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新型 N-芳基脲 3,4-二氢嘧啶-2(1H)-酮脲衍生物的合成及抗炎、抗菌和抗真菌活性评价。

The novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of N-aryl urea: synthesis, anti-inflammatory, antibacterial and antifungal activity evaluation.

机构信息

Department of Chemistry, School of Chemical Sciences, Swami Ramanand Teerth University (SRTM), Nanded, India.

出版信息

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4648-51. doi: 10.1016/j.bmcl.2011.03.062. Epub 2011 Mar 21.

Abstract

A series of novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of biological interest were prepared by sequential Bigineli's reaction, reduction followed by reaction of resulting amines with different arylisocynates. All the synthesized (1-23) compounds were screened against the pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological activity evaluation study reveled that among all the compounds screened, compounds 12 and 17 found to have promising anti-inflammatory activity (68-62% TNF-α and 92-86% IL-6 inhibitory activity at 10 μM). Interestingly compounds 3, 4, 5, 6, 15, 22 and 23 revealed promising antimicrobial activity at MIC of 10-30 μg/mL against selected pathogenic bacteria and fungi.

摘要

一系列具有生物活性的新型 3,4-二氢嘧啶-2(1H)-酮脲衍生物通过连续的比格利尼反应、还原以及所得胺与不同的芳基异氰酸酯反应制备得到。所有合成的(1-23)化合物都针对促炎细胞因子(TNF-α 和 IL-6)和抗菌活性(抗菌和抗真菌)进行了筛选。生物活性评估研究表明,在所筛选的所有化合物中,化合物 12 和 17 表现出有前途的抗炎活性(在 10 μM 时对 TNF-α 的抑制率为 68-62%,对 IL-6 的抑制率为 92-86%)。有趣的是,化合物 3、4、5、6、15、22 和 23 在 MIC 为 10-30 μg/mL 时对选定的病原菌和真菌显示出有希望的抗菌活性。

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