| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374762 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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%.
Graphical abstractDiscovery of diacylphloroglucinols as a new class of GPR40 agonists is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sandip B. Bharate, Atish Rodge, Rajendra K. Joshi, Jaspreet Kaur, Shaila Srinivasan, S. Senthil Kumar, Asha Kulkarni-Almeida, Sarala Balachandran, Arun Balakrishnan, Ram A. Vishwakarma,