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Curr Opin Drug Discov Devel. 2005 Jul;8(4):458-68.

Recent advances in the design and optimization of adenosine A2A receptor antagonists.

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  • 1Biogen Idec Inc, Department of Medicinal Chemistry, 14 Cambridge Center, Cambridge, MA 02142, USA.


In recent years, the adenosine A2A receptor has gained interest as a potential therapeutic target for alleviating the symptoms of Parkinson's disease. Adenosine A2A receptor antagonists are orally effective in a variety of rodent models of Parkinson's disease. Traditionally, adenosine A2A, receptor antagonists are divided into two general classes, xanthine or non-xanthine derivatives. Extensive optimization among the xanthine derivatives has already led to the clinical candidate KW-6002 (Kyowa Hakko Kogyo Co Ltd). However, there is increasing interest among researchers in this field to explore other classes of compounds as potential antagonists for this particular receptor. This review highlights the more recent developments in the design and optimization of non-xanthine derivatives as adenosine A2A receptor antagonists.

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