降压新药血管紧张素Ⅱ受体拮抗剂的研究  

Study on angiotensin Ⅱ receptor antagonists as a new type of antihypertensive drug

作　　者：乜永艳[1] 李福民[1] 郑皓[1] 陈志龙[1] 

机构地区：[1]东华大学化学与生物学院生物医药研究室,上海201600

出　　处：《中国新药杂志》2012年第3期273-282,共10页Chinese Journal of New Drugs

摘　　要：高血压会严重损害心脏、大脑和肾脏等靶器官。血管紧张素Ⅱ受体拮抗剂(angiotensinⅡre-ceptor blockers,ARB)是继血管紧张素转换酶抑制剂(angiotension converting enzyme inhibitors,ACEI)后发展起来的一类新型降压药,其降压作用显著,效果持久,能够逆转高血压引起的靶器官损害,并有效降低心血管疾病发生的几率,每天服用一次可以24 h良好控制血压。此外,它克服了ACEI具有的致咳、血管性水肿等不良反应,是目前临床应用的一线降压药。本文对近年来文献报道的活性较高的ARB进行了介绍,并对其分子设计和构效关系进行了阐述,同时介绍了计算机辅助设计在该类药物研发中的应用。Hypertension is a major risk factor for human morbidity and mortality through its effects on target organs like heart, brain and kidneys. Angiotensin Ⅱ receptor blockers are a new type of antihypertensive drugs developed after ACEI, which can depress blood pressure, prevent and reverse the target organ injury induced by hypertension, reduce the risk caused by cardiovascular disease, and control blood pressure effectively for 24 hours when administered once a day. There is no adverse effects such as cough and angioedema which are associated with ACEI. Angiotensin Ⅱ receptor antagonists have been commonly used as first line antihypertensive drugs in clinical practice. This article introduces the active angiotensin Ⅱ receptor blockers which were reported by literatures. In addition, their molecular design and structure-activity relationship are described. Moreover, the application of the computer aided design on the development of angiotensin Ⅱ receptor blockers is also presented.

关 键 词：血管紧张素Ⅱ受体拮抗剂 高血压 构效关系 计算机辅助药物设计 

分 类 号：R972.4[医药卫生—药品]