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ID: ALA1147932

Journal: Bioorg Med Chem

Title: Design, synthesis, and biological activities of novel Ligustrazine derivatives.

Authors: Cheng XC, Liu XY, Xu WF, Guo XL, Ou Y.

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.

CiteXplore: 17383884

DOI: 10.1016/j.bmc.2007.03.033