Ligustrazine derivatives. Part 3: Design, synthesis and evaluation of novel acylpiperazinyl derivatives as potential cerebrocardiac vascular agents

Xian-Chao Cheng; Xin-Yong Liu; Wen-Fang Xu; Xiu-Li Guo; Ning Zhang; Yu-Ning Song

doi:10.1016/j.bmc.2009.03.012

Ligustrazine derivatives. Part 3: Design, synthesis and evaluation of novel acylpiperazinyl derivatives as potential cerebrocardiac vascular agents

Bioorg Med Chem. 2009 Apr 15;17(8):3018-24. doi: 10.1016/j.bmc.2009.03.012. Epub 2009 Mar 13.

Authors

Xian-Chao Cheng¹, Xin-Yong Liu, Wen-Fang Xu, Xiu-Li Guo, Ning Zhang, Yu-Ning Song

Affiliation

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

PMID: 19329327
DOI: 10.1016/j.bmc.2009.03.012

Abstract

A series of novel acylpiperazinyl Ligustrazine derivatives was designed, synthesized, and their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities were evaluated. The results showed that compound E33 displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound E1 was found to be the most active antiplatelet aggregation agent. Structure-activity relationships were briefly discussed.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cells, Cultured
Drug Design
Endothelial Cells / drug effects
Humans
Inhibitory Concentration 50
Platelet Aggregation Inhibitors / chemical synthesis*
Platelet Aggregation Inhibitors / pharmacology*
Pyrazines / chemical synthesis*
Pyrazines / pharmacology*
Structure-Activity Relationship

Substances

Platelet Aggregation Inhibitors
Pyrazines
tetramethylpyrazine