Synthesis and evaluation of azaproline peptides as potential inhibitors of dipeptidyl peptidase IV and prolyl oligopeptidase

被引：11

作者：

Borloo, M ^{[1
]}

Augustyns, K ^{[1
]}

Belyaev, A ^{[1
]}

deMeester, I ^{[1
]}

Lambeir, AM ^{[1
]}

Goossens, F ^{[1
]}

Bollaert, W ^{[1
]}

Rajan, P ^{[1
]}

Scharpe, S ^{[1
]}

Haemers, A ^{[1
]}

机构：

[1] UNIV ANTWERP,DEPT PHARMACEUT SCI,B-2610 ANTWERP,BELGIUM

来源：

LETTERS IN PEPTIDE SCIENCE | 1995年 / 2卷 / 3-4期

关键词：

azapeptides; N-acylcarbazates; N-acylsemicarbazides; N-acyl-N'-sulphonylhydrazines; N; N'-diacylhydrazines; pyrazolidines;

D O I：

10.1007/BF00119152

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 azaproline dipeptides with various N-substituents were synthesized as possible active-site-directed inhibitors of two proline-specific serine proteases, dipeptidyl peptidase IV and prolyl oligopeptidase. Compounds with semicarbazide, carbazate, acylhydrazine and sulphonylhydrazine structures were tested. Some compounds show moderate activity, i.e., in the millimolar range.

引用

页码：198 / 202

页数：5

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