Synthesis and Biological Study of 3-Butyl-1-(2,6-dichlorophenyl)-1H-[1,2,4]triazol-5(4H)-one Derivatives as Anti-hypertension Drugs

被引：7
|
作者：
Zhang, Yanchun [1 ]
Zhou, Jinpei [1 ]
Pan, Weihong [1 ]
Wu, Xiaoming [1 ]
Wang, Shuai [1 ]
机构：
[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 01期
关键词：
AT1; antagonist; Nitric oxide-donating; Anti-hypertension; Synthesis; NITRIC-OXIDE; ANGIOTENSIN-II; PHARMACODYNAMIC HYBRIDS; DONOR;
D O I：
10.2174/157018010789869370
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of nitric oxide-donating derivatives of [1,2,4]triazol-5(4H)-one (9a-f and 15a-f) as a novel class of angiotensin II receptor AT1 antagonists have been designed and synthesized by coupling furoxan and nitric oxide with lead compound 1. The synthesized compounds were evaluated for their antagonism of AT1 receptor with induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9b, 15b and 15d exhibited potent antagonistic activity of AT1 receptor. Moreover 9b, 15b, 15d, 15e had good maximum NO release amount of this series.
引用
收藏
页码：18 / 22
页数：5
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