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7-β-D-呋喃核糖基黄嘌呤的合成及腺苷受体亲和力

Synthesis and adenosine receptor affinity of 7-beta-D-ribofuranosylxanthine.

作者信息

Bridson P K, Lin X, Melman N, Ji X D, Jacobson K A

机构信息

Chemistry Department, University of Memphis, TN 38152, USA.

出版信息

Nucleosides Nucleotides. 1998 Apr;17(4):759-68. doi: 10.1080/07328319808004673.

Abstract

7-beta-D-Ribofuranosylxanthine, a previously unreported isomer of xanthosine, was prepared in four steps from 7-benzylxanthine. The procedure, which involves the use of pivaloyloxymethyl groups to protect the xanthine ring, was also applied to preparation of some 1-N-alkyl derivatives of 7-ribosylxanthine. Adenosine receptor affinity for these compounds was determined. 7-beta-D-Ribofuranosylxanthine was found to have higher affinity and greater selectivity for the A1 receptor than previously reported xanthine nucleosides, and to be a partial agonist.

摘要

7-β-D-呋喃核糖基黄嘌呤是一种以前未报道过的黄苷异构体,由7-苄基黄嘌呤经四步反应制得。该方法涉及使用新戊酰氧基甲基基团保护黄嘌呤环,也用于制备7-核糖基黄嘌呤的一些1-N-烷基衍生物。测定了这些化合物对腺苷受体的亲和力。发现7-β-D-呋喃核糖基黄嘌呤对A1受体的亲和力和选择性高于先前报道的黄嘌呤核苷,并且是一种部分激动剂。

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