Title:Ligustrazine Derivatives. Part 6: Design, Synthesis and Evaluation of Novel Ligustrazinyl Acylguanidine Derivatives as Potential Cardiovascular Agents
VOLUME: 8 ISSUE: 5
Author(s):Zhenyu Li, Fang Yu, Lei Cui, Peng Zhan, Shouxun Wang, Yuemao Shen and Xinyong Liu
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.
Keywords:Ligustrazine, Acylguanidines, Synthesis, Cardiovascular disease, endothelial cell, CVDs, vasodilator, pharmacokinetics, anticoagulant agents, exchanger
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 EC50 values of 0.097,
0.059 and 0.094 mM, respectively. Structure-activity relationships were briefly discussed.
