4-CYANOTHIAZOLIDIDES AS VERY POTENT, STABLE INHIBITORS OF DIPEPTIDYL-PEPTIDASE-IV

Authors
ASHWORTH DM ATRASH B BAKER GR BAXTER AJ JENKINS PD JONES DM SZELKE M
Citation
Dm. Ashworth et al., 4-CYANOTHIAZOLIDIDES AS VERY POTENT, STABLE INHIBITORS OF DIPEPTIDYL-PEPTIDASE-IV, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2745-2748
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2745 - 2748
Database
ISI
SICI code
0960-894X(1996)6:22<2745:4AVPSI>2.0.ZU;2-X
Abstract
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 ver sus human DP-IV and half-lives of between 5 and 27h in aqueous solutio n (pH 7.4). Copyright (C) 1996 Elsevier Science Ltd