Design, synthesis and biological activity of Phenoxyacetic acid (cas 122-59-8) derivatives as novel free fatty acid receptor 1 agonists

Add time:09/09/2019    Source:sciencedirect.com

The free fatty acid receptor 1 (FFA1) is a novel antidiabetic target for the treatment of type 2 diabetes based on particular mechanism in amplifying glucose-stimulated insulin secretion. We have previously identified a series of Phenoxyacetic acid (cas 122-59-8) derivatives. Herein, we describe the further chemical modification of this series directed by ligand efficiency and ligand lipophilicity efficiency. All of these efforts lead to the discovery of the promising candidate 16, an excellent FFA1 agonist with robust agonistic activity (43.6 nM), desired LE and LLE values. Moreover, compound 16 revealed a great potential for improving the hyperglycemia levels in both normal and type 2 diabetic mice without the risk of hypoglycemia even at the high dose of 40 mg/kg.

We also recommend Trading Suppliers and Manufacturers of Phenoxyacetic acid (cas 122-59-8). Pls Click Website Link as below: cas 122-59-8 suppliers

Prev:Raman spectral analysis of Phenoxyacetic acid (cas 122-59-8) and some chloro substituted Phenoxyacetic acid (cas 122-59-8)s
Next:Photocatalytic organic synthesis in an NMR tube: CC coupling of Phenoxyacetic acid (cas 122-59-8) and acrylamide☆)