4-cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV

被引:27
作者
Ashworth, DM [1 ]
Atrash, B [1 ]
Baker, GR [1 ]
Baxter, AJ [1 ]
Jenkins, PD [1 ]
Jones, DM [1 ]
Szelke, M [1 ]
机构
[1] FERRING RES INST,CHILWORTH RES CTR,SOUTHAMPTON SO16 7NP,HANTS,ENGLAND
关键词
D O I
10.1016/S0960-894X(96)00491-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of stable, very potent inhibitors of dipeptidyl peptidase IV has been developed. A number of dipeptide analogues, incorporating a 4-cyanothiazolidide were found to have K-i values of less than 1 nM versus human DP-IV and half-lives of between 5 and 27h in aqueous solution (pH 7.4). Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:2745 / 2748
页数:4
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