Title of article
4-Arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV
Author/Authors
David E. Kaelin، نويسنده , , Abigail L. Smenton، نويسنده , , George J. Eiermann، نويسنده , , Huaibing He، نويسنده , , Barbara Leiting، نويسنده , , Kathryn A. Lyons، نويسنده , , Reshma A. Patel، نويسنده , , Sangita B. Patel، نويسنده , , Alexsandr Petrov، نويسنده , , Giovanna Scapin، نويسنده , , Joseph K. Wu، نويسنده , , Nancy A. Thornberry، نويسنده , , Ann E. Weber، نويسنده , , Joseph L. Duffy، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
5806
To page
5811
Abstract
A novel series of 4-arylcyclohexylalanine DPP-4 inhibitors was synthesized and tested for inhibitory activity as well as selectivity over the related proline-specific enzymes DPP-8 and DPP-9. Optimization of this series led to 28 (DPP-4 IC50 = 4.8 nM), which showed an excellent pharmacokinetic profile across several preclinical species. Evaluation of 28 in an oral glucose tolerance test demonstrated that this compound effectively reduced glucose excursion in lean mice.
Keywords
DPP-4 inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798701
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