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 0.5–3.2lg/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC 90=0.5lg/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested.
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains / Carta, Antonio; Palomba, Michele Francesco Luigi; Paglietti, G; Molicotti, Paola; Paglietti, B; Cannas, Sara; Zanetti, Stefania Anna Lucia. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 17:(2007), pp. 4791-4794. [10.1016/j.bmcl.2007.06.064]
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains
CARTA, Antonio;PALOMBA, Michele Francesco Luigi;MOLICOTTI, Paola;PAGLIETTI B;CANNAS, Sara;ZANETTI, Stefania Anna Lucia
2007-01-01
Abstract
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 0.5–3.2lg/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC 90=0.5lg/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
