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Discovery of carmegliptin : a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Mattei, P. and Boehringer, M. and Di Giorgio, P. and Fischer, H. and Hennig, M. and Huwyler, J. and Kocer, B. and Kuhn, B. and Loeffler, B. M. and Macdonald, A. and Narquizian, R. and Rauber, E. and Sebokova, E. and 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 letters, Vol. 20, H. 3. pp. 1109-1113.

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Official URL: http://edoc.unibas.ch/dok/A5840962

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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.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Technologie (Huwyler)
UniBasel Contributors:Huwyler, Jörg
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Pergamon
ISSN:0960-894X
Note:Publication type according to Uni Basel Research Database: Journal article
Last Modified:08 Jun 2012 06:56
Deposited On:08 Jun 2012 06:51

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