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新型喹喔啉-2-甲腈及喹喔啉-2-甲腈1,4-二氮氧化物衍生物的抗分枝杆菌活性

Antimycobacterial activity of new quinoxaline-2-carbonitrile and quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.

作者信息

Ortega M A, Montoya M E, Jaso A, Zarranz B, Tirapu I, Aldana I, Monge A

机构信息

Unidad de Investigación y Desarrollo de Nuevos Medicamentos, Facultad de Farmacia, CIFA, Universidad de Navarra, Pamplona, España.

出版信息

Pharmazie. 2001 Mar;56(3):205-7.

PMID:11265583
Abstract

The compounds being reported in this paper have all been evaluated within the TAACF Antituberculosis Screen Program, and some of them have been shown to possess high growth inhibition activity against Mycobacterium tuberculosis and Mycobacterium avium in the run of the first and second level in vitro screenings. The three compounds which have shown a good SI (Selectivity Index) are 2b, 4b and 4d; in addition, 6,7-dimethyl-3-[4-(4'-nitrophenyl)piperazinl-yl]quinoxaline-2-carbonitrilo 1,4-di-N-oxide (4b) is currently being tested within the in vivo antituberculosis screening in view of its very good in vitro activity.

摘要

本文报道的化合物均已在TAACF抗结核筛选项目中进行了评估，其中一些化合物在一级和二级体外筛选过程中显示出对结核分枝杆菌和鸟分枝杆菌具有高生长抑制活性。显示出良好选择性指数（SI）的三种化合物是2b、4b和4d；此外，鉴于6,7-二甲基-3-[4-(4'-硝基苯基)哌嗪基]喹喔啉-2-甲腈1,4-二-N-氧化物（4b）具有非常好的体外活性，目前正在进行体内抗结核筛选测试。

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