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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, an aspartic protease, is an important component of the renin-angiotensin-aldosterone system (RAAS) and is also a key substance in maintaining vascular function and normotensive blood pressure. Blocking this pathway by inhibiting renin and thereby blocking this pathway upstream of RAAS is of great importance for the treatment of hypertension and the development of new antihypertensives. At present, major pharmaceutical companies are developing various new and effective oral inhibitory renin Agent. The structural remodeling, structure-activity relationship and clinical application of non-peptide renin inhibitors with different structural skeletons are reviewed.