title: Synthesis and biological activity of trisubstituted adenines as A 2A adenosine receptor antagonists.
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.
authors: Dipartimento di Scienze Chimiche, Università di Camerino, I-62032 Camerino, MC, Italy. catia.lambertucci@unicam.it
authors: Catia
authors: C
authors: Lambertucci
authors: Sauro
authors: S
authors: Vittori
authors: Ram Chandra
authors: RC
authors: Mishra
authors: Diego
authors: D
authors: Dal Ben
authors: Karl-Norbert
authors: KN
authors: Klotz
authors: Rosaria
authors: R
authors: Volpini
authors: Gloria
authors: G
authors: Cristalli
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000737:chemistry; D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D000978:Antiparkinson Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; C001172:9-ethyladenine; D000225:Adenine