摘要/Abstract

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.
关键词: IL-6, TNF-α, 苯丙烯酰氨基酸, 合成
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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