期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 14, 页码 6624-6628出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm3002026
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资金
- Danish Council for Independent Research\Technology and Production [09-070364]
- Danish Council for Strategic Research [11-116196]
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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