title: Expeditious synthesis and biological evaluation of new C-6 1,2,3-triazole adenosine derivatives A1 receptor antagonists or agonists.
abstract: The synthesis of new C-6 1,2,3-triazole adenosine derivatives via microwave assisted 1,3-dipolar cycloaddition as key step is described. The binding on membranes of cells that over express A(1) adenosine receptors (A(1)AR) was also evaluated. Among them, four compounds increased cAMP production, in a dose-dependent manner acting as antagonists of the A(1)AR, while two compounds act as agonists.
authors.affiliation: Aix-Marseille Université, Institut des Sciences Moléculaires de Marseille, iSm2-UMR CNRS 6263, Centre Saint Jérôme, Service 532, 13397, Marseille Cedex 20, France.
authors.forename: Smitha C
authors.initials: SC
authors.lastname: Mathew
authors.forename: Youlet
authors.initials: Y
authors.lastname: By
authors.forename: Aurélie
authors.initials: A
authors.lastname: Berthault
authors.forename: Marie-Alice
authors.initials: MA
authors.lastname: Virolleaud
authors.forename: Louis
authors.initials: L
authors.lastname: Carrega
authors.forename: Gaëlle
authors.initials: G
authors.lastname: Chouraqui
authors.forename: Laurent
authors.initials: L
authors.lastname: Commeiras
authors.forename: Jocelyne
authors.initials: J
authors.lastname: Condo
authors.forename: Mireille
authors.initials: M
authors.lastname: Attolini
authors.forename: Anouk
authors.initials: A
authors.lastname: Gaudel-Siri
authors.forename: Jean
authors.initials: J
authors.lastname: Ruf
authors.forename: Jean
authors.initials: J
authors.lastname: Rodriguez
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Parrain
authors.forename: Régis
authors.initials: R
authors.lastname: Guieu
mesh_terms: D000241:Adenosine / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002460:Cell Line; D000242:Cyclic AMP / Q000096:biosynthesis; D006801:Humans; D015394:Molecular Structure; D058906:Purinergic P1 Receptor Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D058915:Purinergic P1 Receptor Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D058906:Purinergic P1 Receptor Agonists; D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1; D014230:Triazoles; D000242:Cyclic AMP; D000241:Adenosine