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 |
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Authors: | Romagnoli Romeo Baraldi Pier Giovanni Carrion Maria Dora Cara Carlota Lopez Cruz-Lopez Olga Iaconinoto Maria Antonietta Preti Delia Shryock John C Moorman Allan R Vincenzi Fabrizio Varani Katia Andrea Borea Pier |
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Affiliation: | Dipartimento di Scienze Farmaceutiche, UniVersità di Ferrara, Ferrara, Italy. rmr@unife.it, baraldi@unife.it |
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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 A 1-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. |
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