Carta Antonio, Palomba Michele, Paglietti Giuseppe, Molicotti Paola, Paglietti Bianca, Cannas Sara, Zanetti Stefania
Dipartimento Farmaco Chimico Tossicologico, Università degli Studi di Sassari, Via Muroni 23/a, 07100, Sassari, Italy.
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4791-4. doi: 10.1016/j.bmcl.2007.06.064. Epub 2007 Jun 26.
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.
在这项初步研究中，我们报告了3-甲基-9-取代-6-氧代-6,9-二氢-3H-[1,2,3]-三唑并[4,5-h]喹诺酮羧酸及其酯作为一类新型抗感染剂对耐多药结核分枝杆菌的活性。在针对H37Rv和11株临床分离的结核分枝杆菌菌株的抗结核筛选中，几种衍生物（1o、3a、c、i、j、p）的最低抑菌浓度（MIC）（90）在0.5-3.2微克/毫升范围内。3c没有细胞毒性，并且被证明是最有效的衍生物，对所有测试的结核分枝杆菌菌株和受感染的人类巨噬细胞（J774-A1）的MIC（90）=0.5微克/毫升。
