Letters in Drug Design & Discovery

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


Synthesis and Biological Evaluations of Novel Nitric Oxide-donating Derivatives of [1,2,4]triazol-5(4H)-one with N-phenylpyrrolyl-2-tetrazole Moiety as Anti-hypertension Candidates


Graphical Abstract:


By coupling nitric oxide (NO)-donating moieties with ATPT, an orally active AT1 receptor antagonist, a series of novel NO-releasing derivatives with N-phenylpyrrolyl-2-tetrazole moiety were designed and synthesized. The NOreleasing assay indicated that compound 4c had good maximum amount of NO release. Moreover the target compounds were evaluated for their antagonism of AT1 receptor with induced contraction in the rat thoracic aortic ring, and the results showed that compound 4c exhibited potent antagonistic activity of AT1 receptor, which was obviously superior to that of the control drug losartan. These results suggested that NO-donor ATPT hybrids may provide a promising approach for the search for novel antihypertensive agents.

Keywords: AT1 antagonist, anti-hypertension, ATPT, nitric oxide-donating.

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Article Details

Year: 2015
Page: [206 - 210]
Pages: 5
DOI: 10.2174/1570180811666141009235816
Price: $58