ALPHA-MERCAPTOACYL DIPEPTIDES THAT INHIBIT ANGIOTENSIN-CONVERTING ENZYME AND NEUTRAL ENDOPEPTIDASE-24.11

被引：11

作者：

BHAGWAT, SS

FINK, CA

GUDE, C

CHAN, K

QIAO, Y

SAKANE, Y

BERRY, C

GHAI, RD

机构：

[1] Research Department, Pharmaceuticals Division, Ciba-Geigy Corporation, Summit, NJ 07901

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 07期

关键词：

D O I：

10.1016/0960-894X(95)00105-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

alpha-Mercaptoacyl dipeptides were prepared and found to inhibit angiotensin converting enzyme (ACE) and neutral endopeptidase 24.11 (NEP). Compounds with a proline as the C-terminal amino acid, and possessing the S-stereochemistry at the thiol bearing carbon were preferred for optimal ACE inhibition while, R-stereochemistry was preferred for optimal NEP inhibition. Compounds containing alternative amino acid residues at the C-terminal position displayed optimal dual ACE/NEP inhibition when the stereochemistry was 'S' at this carbon atom.

引用

页码：735 / 738

页数：4

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