有机化学 ›› 2019, Vol. 39 ›› Issue (7): 1953-1961.DOI: 10.6023/cjoc201812037 上一篇    下一篇

研究论文

新型苯丙烯酰氨基酸化合物的设计合成及生物活性

高粟繁a,b, 张艳春a,b, 李家明a,b, 张斌a,b, 杨雨a,b, 胡孟奇a,b   

  1. a 安徽中医药大学药学院 合肥 230012;
    b 安徽省中医药科学院药物化学研究所 合肥 230012
  • 收稿日期:2018-12-19 修回日期:2019-02-02 出版日期:2019-07-25 发布日期:2019-04-08
  • 通讯作者: 李家明 E-mail:lijiaming2004@sina.com
  • 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

Gao Sufana,b, Zhang Yanchuna,b, Li Jiaminga,b, Zhang Bina,b, Yang Yua,b, Hu Mengqia,b   

  1. a College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012;
    b Deparment of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230012
  • Received:2018-12-19 Revised:2019-02-02 Online:2019-07-25 Published:2019-04-08
  • Contact: 10.6023/cjoc201812037 E-mail:lijiaming2004@sina.com
  • Supported by:

    Project supported by the National Science and Technology Major Project in 12th Five-Year (No. 2012ZX09401-006).

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