Design, synthesis, and biological activities of novel Ligustrazine derivatives

Bioorg Med Chem. 2007 May 15;15(10):3315-20. doi: 10.1016/j.bmc.2007.03.033.

Xian-Chao Cheng ¹, Xin-Yong Liu, Wen-Fang Xu, Xiu-Li Guo, Yang Ou

Affiliations

Affiliation

1 Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan 250012, China.

PMID: 17383884 DOI: 10.1016/j.bmc.2007.03.033

Abstract

A series of novel Ligustrazine derivatives was designed, synthesized, and assayed for their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities. The results showed that most Ligustrazine derivatives exhibited lower EC(50) values for protective effects on the ECV-304 cells damaged by hydrogen peroxide in comparison with Ligustrazine. And some Ligustrazine derivatives presented better antiplatelet aggregation activities than Ligustrazine. The derivatives containing the bisphenylmethyl pharmacophore (7a-c) exhibited highest potency. Compound 7a displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound 7c was found to be the most active antiplatelet aggregation agent. Structure-activity relationships were briefly discussed.

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