Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists

✍ Scribed by Anette Graven Sams; Gitte Kobberøe Mikkelsen; Mogens Larsen; Lars Torup; Lise Tøttrup Brennum; Tenna Juul Schrøder; Benny Bang-Andersen

• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 475 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.06.138

✦ Synopsis

Chart 1. Structures and hA 2A and hA 1 binding affinities of istradefylline (KW-6002, 1), preladenant (SCH-420814, 2) and HTS hit 3.