The design of a new group of angiotensin‐converting enzyme inhibitors

FEBS Letters

Anthony Thomas, W.¹  Hassall, Cedric H.¹  Moody, Christopher J.¹  Kröhn, Antonin¹ 

[1] Roche Products Limited, Welwyn Garden City, Hertfordshire, England

关键词: Angiotensin-converting enzyme;    Inhibitors;    Design;    Antihypertensive;   

DOI  :  10.1016/0014-5793(82)81036-3

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Using X-ray and NMR data relating to the conformation of the antihypertensive, angiotensin-converting enzyme inhibitor, captopril, and structure—activity relationships of analogues, it has been possible to postulate with the aid of computer graphics, the orientation of the three functions, the thiol, the terminal carboxyl and the carbonyl group which are involved in binding to the enzyme. Bicyclic mimetics of captopril, with related arrays of these functions, have been designed and synthesized. Compounds with the closest approximation to the array in captopril are the most active inhibitors of angiotensin converting enzyme, in vitro.

【 授权许可】

Unknown