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Synthesis of the novel liqustrazine derivatives and Their protective effect on injured vascular endothelial cell damaged by hydrogen peroxide.

作者信息

Liu Xinyong, Zhang Rui, Xu Wenfang, Li Chaowu, Zhao Quanqin, Wang Xingpo

机构信息

Institute of Medicinal Chemistry, School of Pharmacy, No. 44 Wenhuaxi Road, 250012, Jinan, China.

出版信息

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2123-6. doi: 10.1016/s0960-894x(03)00359-7.

DOI:10.1016/s0960-894x(03)00359-7
PMID:12798318
Abstract

A series of novel 2-acyloxymethyl-3,5,6-trimethylpyrazine derivatives was designed and synthesized. Most compounds were found to be 1.5-4.5-fold higher potency than tetramethylpyrazine (TMP) in stimulating the proliferation of normal vascular endothelial cells and in protecting against hyperoxic acute injury. The most active one is the 2-nicotinoyl ester 5a exhibiting the maximum proliferation rate (P(max)) of 88.57% at the concentration of 0.1 mmol L(-1). Structure-activity relationships of these compounds were discussed.

摘要

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