具有抗高血压活性的6-苯并恶唑苯并咪唑衍生物的设计、合成及生物学评价
Design, Synthesis, and Biological Evaluation of 6-Benzoxazole Benzimidazole Derivatives with Antihypertension Activities.
作者信息
Wu Zhuo, Bao Xiao-Lu, Zhu Wei-Bo, Wang Yan-Hui, Phuong Anh Nguyen Thi, Wu Xiao-Feng, Yan Yi-Jia, Chen Zhi-Long
机构信息
Department of Pharmaceutical Science and Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
Shanghai Xianhui Pharmaceutical Co., Ltd., Shanghai 200433, China.
出版信息
ACS Med Chem Lett. 2018 Dec 31;10(1):40-43. doi: 10.1021/acsmedchemlett.8b00335. eCollection 2019 Jan 10.
Abstract
A series of new angiotensin II receptor 1 antagonists were prepared. They displayed nanomolar affinity to AT receptor and could decrease blood pressure efficiently in spontaneously hypertensive rats. Among them, compounds and could reduce the blood pressure with more or equal potency compared to Losartan. So, compounds and could be considered as potential antihypertension drug candidates.
摘要
制备了一系列新型血管紧张素II受体1拮抗剂。它们对AT受体表现出纳摩尔级亲和力，并且能够在自发性高血压大鼠中有效降低血压。其中，化合物 和 与氯沙坦相比，能够以相同或更强的效力降低血压。因此，化合物 和 可被视为潜在的抗高血压药物候选物。
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