Issue 5, 2013
From the journal:

MedChemComm

Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents†

Hongfei Chen,a   Guoning Li,a   Peng Zhan,a   Xiuli Guo,b   Qian Ding,c   Shouxun Wangc  and  Xinyong Liu*a  

* Corresponding authors

a Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Educational Ministry of China), School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, China
E-mail: xinyongl@sdu.edu.cn

b Department of Pharmacology, School of Pharmaceutical Sciences, Shandong University, No. 44, Wenhuaxi Road, Jinan 250012, China

c Department of Biological Chemistry and Molecular Biology, School of Medicine, Weifang Medical University, No.7166, Baotongxi Road, Weifang 261053, China

Abstract

A series of novel ligustrazinylated derivatives was designed, synthesized and evaluated for their protective effects against hydrogen peroxide (H2O2)-induced oxidative damage on ECV-304 cells, and also assayed for their inhibition effects on platelet aggregation induced by adenosine diphosphate (ADP). Biological results showed that some compounds exhibited moderate to potent activities in one or both of the assays. Among these compounds, compound 3 displayed the highest protective effect on the damaged ECV-304 cells with EC50 = 0.0040 mM, and compound 1c was the most active platelet aggregation inhibitor (EC50 = 0.40 mM). Structure–activity relationships were briefly discussed.

Graphical abstract: Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents

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Article information

DOI
https://doi.org/10.1039/C3MD20352B
Article type
Concise Article
Submitted
22 Nov 2012
Accepted
10 Mar 2013
First published
11 Mar 2013

Med. Chem. Commun., 2013,4, 827-832

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Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents

H. Chen, G. Li, P. Zhan, X. Guo, Q. Ding, S. Wang and X. Liu, Med. Chem. Commun., 2013, 4, 827 DOI: 10.1039/C3MD20352B

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