SLOW, TIGHT-BINDING TO HUMAN RENIN OF SOME NONPEPTIDIC RENIN INHIBITORS CONTAINING A 4-METHOXYMETHOXYPIPERIDINYLAMIDE AT THE P4-POSITION

被引：4

作者：

STEIN, HH

FUNG, AKL

COHEN, J

BAKER, WR

ROSENBERG, SH

BOYD, SA

DAYTON, BD

ARMIGER, YLST

CONDON, SL

MANTEI, RA

KLEINERT, HD

机构：

[1] Abbott Laboratories, Cardiovascular Research Division, Abbott Park

来源：

FEBS LETTERS | 1992年 / 300卷 / 03期

关键词：

HUMAN RENIN; ENZYME INHIBITION; SLOW BINDING;

D O I：

10.1016/0014-5793(92)80867-G

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of nonpeptidic human renin inhibitors with a 4-methoxymethoxypiperidinylamide at the P4 position of the molecule exhibited slow tight binding to the enzyme. Replacement of the methoxymethoxy moiety on the piperidine ring with H, OH, methoxyethyl, propyloxy or n-butyl eliminated the effect. The inhibition was partially reversed by prolonged dialysis at 4-degrees-C, arguing against formation of a covalent bond in the tightened complex.

引用

页码：301 / 304

页数：4

共 13 条

[1]

BAKER WR, 1992, IN PRESS J MED CHEM

[2]

BANGHAM DR, 1975, CLIN SCI MOL MED, V48, pS135

[3]

BOYD SA, 1991, APR AM CHEM SOC M AT

[4] KINETICS OF SLOW, TIGHT-BINDING INHIBITORS OF ANGIOTENSIN CONVERTING ENZYME [J].