文献类型：期刊文献

英文题名：Synthesis, Preliminary Bioevaluation and Computational Analysis of Caffeic Acid Analogues

作者：Liu, Zhiqian[1];Fu, Jianjun[2];Shan, Lei[1];Sun, Qingyan[1];Zhang, Weidong[1]

机构：[1]Second Mil Med Univ, Dept Phytochem, Sch Pharm, Shanghai 200433, Peoples R China;[2]E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

年份：2014

卷号：15

期号：5

起止页码：8808

外文期刊名：INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000336841800100)】；

基金：The work was supported by programfor New Century Excellent Talents in University Foundation, National Natural Science Foundation of China (81230090), partially supported by Global Research Network for Medicinal Plants (GRNMP) and King Saud University, Shanghai Leading Academic Discipline Project (B906), Key laboratory of drug research for special environments, PLA, Shanghai Engineering Research Center for the Preparation of Bioactive Natural Products (10DZ2251300), the Scientific Foundation of Shanghai China (12401900801,09DZ1975700, 09DZ1971500, 10DZ1971700), National Major Project of China (2011ZX09307-002-03), and National Key Technology R&D Program of China (2012BAI29B06).

语种：英文

外文关键词：anti-inflammatory; caffeic acid amides; synthesis; pharmacophore; target predication

摘要：A series of caffeic acid amides were designed, synthesized and evaluated for anti-inflammatory activity. Most of them exhibited promising anti-inflammatory activity against nitric oxide (NO) generation in murine macrophage RAW264.7 cells. A 3D pharmacophore model was created based on the biological results for further structural optimization. Moreover, predication of the potential targets was also carried out by the PharmMapper server. These amide analogues represent a promising class of anti-inflammatory scaffold for further exploration and target identification.