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期刊论文
Synthesis of the Novel Liqustrazine Derivatives and Their Protective Effect on Injured Vascular Endothelial Cell Damaged by Hydrogen Peroxide
Bioorganic & Medicinal Chemistry Letters 13 (2003) 2123-2126,-0001,():
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 (Pmax) of 88.57% at the concentration of 0.1 mmol L1. Structure-activity relationships of these compounds were discussed.
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