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

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).

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-11, Vol.6 (22), p.2745-2748
Main Authors: Ashworth, Doreen M., Atrash, Butrus, Baker, Graham R., Baxter, Andrew J., Jenkins, Paul D., Jones, D. Michael, Szelke, Michael
Format: Article
Language:English
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Summary: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).
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(96)00491-X