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ID: ALA1141015
Journal: Bioorg Med Chem Lett
Title: Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.
Authors: Bharate SB, Rodge A, Joshi RK, Kaur J, Srinivasan S, Kumar SS, Kulkarni-Almeida A, Balachandran S, Balakrishnan A, Vishwakarma RA.
Abstract: 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 microM (pEC(50) 7.12-5.09), respectively, with maximal agonistic response of 84-102%.
CiteXplore: 18993064