Kaelin_2007_Bioorg.Med.Chem.Lett_17_5806

Reference

Title : 4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV - Kaelin_2007_Bioorg.Med.Chem.Lett_17_5806
Author(s) : Kaelin DE , Smenton AL , Eiermann GJ , He H , Leiting B , Lyons KA , Patel RA , Patel SB , Petrov A , Scapin G , Wu JK , Thornberry NA , Weber AE , Duffy JL
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :5806 , 2007
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.

PubMedSearch : Kaelin_2007_Bioorg.Med.Chem.Lett_17_5806
PubMedID: 17851076
Gene_locus related to this paper: human-DPP4

Citations formats

Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL (2007)
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV
Bioorganic & Medicinal Chemistry Lett 17 :5806

Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL (2007)
Bioorganic & Medicinal Chemistry Lett 17 :5806