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