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Synthesis of 8-(cyclopentyloxy)phenyl substituted xanthine derivatives as adenosine A2A ligands

Bansal, R. and Kumar, G. and Gandhi, D. and Yadav, R. and Young, L.C. and Harvey, A.L. (2009) Synthesis of 8-(cyclopentyloxy)phenyl substituted xanthine derivatives as adenosine A2A ligands. ChemInform, 41 (33). pp. 131-136. ISSN 0931-7597

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Abstract

The present paper describes the synthesis of a series of 8-(cyclopentyloxy)phenyl-xanthines and their evaluation for affinity for A1 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) (K(i)= 100 nM) and 8-[(4-cyclopentyloxy)-3-methoxyphenyl] -3-methyl-1-propylxanthine (12) (K(i) = 150 nM) displayed the highest affinity at A2A receptors as well as over 1000 fold selectivity over the A1 adenosine receptor subtype.

Item type: Article
ID code: 25992
Notes: PMID: 20422944
Keywords: purine derivatives, ring closure reactions, receptor binding activity, Pharmacy and materia medica, Therapeutics. Pharmacology
Subjects: Medicine > Pharmacy and materia medica
Medicine > Therapeutics. Pharmacology
Department: Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
Related URLs:
    Depositing user: Strathprints Administrator
    Date Deposited: 20 Aug 2010 12:19
    Last modified: 26 Apr 2012 15:02
    URI: http://strathprints.strath.ac.uk/id/eprint/25992

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