| Literature DB >> 17851076 |
David E Kaelin1, 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.
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 IC(50)=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.Entities:
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Year: 2007 PMID： 17851076 DOI： 10.1016/j.bmcl.2007.08.049
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823