Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

Author(s): Yanchun Zhang, Jinpei Zhou, Weihong Pan, Xiaoming Wu, Shuai Wang.

Abstract:

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.

Keywords: AT1 antagonist, Nitric oxide-donating, Anti-hypertension, Synthesis

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Article Details

VOLUME: 7
ISSUE: 1
Year: 2010
Page: [18 - 22]
Pages: 5
DOI: 10.2174/157018010789869370