4.5 Article

Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 17, 页码 4332-4335

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.06.071

关键词

GPR119; GDIR; APD597; Diabetes

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A series of 5-fluoro-4,6-dialkoxypyrimidine GPR119 modulators were discovered and optimized for in vitro agonist activity. A lead molecule was identified that has improved agonist efficacy relative to our clinical compound (APD597) and possesses reduced CYP2C9 inhibitory potential. This optimized lead was found to be efficacious in rodent models of glucose control both alone and in combination with a Dipeptidyl peptidase-4 (DPP-4) inhibitor. (C) 2014 Elsevier Ltd. All rights reserved.

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