Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

TY - JOUR

T1 - Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

AU - Christiansen, Elisabeth

AU - Due-Hansen, Maria E

AU - Urban, Christian

AU - Grundmann, Manuel

AU - Schröder, Ralf

AU - Hudson, Brian D

AU - Milligan, Graeme

AU - Cawthorne, Michael A

AU - Kostenis, Evi

AU - Kassack, Matthias U

AU - Ulven, Trond

PY - 2012

Y1 - 2012

N2 - 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.

AB - 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.

U2 - 10.1021/jm3002026

DO - 10.1021/jm3002026

M3 - Journal article

SN - 0022-2623

VL - 55

SP - 6624

EP - 6628

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 14

ER -