title: 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.
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.
authors: Dipartimento di Scienze Farmaceutiche, UniVersità di Ferrara, Ferrara, Italy. rmr@unife.it, baraldi@unife.it
authors: Romeo
authors: R
authors: Romagnoli
authors: Pier Giovanni
authors: PG
authors: Baraldi
authors: Maria Dora
authors: MD
authors: Carrion
authors: Carlota Lopez
authors: CL
authors: Cara
authors: Olga
authors: O
authors: Cruz-Lopez
authors: Maria Antonietta
authors: MA
authors: Iaconinoto
authors: Delia
authors: D
authors: Preti
authors: John C
authors: JC
authors: Shryock
authors: Allan R
authors: AR
authors: Moorman
authors: Fabrizio
authors: F
authors: Vincenzi
authors: Katia
authors: K
authors: Varani
authors: Pier
authors: P
authors: Andrea Borea
mesh_terms: D058907:Adenosine A1 Receptor Agonists; D000494:Allosteric Regulation; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D058907:Adenosine A1 Receptor Agonists; D013876:Thiophenes