New 1,4-di-N-oxide-quinoxaline-2-ylmethylene isonicotinic acid hydrazide derivatives as anti-Mycobacterium tuberculosis agents

被引:74
|
作者
Torres, Enrique [1 ]
Moreno, Elsa [1 ]
Ancizu, Saioa [1 ]
Barea, Carlos [1 ]
Galiano, Silvia [1 ]
Aldana, Ignacio [1 ]
Monge, Antonio [1 ]
Perez-Silanes, Silvia [1 ]
机构
[1] Univ Navarra, Unidad Invest & Desarrollo Medicamentos, CIFA, Pamplona 31008, Spain
关键词
Anti-tuberculosis agents; Quinoxaline 1,4-di-N-oxide derivatives; Isoniazid; Microwave assisted synthesis; Druglikeness; QUINOXALINE 1,4-DI-N-OXIDE DERIVATIVES; IN-VITRO EVALUATION; ANTIMYCOBACTERIAL ACTIVITY; DESIGN; QUINOXALINE-2-CARBONITRILE; HYDRAZONES; SAR;
D O I
10.1016/j.bmcl.2011.04.072
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The increase in the prevalence of drug-resistant tuberculosis cases demonstrates the need of discovering new and promising compounds with antimycobacterial activity. As a continuation of our research and with the aim of identifying new antitubercular drugs candidates, a new series of quinoxaline 1,4-di-N-oxide derivatives containing isoniazid was synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain. Moreover, various drug-like properties of new compounds were predicted. Taking into account the biological results and the promising drug-likeness profile of these compounds, make them valid leads for further experimental research. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3699 / 3703
页数:5
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