1059604-17-9Relevant academic research and scientific papers
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,Carrion, Maria Dora,Cara, Carlota Lopez,Cruz-Lopez, Olga,Iaconinoto, Maria Antonietta,Preti, Delia,Shryock, John C.,Moorman, Allan R.,Vincenzi, Fabrizio,Varani, Katia,Borea, Pier Andrea
supporting information; experimental part, p. 5875 - 5879 (2009/09/25)
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.
