Document Report Card

ID: ALA2163258

Journal: J Med Chem

Title: Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties.

Authors: Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schröder R, Hudson BD, Milligan G, Cawthorne MA, Kostenis E, Kassack MU, Ulven T.

Abstract: FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.

CiteXplore: 22724451

DOI: 10.1021/jm3002026