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1-取代喹喔啉-2,3(1H,4H)-二酮的体外抗结核和抗菌活性。

In vitro antitubercular and antimicrobial activities of 1-substituted quinoxaline-2,3(1H,4H)-diones.

机构信息

Raghavendra Institute of Pharmaceutical Education and Research, Anantapur, Andhra Pradesh 515 721, India.

出版信息

Bioorg Med Chem Lett. 2010 Jan 1;20(1):406-8. doi: 10.1016/j.bmcl.2009.10.026. Epub 2009 Oct 12.

Abstract

1-((Substituted)methyl)quinoxaline-2,3(1H,4H)-dione (2a-e) and 1-((substituted)acryloyl)quinoxaline-2,3(1H,4H)-dione (4a-c) were synthesized from quinoxaline-2,3(1H,4H)-dione 1 and evaluated for their antimicrobial activities. Results of the antitubercular screening against Mycobacterium tuberculosis H(37)Rv showed that the compounds 2b,3, and 4a were the most effective, with minimum inhibitory concentrations of 8.012, 8.561, and 8.928microg/ml, respectively. All the compounds exhibited significant antibacterial and considerable antifungal activities.

摘要

1-((取代)甲基)喹喔啉-2,3(1H,4H)-二酮(2a-e)和 1-((取代)丙烯酰基)喹喔啉-2,3(1H,4H)-二酮(4a-c)是由喹喔啉-2,3(1H,4H)-二酮 1 合成的,并对其进行了抗菌活性评价。对结核分枝杆菌 H(37)Rv 的抗结核筛选结果表明,化合物 2b、3 和 4a 最为有效,其最小抑菌浓度分别为 8.012、8.561 和 8.928μg/ml。所有化合物均表现出显著的抗菌活性和相当强的抗真菌活性。

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