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。
出处
《药学学报》
CAS
CSCD
北大核心
1996年第9期666-670,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
降压药
膦三肽
ACE抑制剂
合成
构效
Angiotensin-converting enzyme inhibitors
Hypertension drugs
Phosphono-tripeptides