Synthesis of new 2-acetyl and 2-benzoyl quinoxaline 1,4-di-N-oxide derivatives as anti-Mycobacterium tuberculosis agents

被引：106
|
作者：
Jaso, A [1 ]
Zarranz, B [1 ]
Aldana, I [1 ]
Monge, A [1 ]
机构：
[1] Univ Navarra, Ctr Invest Farmacobiol Aplicada, Unidad Invest & Desarrollo Medicamentos, Pamplona 31080, Spain
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 38卷 / 09期
关键词：
quinoxaline-1,4-dioxide; tuberculosis; anti-Mycobacterium;
D O I：
10.1016/S0223-5234(03)00137-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2-acetyl and 2-benzoyl-6(7)-substituted quinoxaline 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro antituberculosis activity. The results show that 2-acetyl-3-methylquinoxaline 1,4-di-N-oxide derivatives with chlorine, methyl or methoxy group in position 7 of the benzene moiety (compounds 2, 4 and 6, respectively) and unsubstituted (3) have good antitubercular activity, exhibiting EC90/MIC values between 0.80 and 4.29. In conclusion, the potency, selectivity and low cytotoxicity of these compounds make them valid leads for synthesizing new compounds that possess better activity. (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码：791 / 800
页数：10
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