| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372096 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
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.
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Authors
Patrizio Mattei, Markus Boehringer, Patrick Di Giorgio, Holger Fischer, Michael Hennig, Joerg Huwyler, Buelent Koçer, Bernd Kuhn, Bernd M. Loeffler, Alexander MacDonald, Robert Narquizian, Etienne Rauber, Elena Sebokova, Urs Sprecher,