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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Data di pubblicazione: | 2008 | |
Titolo: | 1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists | |
Autori: | 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. | |
Rivista: | BIOORGANIC & MEDICINAL CHEMISTRY | |
Parole Chiave: | A; 2B; antagonists; Adenosine receptors; Binding; Biological activity; Functional; Human; Phenylacetamide; Xanthine; | |
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. | |
Digital Object Identifier (DOI): | 10.1016/j.bmc.2007.11.058 | |
Handle: | http://hdl.handle.net/11392/530102 | |
Appare nelle tipologie: | 03.1 Articolo su rivista |