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Newly synthesized 6-benzoxazole benzimidazole derivatives, specifically compounds 1b and 2b, act as potent angiotensin II receptor 1 antagonists and reduce blood pressure in spontaneously hypertensive rats with efficacy equal to or greater than Losartan. Novelty: ClaimNovelty.NOVEL_FINDING. Consensus alignment: ConsensusAlignment.NEUTRAL.

December 31, 2018

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

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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.

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Authors

Zhuo Wu

Fudan University

Xiaolu Bao

Shanghai Ninth People's Hospital

Weibo Zhu

Donghua University

Journals

ACS Medicinal Chemistry Letters

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Donghua University

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

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Abstract

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