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

被引：55

作者：

Moreno, Elsa ^{[1
]}

Ancizu, Saioa ^{[1
]}

Perez-Silanes, Silvia ^{[1
]}

Torres, Enrique ^{[1
]}

Aldana, Ignacio ^{[1
]}

Monge, Antonio ^{[1
]}

机构：

[1] Univ Navarra, CIFA, Unidad Invest & Desarrollo Medicamentos, Pamplona 31008, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 10期

关键词：

Quinoxaline; N-oxides; Anti-tuberculosis agents; Mycobacterium tuberculosis; MYCOBACTERIUM-TUBERCULOSIS;

D O I：

10.1016/j.ejmech.2010.06.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As a continuation of our research and with the aim of obtaining new anti-tuberculosis agents which can improve the current chemotherapeutic anti-tuberculosis treatments, forty-three new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis strain H(37)Rv. Active compounds were also screened to assess toxicity to a VERO cell line. Results indicate that compounds with a methyl moiety substituted in position 3 and unsubstituted benzyl substituted on the carboxamide group provide an efficient approach for further development of anti-tuberculosis agents. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：4418 / 4426

页数：9

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