Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 14, Pages 6624-6628Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm3002026
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Funding
- Danish Council for Independent Research\Technology and Production [09-070364]
- Danish Council for Strategic Research [11-116196]
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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 S. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.
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