Synthesis of the novel liqustrazine derivatives and their protective effect on injured vascular endothelial cell damaged by hydrogen peroxide
Synthesis of the novel liqustrazine derivatives and their protective effect on injured vascular endothelial cell damaged by hydrogen peroxide
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DOI：
10.1016/s0960-894x(03)00359-7
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发表时间：
2003-07-07
影响因子：
2.7
通讯作者：
Wang, XP
中科院分区：
文献类型：
--
作者：
Liu, XY;Zhang, R;Wang, XP
设计并合成了一系列新型2-酰氧基甲基-3,5,6-三甲基吡嗪衍生物。大多数化合物在刺激正常血管内皮细胞增殖和防止高氧急性损伤方面的效力比四甲基吡嗪 (TMP) 高 1.5-4.5 倍。最活跃的是 2-烟酰酯 5a，在 0.1 mmol L-1 浓度下表现出最大增殖率 (P-max) 88.57%。讨论了这些化合物的构效关系。 (C) 2003 Elsevier Science Ltd. 保留所有权利。
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. (C) 2003 Elsevier Science Ltd. All rights reserved.