[1,2,3]triazolo[4,5-h]quinolones.: A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains

被引：47
作者：
Carta, Antonio
Palomba, Michele
Paglietti, Giuseppe
Molicotti, Paola
Paglietti, Bianca
Cannas, Sara
Zanetti, Stefania
机构：
[1] Univ Sassari, Dipartimento Farmacochim Tossicol, I-07100 Sassari, Italy
[2] Univ Sassari, Dipartimento Sci Biomed, I-07100 Sassari, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 17期
关键词：
triazolo[4,5-h]quinolones; MDR M. tuberculosis; in vitro antitubercular activity;
D O I：
10.1016/j.bmcl.2007.06.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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-earboxylic 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 mu g/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC90 = 0.5 mu g/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested. (c) 2007 Elsevier Ltd. All rights reserved.
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收藏
页码：4791 / 4794
页数：4
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