| Literature DB >> 20031405 |
Patrizio Mattei1, 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.
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. Copyright (c) 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20031405 DOI： 10.1016/j.bmcl.2009.12.024
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823