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Design, Synthesis, and Biological Evaluation of 6-Benzoxazole Benzimidazole Derivatives with Antihypertension Activities.

ABSTRACT: A series of new angiotensin II receptor 1 antagonists were prepared. They displayed nanomolar affinity to AT1 receptor and could decrease blood pressure efficiently in spontaneously hypertensive rats. Among them, compounds 1b and 2b could reduce the blood pressure with more or equal potency compared to Losartan. So, compounds 1b and 2b could be considered as potential antihypertension drug candidates.

SUBMITTER: Wu Z 

PROVIDER: S-EPMC6331155 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Biological Evaluation of 6-Benzoxazole Benzimidazole Derivatives with Antihypertension Activities.

Wu Zhuo Z   Bao Xiao-Lu XL   Zhu Wei-Bo WB   Wang Yan-Hui YH   Phuong Anh Nguyen Thi NT   Wu Xiao-Feng XF   Yan Yi-Jia YJ   Chen Zhi-Long ZL  

ACS medicinal chemistry letters 20181231 1

A series of new angiotensin II receptor 1 antagonists were prepared. They displayed nanomolar affinity to AT<sub>1</sub> receptor and could decrease blood pressure efficiently in spontaneously hypertensive rats. Among them, compounds <b>1b</b> and <b>2b</b> could reduce the blood pressure with more or equal potency compared to Losartan. So, compounds <b>1b</b> and <b>2b</b> could be considered as potential antihypertension drug candidates. ...[more]

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