title: Ligustrazine derivatives. Part 5: design, synthesis and biological evaluation of novel ligustrazinyloxy-cinnamic acid derivatives as potent cardiovascular agents.
abstract: A series of novel ligustrazinyloxy-cinnamic acid derivatives were designed, synthesized and evaluated for their inhibitory effect on adenosine diphosphate (ADP)-induced platelet aggregation in vitro, and also assayed for their protective effect against hydrogen peroxide (H(2)O(2))-induced oxidative damage on ECV-304 cells. Some compounds exhibited high activity in one or both of the assays, of which, compound 2e displayed the highest protective effect on the proliferation of the damaged ECV-304 cells (EC(50) = 0.020 mM), and compound 2f was the most active anti-platelet aggregation agent (EC(50) = 0.054 mM). Structure-activity relationships were briefly discussed.
authors: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No 44, Wenhuaxi Road, Jinan 250012, PR China.
authors: Hongfei
authors: H
authors: Chen
authors: Guoning
authors: G
authors: Li
authors: Peng
authors: P
authors: Zhan
authors: Xinyong
authors: X
authors: Liu
mesh_terms: D000818:Animals; D002317:Cardiovascular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D060326:Chemistry Techniques, Synthetic; D002934:Cinnamates / Q000737:chemistry*; D019610:Cytoprotection / Q000187:drug effects; D015195:Drug Design; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D002317:Cardiovascular Agents; D002934:Cinnamates; D011719:Pyrazines; C029010:cinnamic acid; C017953:tetramethylpyrazine