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

Yanchun Zhang, Jinpei Zhou, Weihong Pan, Xiaoming Wu, Shuai Wang
2010 Letters in Drug Design & Discovery  
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.
more » ... AT1 receptor. Moreover 9b, 15b, 15d, 15e had good maximum NO release amount of this series.
doi:10.2174/157018010789869370 fatcat:py2zolvhrbegfcaf26w3xtxpae