Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374661 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
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 hypolocomotion, a model of motor dysfunction in Parkinson’s Disease.
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Related Topics
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Authors
Anette Graven Sams, Gitte Kobberøe Mikkelsen, Mogens Larsen, Lars Torup, Lise Tøttrup Brennum, Tenna Juul Schrøder, Benny Bang-Andersen,