新型苯丙烯酰氨基酸化合物的设计合成及生物活性（英文）

Synthesis and Biological Evaluation of Novel Phenylpropenoyl-amino Acid Derivatives

依据药效团的拼合策略,以上市药瑞巴派特为先导化合物,设计并合成了一系列具有苯丙烯酰氨基酸结构化合物,其结构均经1H NMR、13C NMR和MS确证.用Elisa法测定目标化合物对LPS诱导的RAW264.7细胞释放IL-6和TNF-α的抑制活性.结果显示所设计化合物显示出良好的抑制活性,其中有4个化合物的活性明显优于瑞巴派特.

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-αhad been investigated.The results demonstrated that all compounds exhibited moderate IL-6 and TNF-αinhibitory activities.In particular,the activities of four compounds were significantly improved than that of rebamipide.