8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands

被引：54

作者：

Lambertucci, Catia ^{[1
]}

Antonini, Ippolito ^{[1
]}

Buccioni, Michela ^{[1
]}

Dal Ben, Diego ^{[1
]}

Kachare, Dhuldeo D. ^{[1
]}

Volpini, Rosaria ^{[1
]}

Klotz, Karl-Norbert ^{[2
]}

Cristalli, Gloria ^{[1
]}

机构：

[1] Univ Camerino, Dipartimento Sci Chim, I-62032 Camerino, Italy

[2] Univ Wurzburg, Inst Pharmakol & Toxikol, D-97078 Wurzburg, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 07期

关键词：

Adenosine; Adenosine receptors; Adenosine receptor antagonists; Purine derivatives; Substituted adenines; MOLECULAR-FORCE FIELD; POTENTIAL ANTICANCER AGENTS; CONFORMATIONAL ENERGIES; BIOLOGICAL EVALUATION; NUCLEIC-ACIDS; ANTAGONISTS; ALKYLATION; PURINES; ANALOGS; PHARMACOLOGY;

D O I：

10.1016/j.bmc.2009.02.030

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Importance of making available selective adenosine receptor antagonists is boosted by recent findings of adenosine involvement in many CNS dysfunctions. In the present work a series of 8-bromo-9-alkyl adenines are prepared and fully characterized in radioligand binding assays or functional cyclase experiments in respect to their interaction with all the four adenosine receptor subtypes. Results show that the presence of the bromine atom in 8-position of 9-substituted adenines promotes in general the interaction with the adenosine receptors, in particular at the A(2A) subtype. The present study also demonstrates that adenine derivatives could be a good starting point to obtain selective adenosine A(2B) receptor antagonists. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2812 / 2822

页数：11

共 70 条

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