新型苯丙烯酰氨基酸化合物的设计合成及生物活性
收稿日期: 2018-12-19
修回日期: 2019-02-02
网络出版日期: 2019-04-08
基金资助
十二五国家科技重大专项（No.2012ZX09401-006）资助项目.
Synthesis and Biological Evaluation of Novel Phenylpropenoyl-amino Acid Derivatives
Received date: 2018-12-19
Revised date: 2019-02-02
Online published: 2019-04-08
Supported by
Project supported by the National Science and Technology Major Project in 12th Five-Year (No. 2012ZX09401-006).
高粟繁 , 张艳春 , 李家明 , 张斌 , 杨雨 , 胡孟奇 . 新型苯丙烯酰氨基酸化合物的设计合成及生物活性[J]. 有机化学, 2019 , 39(7) : 1953 -1961 . DOI: 10.6023/cjoc201812037
Based on the listed drug rebamipide, a series of novel compounds of phenylpropenoyl-amino acid structures were designed and synthesized according to the pharmacophore-combination strategy. The structures of the target compounds were confirmed by NMR and MS. The inhibitory activities against IL-6 and TNF-α had been investigated. The results demonstrated that all compounds exhibited moderate IL-6 and TNF-α inhibitory activities. In particular, the activities of four compounds were significantly improved than that of rebamipide.
Key words： IL-6; TNF-α; phenylpropenoyl-amino acid; synthesis
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