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

被引：0

作者：

Zhang, Yanchun ^{[1
]}

Chen, Jichao ^{[2
]}

Xu, Jinyi ^{[2
]}

Zhou, Jinpei ^{[2
]}

Wu, Xiaoming ^{[2
]}

机构：

[1] Anhui Univ Chinese Med, Dept Med Chem, Hefei 230001, Peoples R China

[2] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2015年 / 12卷 / 03期

关键词：

AT1; antagonist; anti-hypertension; ATPT; nitric oxide-donating; II RECEPTOR ANTAGONISTS; PHARMACODYNAMIC HYBRIDS; HYPERTENSION; DRUGS; RATS;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 NO-releasing 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.

引用

页码：206 / 210

页数：5

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