The free fatty acid 1 receptor (FFA1/GPR40) is highly expressed on pancreatic �-cells and amplifies glucose-stimulated insulin secretion, making it an attractive target for the treatment of type 2 diabetes. Series of potent FFA1 agonists have been identified starting with free fatty acids as lead structures. These typically comprise a carboxylic acid groups that is crucial for the receptor interaction. Bioisosteres are replacement groups that often elicit effects similar to the group they replace in biological systems, and represent a rational approach in lead optimization. The described structure-activity relationships study investigates the effect of bioisosteric replacement of a carboxylic acid group in FFA1 agonists.

Carboxylic acid bioisosteres in free fatty acid receptor 1 (FFA1/GPR40) agonists

243rd National Meeting (2012)

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