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Synthesis of a New Series of 1 H ‐Imidazol‐1‐yl Substituted 8‐Phenylxanthines as Adenosine Receptor Ligands
Author(s) -
Bansal Ranju,
Kumar Gulshan,
Gandhi Deepika,
Young Louise C.,
Harvey Alan L.
Publication year - 2011
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201000141
Subject(s) - chemistry , adenosine receptor , adenosine , stereochemistry , receptor , combinatorial chemistry , biochemistry , agonist
A new series of 1 H ‐imidazol‐1‐yl substituted 8‐phenylxanthine analogs has been synthesized to study the effects of the imidazole group on the binding affinity of compounds for adenosine receptors. Competition binding studies of these compounds were carried out in vitro with human cloned receptors using [ 3 H]DPCPX and [ 3 H]ZM 241385 as radioligands at A 1 and A 2A adenosine receptors, respectively. The effect of the substitution pattern of the (imidazolyl)alkoxy group on various positions of the phenyl ring at C(8) was also studied. The xanthine derivatives displayed varying degrees of affinity and selectivity towards A 1 and A 2A receptor subtypes despite a common but variedly substituted ArC(8).