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

阅读量:

25

作者:

CH HassallA KröhnCJ MoodyWA Thomas

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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.

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DOI:

10.1016/0014-5793(82)81036-3

被引量:

187

年份:

1982

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来源期刊

Febs Letters
1982/10/18

引用走势

1990
被引量:19

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