The synthesis and biol. evaluation of a new class of 2-phenyl-2,5-di(hydro)pyrazolo[4,3-c]quinolin-4-one derivs. as A3 adenosine receptor antagonists was reported. A new route based on the Kira-Vilsmeier reaction for the synthesis of this class of compds. was designed. Some of the synthesized compds. showed A3 adenosine receptor affinity in the nanomolar range and good selectivity as evaluated in radioligand binding assays at human (h) A1, A2A, A2B, and A3 adenosine receptor subtypes. Several substituents on the 2-Ph ring were introduced. In particular substitution at the 4-position by Me, methoxy, and chlorine gave optimal activity and selectivity. In conclusion, the 2-phenyl-2,5-dihydro-pyrazolo[4,3-c]quinolin-4-one derivs. described herein represent a new family of in vitro selective antagonists for the adenosine A3 receptor. Selective adenosine A3 receptor antagonists are potential antiasthmatic, antiinflammatory, or cerebroprotective agents (no data).

New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A(3) adenosine receptor antagonists

BARALDI, Pier Giovanni;AGHAZADEH TABRIZI, Mojgan;PRETI, Delia;BOVERO, Andrea;FRUTTAROLO, Francesca;ROMAGNOLI, Romeo;VARANI, Katia;BOREA, Pier Andrea
2005

Abstract

The synthesis and biol. evaluation of a new class of 2-phenyl-2,5-di(hydro)pyrazolo[4,3-c]quinolin-4-one derivs. as A3 adenosine receptor antagonists was reported. A new route based on the Kira-Vilsmeier reaction for the synthesis of this class of compds. was designed. Some of the synthesized compds. showed A3 adenosine receptor affinity in the nanomolar range and good selectivity as evaluated in radioligand binding assays at human (h) A1, A2A, A2B, and A3 adenosine receptor subtypes. Several substituents on the 2-Ph ring were introduced. In particular substitution at the 4-position by Me, methoxy, and chlorine gave optimal activity and selectivity. In conclusion, the 2-phenyl-2,5-dihydro-pyrazolo[4,3-c]quinolin-4-one derivs. described herein represent a new family of in vitro selective antagonists for the adenosine A3 receptor. Selective adenosine A3 receptor antagonists are potential antiasthmatic, antiinflammatory, or cerebroprotective agents (no data).
Baraldi, Pier Giovanni; AGHAZADEH TABRIZI, Mojgan; Preti, Delia; Bovero, Andrea; Fruttarolo, Francesca; Romagnoli, Romeo; Zaid, Na; Moorman, Ar; 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/11392/516943
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