Mattei_2010_Bioorg.Med.Chem.Lett_20_1109

Reference

Title : Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Mattei_2010_Bioorg.Med.Chem.Lett_20_1109
Author(s) : Mattei P , Boehringer M , Di Giorgio P , Fischer H , Hennig M , Huwyler J , Kocer B , Kuhn B , Loeffler BM , Macdonald A , Narquizian R , Rauber E , Sebokova E , Sprecher U
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :1109 , 2010
Abstract :

Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical development. Its X-ray structure in complex with the enzyme and early efficacy data in animal models of type 2 diabetes are also presented.

PubMedSearch : Mattei_2010_Bioorg.Med.Chem.Lett_20_1109
PubMedID: 20031405
Gene_locus related to this paper: human-DPP4

Related information

Inhibitor Carmegliptin    B2Q
Gene_locus human-DPP4
Structure 3KWF    3OC0

Citations formats

Mattei P, Boehringer M, Di Giorgio P, Fischer H, Hennig M, Huwyler J, Kocer B, Kuhn B, Loeffler BM, Macdonald A, Narquizian R, Rauber E, Sebokova E, Sprecher U (2010)
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Bioorganic & Medicinal Chemistry Lett 20 :1109

Mattei P, Boehringer M, Di Giorgio P, Fischer H, Hennig M, Huwyler J, Kocer B, Kuhn B, Loeffler BM, Macdonald A, Narquizian R, Rauber E, Sebokova E, Sprecher U (2010)
Bioorganic & Medicinal Chemistry Lett 20 :1109