Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 24, Pages 6357-6361Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.085
Keywords
Diacylphloroglucinols; FFAR1 agonist; GPR40 agonist; Type-2 diabetes
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In this letter, we report discovery of diacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists. Several diacylphloroglucinols with varying length of acyl functionality and substitution on aromatic hydroxyls were synthesized and evaluated for GPR40 agonism using functional calcium-flux assay. Out of 17 compounds evaluated, 14, 17, 19 and 25 exhibited good GPR40 agonistic activity with EC(50) values ranging from 0.07 to 8 mu M (pEC(50) 7.12-5.09), respectively, with maximal agonistic response of 84-102%. (C) 2008 Elsevier Ltd. All rights reserved.
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