Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A 2A receptor antagonists

…, LT Brennum, TJ Schrøder, B Bang-Andersen

Index: Sams, Anette Graven; Mikkelsen, Gitte Kobberoe; Larsen, Mogens; Torup, Lars; Brennum, Lise Tottrup; Schroder, Tenna Juul; Bang-Andersen, Benny Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 5241 - 5244

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Citation Number: 10

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 ...

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