1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine Derivatives as Highly Potent and Selective Human A(2B) Adenosine Receptor Antagonists
Publication Type
Original research
Authors
Abdel Naser Zaid
Mojgan Aghazadeh Tabrizi
Pier Giovanni Baraldi
Delia Preti
Romeo Romagnoli
Giulia Saponaro
Stefania Baraldi
Allan R. Moorman
Katia Varani
Pier Andrea Borea
A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A(2B) adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A(2B), A(1), A(2A), and A(3) adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A(2B) adenosine receptor K(i)=7nM and good selectivity (A(1), A(2A), A(3)/A(2B)>140). Synthesis and SAR of this novel class of compounds is presented herein.