title: Ligustrazine derivatives. Part 8: design, synthesis, and preliminary biological evaluation of novel Ligustrazinyl amides as cardiovascular agents.
abstract: A series of novel Ligustrazinyl amides was designed, synthesized and evaluated for their protective effect on the injured vascular endothelial cells. The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured human umbilical vascular endothelial cells (HUVECs) that is damaged by hydrogen peroxide. Among the active compounds, compounds 8i, 8t and 8u exhibited the highest potency with low EC₅₀ values of 0.037, 0.070 and 0.055 mM, respectively. Structure-activity relationships were briefly discussed.
authors.forename: Zhenyu
authors.initials: Z
authors.lastname: Li
authors.forename: Fang
authors.initials: F
authors.lastname: Yu
authors.forename: Lei
authors.initials: L
authors.lastname: Cui
authors.forename: Wenmin
authors.initials: W
authors.lastname: Chen
authors.forename: Shouxun
authors.initials: S
authors.lastname: Wang
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.forename: Yuemao
authors.initials: Y
authors.lastname: Shen
authors.affiliation: 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. xinyongl@sdu.edu.cn.
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002317:Cardiovascular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D015195:Drug Design; D042783:Endothelial Cells / Q000187:drug effects*; D006801:Humans; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D002317:Cardiovascular Agents; D011719:Pyrazines; C017953:tetramethylpyrazine