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 - PubMed (original) (raw)
. 2008 Sep 25;51(18):5875-9.
doi: 10.1021/jm800586p. Epub 2008 Aug 26.
Pier Giovanni Baraldi, Maria Dora Carrion, Carlota Lopez Cara, Olga Cruz-Lopez, Maria Antonietta Iaconinoto, Delia Preti, John C Shryock, Allan R Moorman, Fabrizio Vincenzi, Katia Varani, Pier Andrea Borea
Affiliations
- PMID: 18729349
- DOI: 10.1021/jm800586p
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
Romeo Romagnoli et al. J Med Chem. 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 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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