非肽类肾素抑制剂的研究进展

Research Progress of Nonpeptide Renin Inhibitors

肾素为一种天冬氨酸蛋白酶,是肾素-血管紧张素-醛固酮系统(RAAS)的重要组成部分,也是维持血管功能和正常血压的关键物质。通过抑制肾素从而在RAAS的上游阻断该通路对于高血压的治疗以及新的抗高血压药物的开发具有非常重要的意义,目前各大制药公司正在研发各种新型的口服有效的肾素抑制剂。综述具有不同结构骨架的非肽类肾素抑制剂的结构改造、构效关系和临床应用研究进展。

Renin, as an aspartic protease, is an important part of renin-angiotensin-aldosterone system （ RAAS）, and is the key material to maintain vascular function and normal blood pressure. Blocking the pathway of RAAS upstream by inhibition of renin for the treatment of hypertension and the development of new antihypertensive drugs has very important significance. The major pharmaceutical companies in the world are currently developing a variety of novel orally potent renin inhibitors. This review summarizes progress in researches on the structural optimization, structure-activity relationship and clinical applications of a variety of non-peptide renin inhibitors possessing different structural skeletons.