A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivs. has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1, A2A, and A3 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 A2B adenosine receptor Ki = 7 nM and good selectivity (A1, A2A, A3/A2B > 140). Synthesis and SAR of this novel class of compds. is presented herein.

1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists

AGHAZADEH TABRIZI, Mojgan;BARALDI, Pier Giovanni;PRETI, Delia;ROMAGNOLI, Romeo;SAPONARO, Giulia;BARALDI, Stefania;VARANI, Katia;BOREA, Pier Andrea
2008

Abstract

A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivs. has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1, A2A, and A3 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 A2B adenosine receptor Ki = 7 nM and good selectivity (A1, A2A, A3/A2B > 140). Synthesis and SAR of this novel class of compds. is presented herein.
AGHAZADEH TABRIZI, Mojgan; Baraldi, Pier Giovanni; Preti, Delia; Romagnoli, Romeo; Saponaro, Giulia; Baraldi, Stefania; Moorman, A. R.; Zaid, A. N.; Varani, Katia; Borea, Pier Andrea
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/530102
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