Medicinal Chemistry 2012-09-01

Ligustrazine derivatives. Part 6: design, synthesis and evaluation of novel ligustrazinyl acylguanidine derivatives as potential cardiovascular agents.

Zhenyu Li, Fang Yu, Lei Cui, Peng Zhan, Shouxun Wang, Yuemao Shen, Xinyong Liu

Index: Med. Chem. 8(5) , 928-33, (2012)

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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.