The synthesis and evaluation of a series of 2-amino-3-(4-chlorobenzoyl)-4- [4-(alkyl/aryl)piperazin-yl]thiophene derivatives as allosteric enhancers of the A1-adenosine receptor are described. The nature of substituents on the phenyl ring tethered to the piperazine seem to exert a fundamental influence on the allosteric enhancer activity, with the 4-chlorophenyl 8f and 4-trifluoromethyl 8j derivatives being the most active compounds in binding (saturation and displacement experiments) and functional cAMP studies. © 2008 American Chemical Society.

Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N- (substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;IACONINOTO, Antonietta;PRETI, Delia;VINCENZI, Fabrizio;VARANI, Katia;BOREA, Pier Andrea
2008

Abstract

The synthesis and evaluation of a series of 2-amino-3-(4-chlorobenzoyl)-4- [4-(alkyl/aryl)piperazin-yl]thiophene derivatives as allosteric enhancers of the A1-adenosine receptor are described. The nature of substituents on the phenyl ring tethered to the piperazine seem to exert a fundamental influence on the allosteric enhancer activity, with the 4-chlorophenyl 8f and 4-trifluoromethyl 8j derivatives being the most active compounds in binding (saturation and displacement experiments) and functional cAMP studies. © 2008 American Chemical Society.
2008
Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Md; Cara, Cl; Cruz Lopez, O; Iaconinoto, Antonietta; Preti, Delia; Shryock, Jc; Moorman, Ar; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/529784
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