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  • Ligustrazine derivatives. Part 5: design, synthesis and biological evaluation of novel ligustrazinyloxy-cinnamic acid derivatives as potent cardiovascular agents.

Ligustrazine derivatives. Part 5: design, synthesis and biological evaluation of novel ligustrazinyloxy-cinnamic acid derivatives as potent cardiovascular agents.

European journal of medicinal chemistry (2011-10-14)
Hongfei Chen, Guoning Li, Peng Zhan, Xinyong Liu
ABSTRACT

A series of novel ligustrazinyloxy-cinnamic acid derivatives were designed, synthesized and evaluated for their inhibitory effect on adenosine diphosphate (ADP)-induced platelet aggregation in vitro, and also assayed for their protective effect against hydrogen peroxide (H(2)O(2))-induced oxidative damage on ECV-304 cells. Some compounds exhibited high activity in one or both of the assays, of which, compound 2e displayed the highest protective effect on the proliferation of the damaged ECV-304 cells (EC(50) = 0.020 mM), and compound 2f was the most active anti-platelet aggregation agent (EC(50) = 0.054 mM). Structure-activity relationships were briefly discussed.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
2,3,5,6-Tetramethylpyrazine, ≥98%, FG
Sigma-Aldrich
2,3,5,6-Tetramethylpyrazine, natural, ≥98%, FG
Sigma-Aldrich
2,3,5,6-Tetramethylpyrazine, 98%