Design, synthesis, and biological evaluation of 1, 2, 4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates

…, H Zhang, R Bai, H Yao, J Jiang, M Shen, X Wu…

文献索引：Liu, Jie; Liu, Qin; Yang, Xue; Xu, Shengtao; Zhang, Hengyuan; Bai, Renren; Yao, Hequan; Jiang, Jieyun; Shen, Mingqin; Wu, Xiaoming; Xu, Jinyi Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 24 p. 7742 - 7751

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被引用次数: 6

摘要

Abstract A series of novel 1, 2, 4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives were designed and synthesized to develop new angiotensin II subtype 2 (AT 2) receptor agonists as novel antihypertensive candidates. It was found that 14f (IC 50= 0.4 nM) and 15e (IC 50= 5.0 nM) displayed potent AT 2 receptor affinity and selectivity in binding assays. Biological evaluation in vivo suggested that 14f is obviously superior to that of ...