Author/Authors :
Sandip B. Bharate، نويسنده , , Atish Rodge، نويسنده , , Rajendra K. Joshi، نويسنده , , Jaspreet Kaur، نويسنده , , Shaila Srinivasan، نويسنده , , S. Senthil Kumar، نويسنده , , Asha Kulkarni-Almeida، نويسنده , , Sarala Balachandran، نويسنده , , Arun Balakrishnan، نويسنده , , Ram A. Vishwakarma، نويسنده ,
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 EC50 values ranging from 0.07 to 8 μM (pEC50 7.12–5.09), respectively, with maximal agonistic response of 84–102%.
Keywords :
Diacylphloroglucinols , type-2 diabetes , FFAR1 agonist , GPR40 agonist
