Free Fatty Acid Receptor
1 (FFA1/GPR40) Agonists:
Mesylpropoxy Appendage Lowers Lipophilicity and Improves ADME Properties
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Abstract
FFA1 (GPR40) is a new target for treatment of type 2
diabetes.
We recently identified the potent FFA1 agonist TUG-469 (<b>5</b>). Inspired by the structurally related TAK-875, we explored the
effects of a mesylpropoxy appendage on <b>5</b>. The appendage
significantly lowers lipophilicity and improves metabolic stability
while preserving potency, resulting in discovery of the potent FFA1
agonist <b>13</b>