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新型喹喔啉-2-甲酰胺 1,4-二-N-氧化物衍生物的合成及抗分枝杆菌活性。

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

机构信息

Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, C/ Irunlarrea s/n, 31008 Pamplona, Spain.

出版信息

Eur J Med Chem. 2010 Oct;45(10):4418-26. doi: 10.1016/j.ejmech.2010.06.036. Epub 2010 Jul 3.

Abstract

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.

摘要

作为我们研究的延续,旨在获得新的抗结核药物,以改善当前的抗结核化疗,我们合成了 43 种新型的喹喔啉-2-甲酰胺 1,4-二-N-氧化物衍生物,并对其进行了体外抗结核活性评估,针对结核分枝杆菌 H(37)Rv 株。还对活性化合物进行了筛选,以评估其对 VERO 细胞系的毒性。结果表明,在 3 位取代甲基和在羧酰胺基团上未取代的苄基的化合物为进一步开发抗结核药物提供了一种有效的方法。

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