Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, China.
Med Chem. 2014;10(1):81-9. doi: 10.2174/157340641130900042.
A series of novel Ligustrazinyl amides was designed, synthesized and evaluated for their protective effect on the injured vascular endothelial cells. The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured human umbilical vascular endothelial cells (HUVECs) that is damaged by hydrogen peroxide. Among the active compounds, compounds 8i, 8t and 8u exhibited the highest potency with low EC₅₀ values of 0.037, 0.070 and 0.055 mM, respectively. Structure-activity relationships were briefly discussed.
一系列新型川芎嗪酰胺被设计、合成并评价其对受损血管内皮细胞的保护作用。初步结果表明，一些化合物在刺激过氧化氢损伤的人脐静脉内皮细胞（HUVEC）复制方面比川芎嗪具有更强的活性。在活性化合物中，化合物 8i、8t 和 8u 表现出最高的活性，EC₅₀ 值分别为 0.037、0.070 和 0.055 mM。简要讨论了构效关系。
