| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365515 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David E. Kaelin, Abigail L. Smenton, George J. Eiermann, Huaibing He, Barbara Leiting, Kathryn A. Lyons, Reshma A. Patel, Sangita B. Patel, Alexsandr Petrov, Giovanna Scapin, Joseph K. Wu, Nancy A. Thornberry, Ann E. Weber, Joseph L. Duffy,