Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists.
作者： Andrew G. Cole , Tara M. Stauffer , Laura L. Rokosz , Axel Metzger , Lawrence W. Dillard
DOI: 10.1016/J.BMCL.2008.11.066
关键词: Adenosine 、 Stereochemistry 、 Chemistry 、 Ligand binding assay 、 Adenosine a 、 Aminothiazole 、 Combinatorial chemistry 、 G protein-coupled receptor 、 Receptor 、 Adenosine A1 receptor 、 Selectivity
摘要: Abstract The discovery and synthesis of a series 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists from small-molecule combinatorial library using high-throughput radioligand-binding assay is described. Antagonists were further characterized in the binding an A1 selectivity assay. Selected examples exhibited excellent affinity for good versus receptor.
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sci-hub.se 参考文章(27)
Peter Jenner, Istradefylline, a novel adenosine A2A receptor antagonist, for the treatment of Parkinson's disease. Expert Opinion on Investigational Drugs. ,vol. 14, pp. 729- 738 ,(2005) , 10.1517/13543784.14.6.729
Sarah Rose, Neil Ramsay Croft, Peter Jenner, The novel adenosine A2a antagonist ST1535 potentiates the effects of a threshold dose of l-dopa in unilaterally 6-OHDA-lesioned rats. Brain Research. ,vol. 1133, pp. 110- 114 ,(2007) , 10.1016/J.BRAINRES.2006.10.038
P Popoli, Effects of SCH 58261, an adenosine A(2A) receptor antagonist, on quinpirole-induced turning in 6-hydroxydopamine-lesioned rats. Lack of tolerance after chronic caffeine intake. Neuropsychopharmacology. ,vol. 22, pp. 522- 529 ,(2000) , 10.1016/S0893-133X(99)00144-X
Jiang-Fan Chen, Michael A. Schwarzschild, Gene knockout approach to adenosine A2A receptors in Parkinson's disease Drug Development Research. ,vol. 58, pp. 354- 367 ,(2003) , 10.1002/DDR.10215
Maria Antonietta Stasi, Franco Borsini, Katia Varani, Fabrizio Vincenzi, Maria Assunta Di Cesare, Patrizia Minetti, Orlando Ghirardi, Paolo Carminati, ST 1535: a preferential A2A adenosine receptor antagonist. The International Journal of Neuropsychopharmacology. ,vol. 9, pp. 575- 584 ,(2006) , 10.1017/S1461145705006188
Stanley Fahn, David Sulzer, Neurodegeneration and Neuroprotection in Parkinson Disease Neurorx. ,vol. 1, pp. 139- 154 ,(2004) , 10.1602/NEURORX.1.1.139
H. Peter Nestler, Paul A. Bartlett, W. Clark Still, A General Method for Molecular Tagging of Encoded Combinatorial Chemistry Libraries Journal of Organic Chemistry. ,vol. 59, pp. 4723- 4724 ,(1994) , 10.1021/JO00096A008
M. Morelli, J. Wardas, Adenosine A2A receptor antagonists: Potential therapeutic and neuroprotective effects in parkinson’s disease Neurotoxicity Research. ,vol. 3, pp. 545- 556 ,(2001) , 10.1007/BF03033210
José A. Obeso, C. Warren Olanow, John G. Nutt, Levodopa motor complications in Parkinson's disease Trends in Neurosciences. ,vol. 23, pp. S2- S7 ,(2000) , 10.1016/S1471-1931(00)00031-8
Bridgette E Garrett, Roland R Griffiths, The Role of Dopamine in the Behavioral Effects of Caffeine in Animals and Humans Pharmacology Biochemistry and Behavior. ,vol. 57, pp. 533- 541 ,(1997) , 10.1016/S0091-3057(96)00435-2