Paola and Paglietti, Bianca and Cannas, Sara and Zanetti, Stefania Anna Lucia (2007) [1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains. Bioorganic & Medicinal Chemistry Letters, Vol. 17 (17), p. 4791-4794. ISSN 0960-894X. Article.
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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 MIC90 in the range 0.5–3.2 μg/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC90 = 0.5 μg/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested.
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