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

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。

Abstract: 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.