Title: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
Volume: 12
Issue: 3
Author(s): Yanchun Zhanga, Jichao Chen, Jinyi Xub*, Jinpei Zhou and Xiaoming Wu*
Affiliation:
- bDepartment of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China
- Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China
Keywords:
AT1 antagonist, anti-hypertension, ATPT, nitric oxide-donating.
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.
