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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 12期

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

页码：3699 / 3703

页数：5

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