Antagonists of the human A 2A receptor. Part 6: Further optimization of pyrimidine-4-carboxamides

…, S Leonardi, J Liu, HL Mansell, S Ng, M Saadi…

Index: Gillespie, Roger J.; Bamford, Samantha J.; Clay, Alex; Gaur, Suneel; Haymes, Tim; Jackson, Philip S.; Jordan, Allan M.; Klenke, Burkhard; Leonardi, Stefania; Liu, Jeanette; Mansell, Howard L.; Ng, Sean; Saadi, Mona; Simmonite, Heather; Stratton, Gemma C.; Todd, Richard S.; Williamson, Douglas S.; Yule, Ian A. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 18 p. 6590 - 6605

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Citation Number: 26

Abstract

Antagonists of the human A2A receptor have been reported to have potential therapeutic benefit in the alleviation of the symptoms associated with neurodegenerative movement disorders such as Parkinson's disease. As part of our efforts to discover potent and selective antagonists of this receptor, we herein describe the detailed optimization and structure– activity relationships of a series of pyrimidine-4-carboxamides. These optimized ...