The synthesis and biological evaluation of 2-amino-4, 5, 6, 7, 8, 9-hexahydrocycloocta [b] thiophenes as allosteric modulators of the A 1 adenosine receptor

…, A Christopoulos, BL Flynn, PJ Scammells…

文献索引：Aurelio, Luigi; Christopoulos, Arthur; Flynn, Bernard L.; Scammells, Peter J.; Sexton, Patrick M.; Valant, Celine Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 12 p. 3704 - 3707

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被引用次数: 17

摘要

Abstract A series of 2-amino-4, 5, 6, 7, 8, 9-hexahydrocycloocta [b] thiophenes were prepared and evaluated as potential allosteric modulators of the A 1 adenosine receptor (AR). The structure–activity relationships of the 3-position were explored along with varying the size of the cycloalkyl ring. 2-Aminothiophenes with amide and hydrazide groups in the 3- position were completely inactive in an A 1-AR-mediated ERK1/2 phosphorylation assay, ...