Expeditious synthesis and biological evaluation of new C-6 1,2,3-triazole adenosine derivatives A1 receptor antagonists or agonists.
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.
Mathew
Smitha C
SC
Aix-Marseille Université, Institut des Sciences Moléculaires de Marseille, iSm2-UMR CNRS 6263, Centre Saint Jérôme, Service 532, 13397, Marseille Cedex 20, France.
By
Youlet
Y
Berthault
Aurélie
A
Virolleaud
Marie-Alice
MA
Carrega
Louis
L
Chouraqui
Gaëlle
G
Commeiras
Laurent
L
Condo
Jocelyne
J
Attolini
Mireille
M
Gaudel-Siri
Anouk
A
Ruf
Jean
J
Rodriguez
Jean
J
Parrain
Jean-Luc
JL
Guieu
Régis
R
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*
D058906:Purinergic P1 Receptor Agonists; D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1; D014230:Triazoles; D000242:Cyclic AMP; D000241:Adenosine