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

Tabrizi, M.A.; Baraldi, P.G.; Preti, D.; Romagnoli, R.; Saponaro, G.; Baraldi, S.; Moorman, A.R.; Zaid, A.N.; Varani, K.; Borea, P.A.

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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.

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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/530102

Titolo:	1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
Autori interni:	AGHAZADEH TABRIZI, Mojgan BARALDI, Pier Giovanni PRETI, Delia ROMAGNOLI, Romeo SAPONARO, Giulia BARALDI, Stefania VARANI, Katia BOREA, Pier Andrea
Data di pubblicazione:	2008
Rivista:	BIOORGANIC & MEDICINAL CHEMISTRY
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.
Handle:	http://hdl.handle.net/11392/530102
Appare nelle tipologie:	03.1 Articolo su rivista

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