Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 15, Pages 4097-4101Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.011
Keywords
Dipeptidyl peptidase-IV; DPP-4; DPP-IV; Dipeptidyl peptidase 8; DPP-8; DPP-9; Quiescient peptidyl peptidase; QPP; GLP-1; Glucagon-like peptide 1; Benzimidazole; Imidazopyridine; Buchwald coupling; Sitagliptin
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Funding
- Center for Advanced Radiation Sources at the University of Chicago
- U. S. Department of Energy, Office of Science, Office of Basic Energy Sciences [W-31-109-Eng-38]
- Offices of Biological and Environmental Research and of Basic Energy Sciences of the US Department of Energy
- National Center for Research Resources of the National Institutes of Health
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A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported. (C) 2009 Elsevier Ltd. All rights reserved.
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