Herein we describe the discovery of a series of novel adenosine A2A receptor antagonists. A successful hit-to-lead optimization of an HTS hit led to replacement of a metabolically labile ester moiety with a heteroaromatic group. A compound from the series,( cyclopropanecarboxylic acid [5-(5-methyl-[1, 2, 4] oxadiazol-3-yl)-4-phenyl-thiazol-2-yl]- amide, compound 13), was shown to be effective in reversing haloperidol-induced ...
