title: Synthesis of a new series of 1H-imidazol-1-yl substituted 8-phenylxanthines as adenosine receptor ligands.
abstract: A new series of 1H-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 Ar-C(8).
authors.affiliation: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh - 160014, India. ranju29in@yahoo.co.in
authors.forename: Ranju
authors.initials: R
authors.lastname: Bansal
authors.forename: Gulshan
authors.initials: G
authors.lastname: Kumar
authors.forename: Deepika
authors.initials: D
authors.lastname: Gandhi
authors.forename: Louise C
authors.initials: LC
authors.lastname: Young
authors.forename: Alan L
authors.initials: AL
authors.lastname: Harvey
mesh_terms: D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008024:Ligands; D011485:Protein Binding; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D014970:Xanthines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D007093:Imidazoles; D008024:Ligands; D018047:Receptors, Purinergic P1; D014970:Xanthines