Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 1, Pages 49-52Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.09.099
Keywords
DPP-IV; diabetes; diazepanone
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Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC50 = 18 nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC50 = 2.6 nM), selective, and efficacious in an oral glucose tolerance test in mice. It was selected for extensive preclinical development as a potential back-up candidate to sitagliptin. (c) 2006 Elsevier Ltd. All rights reserved.
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