膦肽类化合物对血管紧张素转化酶的体外抑制活性及构效关系  

IN VITRO INHIBITIVE ACTIVITY OF PHOSPHONOTRIPEPTIDES TOWARD ANGIOTENSIN- CONVEKTING ENZYME AND STUDY ON STRUCTURE- ACTIVITY RELATIONSHIP

作　　者：陈何如[1] 徐杰诚[1] 

机构地区：[1]中国科学院上海有机化学研究所,广东汕头大学化学系

出　　处：《药学学报》1996年第9期666-670,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：设计与合成了一系列膦三肽化合物。测定化合物对血管紧张素转化酶的体外抑制活性。结果表明，有些化合物的体外抑制活性已接近ｃａｐｔｏｐｒｉｌ的水平。在此基础上，探讨抑制剂的结构与抑制活性之间的关系。A series of phosphonotripeptides were synthesized according to structure-basedrational drug design. The in vitro inhibitive activi ties of these compounds toward angiotensin-converting enzyme were detennined.The in vitro activities of some of these compounds were shownto be comparable with that of Captopril.Furthennore,the structure.activity relationship(SAR)ofthese compounds was discussed。

关 键 词：降压药 膦三肽 ACE抑制剂 合成 构效 

分 类 号：TQ463.6[化学工程—制药化工] R972.4[医药卫生—药品]