Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers

Small molecule mGluR1 enhancers, which are 9H-xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides, have been previously reported. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides with improved pharmacokinetic properties have been designed and synthesized as useful pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors. The synthesis and the structure–activity relationship of this class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.

The synthesis of a new class of selectively fluorinated small molecule mGluR1 enhancers with improved pharmacokinetic properties is presented. Their potential use as pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors is discussed.Figure optionsDownload as PowerPoint slide