Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect

…, H Zheng, X Yang, L Jia, C Wen, L Liang, J Tian…

文献索引：Nie, Yong-Yan; Da, Ya-Jing; Zheng, Hao; Yang, Xiao-Xia; Jia, Lin; Wen, Cai-Hong; Liang, Li-Sha; Tian, Juan; Chen, Zhi-Long Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 8 p. 2747 - 2761

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被引用次数: 8

摘要

A series of novel angiotensin II type 1 receptor antagonists were prepared. Radioligand binding assay suggested that compounds 1b and 1c could be recognized by the AT1 receptor with an IC50 value of 1.6±0.09 nM and 2.64±0.7 nM, respectively. In vivo anti- hypertension experiments showed that compounds (1a, 1b, 1c, 1e) elicited a significant decrease in SBP and DBP of spontaneous hypertensive rats (SHRs). The ...