Synthesis and anti-elastase properties of 6-amino-2-phenyl-4H-3,1-benzoxazin-4-one aminoacyl and dipeptidyl derivatives

被引：26

作者：

Colson, E ^{[1
]}

Wallach, J ^{[1
]}

Hauteville, M ^{[1
]}

机构：

[1] Univ Lyon 1, Lab Biochim Analyt & Synth Bioorgan, F-69622 Villeurbanne, France

来源：

BIOCHIMIE | 2005年 / 87卷 / 02期

关键词：

human leukocyte elastase inhibitor; benzoxazinones; 6-amino-2-phenyl-4H-3,1-benzoxazin-4-one aminoacyl derivatives; 6-amino-2-phenyl-4H3,1-benzoxazin-4-one dipeptidyl derivatives;

D O I：

10.1016/j.biochi.2004.10.015

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 6-amino-2-phenyl-4H-3,1-benzoxazin-4-one aminoacyl and dipeptidyl derivatives, in which aminoacids and dipeptides are linked to the benzoxazinone moiety via an amide bond, were synthesized and tested in vitro for their inhibitory activity towards human leukocyte elastase (HLE). When compared to their values without inhibitors, the residual enzymatic activities decrease with time, indicating a time-dependent inhibition. The most potent inhibitions were obtained when Z-Arg-(Pmc), Z-Val-Phe. Z-Ala-Val or Z-Val-Ala are linked to the 6-amino group. Twenty-five new compounds were synthesized. (c) 2004 Elsevier SAS. All rights reserved.

引用

页码：223 / 230

页数：8

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