STRUCTURAL FACTORS AFFECTING THE KINETICS OF O,N-ACYL TRANSFER IN POTENTIAL O-PEPTIDE PRODRUGS

被引：25

作者：

OLIYAI, R ^{[1
]}

STELLA, VJ ^{[1
]}

机构：

[1] UNIV KANSAS,DEPT PHARMACEUT CHEM,LAWRENCE,KS 66045

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00454-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the present study, the conversion kinetics of a number of O-peptide prodrugs have been investigated to elucidate the importance of side chain bulkiness, backbone cyclization and the reactive amine moiety. The significant difference in the chemical reactivities of iso[Val-MeLeu (3-OH)-Abu] and iso[Val-Leu (3-OH)-Abu], indicated that the nature of amine moiety is important to the kinetics of O,N-acyl migration. The importance of side chain bulkiness and backbone cyclization were found to be less significant.

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页码：2735 / 2740

页数：6

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