%0 Journal Article %1 Lambertucci2007a %A Lambertucci, C. %A Vittori, S. %A Mishra, R. C. %A Ben, D. Dal %A Klotz, K. N. %A Volpini, R. %A Cristalli, G. %D 2007 %J Nucleosides Nucleotides Nucleic Acids %K & A2A/*antagonists Adenine/*analogs Adenosine Agents/chemical Animals Antiparkinson CHO Cricetinae Cricetulus Humans derivatives/chemistry inhibitors synthesis/*chemistry/*pharmacology Receptor Cell %N 10-12 %P 1443-6 %T Synthesis and biological activity of trisubstituted adenines as A 2A adenosine receptor antagonists %U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18066802 %V 26 %X The discovery of new drugs for the treatment of neurodegenerative disorders, such as Parkinson's disease, has become an attractive field of research. Due to the regulation of D(2) receptor activity by A(2A) adenosine receptor, potent and selective ligands of A(2A) subtype could be useful tools to study neurodegenerative disorders. A series of 2,8-disubstituted-9-ethyladenine derivatives was synthesized and tested in binding affinity assay at human adenosine receptors. New compounds showed good affinity and selectivity at A(2A) receptor versus the other subtypes. The introduction of a bromine atom in 8-position increased the affinity of these compounds, leading to ligands with K(i) in the nanomolar range.

@article{Lambertucci2007a, abstract = {The discovery of new drugs for the treatment of neurodegenerative disorders, such as Parkinson's disease, has become an attractive field of research. Due to the regulation of D(2) receptor activity by A(2A) adenosine receptor, potent and selective ligands of A(2A) subtype could be useful tools to study neurodegenerative disorders. A series of 2,8-disubstituted-9-ethyladenine derivatives was synthesized and tested in binding affinity assay at human adenosine receptors. New compounds showed good affinity and selectivity at A(2A) receptor versus the other subtypes. The introduction of a bromine atom in 8-position increased the affinity of these compounds, leading to ligands with K(i) in the nanomolar range.}, added-at = {2010-12-14T18:12:02.000+0100}, author = {Lambertucci, C. and Vittori, S. and Mishra, R. C. and Ben, D. Dal and Klotz, K. N. and Volpini, R. and Cristalli, G.}, biburl = {https://www.bibsonomy.org/bibtex/2f01c6dbd4ca3944074136dbbfc5b7b07/pharmawuerz}, endnotereftype = {Journal Article}, interhash = {8ee07c9e5d84b1c0662037177193c187}, intrahash = {f01c6dbd4ca3944074136dbbfc5b7b07}, issn = {1525-7770 (Print) 1525-7770 (Linking)}, journal = {Nucleosides Nucleotides Nucleic Acids}, keywords = {& A2A/*antagonists Adenine/*analogs Adenosine Agents/chemical Animals Antiparkinson CHO Cricetinae Cricetulus Humans derivatives/chemistry inhibitors synthesis/*chemistry/*pharmacology Receptor Cell}, note = {Lambertucci, Catia Vittori, Sauro Mishra, Ram Chandra Dal Ben, Diego Klotz, Karl-Norbert Volpini, Rosaria Cristalli, Gloria Research Support, Non-U.S. Gov't United States Nucleosides, nucleotides \& nucleic acids Nucleosides Nucleotides Nucleic Acids. 2007;26(10-12):1443-6.}, number = {10-12}, pages = {1443-6}, shorttitle = {Synthesis and biological activity of trisubstituted adenines as A 2A adenosine receptor antagonists}, timestamp = {2010-12-14T18:20:40.000+0100}, title = {Synthesis and biological activity of trisubstituted adenines as A 2A adenosine receptor antagonists}, url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18066802}, volume = 26, year = 2007 }