1262151-06-3Relevant academic research and scientific papers
Synthesis of 8-(cyclopentyloxy)phenyl substituted xanthine derivatives as adenosine A2A ligands
Bansal, Ranju,Kumar, Gulshan,Gandhi, Deepika,Yadav, Rakesh,Young, Louise C.,Harvey, Alan L.
, p. 131 - 136 (2011/07/30)
The present paper describes the synthesis of a series of 8-(cyclopentyloxy)phenyl-xanthines and their evaluation for affinity for A 1 and A2 adenosine receptors using radioligand binding assays. The effects of moving the cyclopentyloxy substituent with or without an ortho methoxy group on the various positions of the 8-phenyl ring have been studied. The vanilloid based xanthines 8-[4-(cyclopentyloxy)-3-methoxyphenyl]-1, 3-dimethylxanthine (6a) (Ki = 100 nM) and 8-[(4-cyclopentyloxy)-3- methoxyphenyl]-3-methyl-1-propylxanthine (12) (Ki = 150 nM) displayed the highest affinity at A2A receptors as well as over 1000 fold selectivity over the A1 adenosine receptor subtype. ECV · Editio Cantor Verlag, Aulendorf (Germany).
