Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives

被引：102
|
作者：
Zarranz, B [1 ]
Jaso, A [1 ]
Aldana, I [1 ]
Monge, A [1 ]
机构：
[1] Univ Navarra, Unidad Invest & Desarrollo Medicamentos, Ctr Invest Farmacobiol Aplicada, E-31080 Pamplona, Spain
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 10期
关键词：
D O I：
10.1016/S0968-0896(03)00119-6
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
As a continuation of our research and with the aim of obtaining new antituberculosis agents which can improve the current chemotherapeutic antituberculosis treatments, new series of quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis strain H(37)Rv, using the radiometric BACTEC 460-TB methodology. Active compounds were also screened by serial dilution to assess toxicity to a VERO cell line. The results indicate that some compounds exhibited a good antituberculosis activity and the arylearboxamide analogues 3, 8, and 9 were the most active compounds (EC90/MICI). Also, the cytotoxic effects indicate that these compounds have a good Selectivity Index (SI). (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2149 / 2156
页数：8
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