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


ID: CHEMBL1153377
Journal: Bioorg Med Chem
Title: 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Authors: Lambertucci C, Antonini I, Buccioni M, Dal Ben D, Kachare DD, Volpini R, Klotz KN, Cristalli G.
Abstract: 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.
CiteXplore: 19282184
Patent ID: ---
ChEMBL IDTarget SimilarityCompound SimilarityReferenceTitlePubMed IDDOI
CHEMBL1134734 10 Bioorg Med Chem Lett (2001) 11:1931-1934 Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor. 11459663 10.1016/s0960-894x(01)00347-x
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CHEMBL1146808 0.80 Bioorg Med Chem Lett (2004) 14:3775-3779 Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma. 15203160 10.1016/j.bmcl.2004.04.099
CHEMBL1135743 0.750 J Med Chem (2002) 45:3337-3344 Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. 12139445 10.1021/jm0208469
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