9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers

Small molecule mGluR1 enhancers based on the lead compound (9H-xanthene-9-carbonyl)-carbamic acid butyl ester derived from random-screening hit diphenylacetyl-carbamic acid ethyl ester were 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 new class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.

Graphical abstractSmall molecule mGluR1 enhancers 3 (X = O, Y = C) and 4 (X = Y = N) were synthesized as pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors.Figure optionsDownload full-size imageDownload as PowerPoint slide