University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh - 160014, India.
Chem Biodivers. 2011 Jul;8(7):1290-300. doi: 10.1002/cbdv.201000141.
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).
已经合成了一系列新的 1H-咪唑-1-基取代的 8-苯基黄嘌呤类似物，以研究咪唑基团对化合物与腺苷受体结合亲和力的影响。使用 [(3)H]DPCPX 和 [(3)H]ZM 241385 作为放射性配体，在体外对这些化合物与人克隆受体进行了竞争结合研究，分别用于 A(1)和 A(2A) 腺苷受体。还研究了（咪唑基）烷氧基基团在 C(8) 位上苯环的不同位置的取代模式对各种位置的影响。尽管存在共同的但取代程度不同的 Ar-C(8)，但黄嘌呤衍生物对 A(1)和 A(2A)受体亚型表现出不同程度的亲和力和选择性。
