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. 2012 Sep;8(5):928-33. doi: 10.2174/157340612802084243.
A series of novel Ligustrazinyl acylguanidines was designed, synthesized and evaluated for their protective effect on injured vascular endothelial cell (ECV-304). The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured endothelial cell. Among the active compounds, compounds 8b, 8f and 8l displayed remarkable antioxidative activity with low EC(50) values of 0.097, 0.059 and 0.094 mM, respectively. Structure-activity relationships were briefly discussed.
设计、合成了一系列新型川芎嗪酰基胍类化合物，并评价了它们对血管内皮细胞（ECV-304）损伤的保护作用。初步结果表明，一些化合物在刺激损伤内皮细胞增殖方面比川芎嗪具有更强的活性。在活性化合物中，化合物 8b、8f 和 8l 表现出显著的抗氧化活性，其 EC50 值分别为 0.097、0.059 和 0.094mM。讨论了构效关系。
