| Literature DB >> 19695884 |
Roger J Gillespie1, Samantha J Bamford, Alex Clay, Suneel Gaur, Tim Haymes, Philip S Jackson, Allan M Jordan, Burkhard Klenke, Stefania Leonardi, Jeanette Liu, Howard L Mansell, Sean Ng, Mona Saadi, Heather Simmonite, Gemma C Stratton, Richard S Todd, Douglas S Williamson, Ian A Yule.
Abstract
Antagonists of the human A(2A) 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 derivatives display desirable physiochemical and pharmacokinetic profiles, which have led to promising oral activity in clinically relevant models of Parkinson's disease.Entities:
Mesh：
Substances：
Year: 2009 PMID： 19695884 DOI： 10.1016/j.bmc.2009.07.078
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641