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Eur J Med Chem. 2011 Nov;46(11):5609-15. doi: 10.1016/j.ejmech.2011.09.030. Epub 2011 Sep 29.

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

Author information

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

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.

PMID:
21993151
DOI:
10.1016/j.ejmech.2011.09.030
[Indexed for MEDLINE]

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