Title of article
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors
Author/Authors
S.J., Pearton, J.W., Corbett, M., Stavola، نويسنده , , K. Dirico، نويسنده , , W. Song، نويسنده , , B.P. Boscoe، نويسنده , , S.D. Doran، نويسنده , , D. Boyer، نويسنده , , X. Qiu، نويسنده , , M. Ammirati، نويسنده , , M.A. VanVolkenburg، نويسنده , , R.K. McPherson، نويسنده , , J.C. Parker، نويسنده , , E.D. Cox، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
7
From page
6707
To page
6713
Abstract
The cis-3-amino-4-(2-cyanopyrrolidide)-pyrrolidine template has been shown to afford low nanomolar inhibitors of human DPP-IV that exhibit a robust PK/PD profile. An X-ray co-crystal structure of 5 confirmed the proposed mode of binding. The potent single digit DPP-IV inhibitor 53 exhibited a preferred PK/PD profile in preclinical animal models and was selected for additional profiling.
Keywords
Dipeptidyl peptidase IV , DPP-IV , Diabetes
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798872
Link To Document