title: Ligustrazine derivatives. Part 6: design, synthesis and evaluation of novel ligustrazinyl acylguanidine derivatives as potential cardiovascular agents.
abstract: A series of novel Ligustrazinyl acylguanidines was designed, synthesized and evaluated for their protective effect on injured vascular endothelial cell (ECV-304). The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured endothelial cell. Among the active compounds, compounds 8b, 8f and 8l displayed remarkable antioxidative activity with low EC(50) values of 0.097, 0.059 and 0.094 mM, respectively. Structure-activity relationships were briefly discussed.
authors: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, China.
authors: Zhenyu
authors: Z
authors: Li
authors: Fang
authors: F
authors: Yu
authors: Lei
authors: L
authors: Cui
authors: Peng
authors: P
authors: Zhan
authors: Shouxun
authors: S
authors: Wang
authors: Yuemao
authors: Y
authors: Shen
authors: Xinyong
authors: X
authors: Liu
mesh_terms: D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology; D002317:Cardiovascular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D042783:Endothelial Cells / Q000187:drug effects / Q000473:pathology; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000975:Antioxidants; D002317:Cardiovascular Agents; D006146:Guanidines; D011719:Pyrazines; C017953:tetramethylpyrazine