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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- 作者：Romeo Romagnoli ; 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 V
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：September 25, 2008
- 年：2008
- 卷：51
- 期：18
- 页码：5875-5879
- 全文大小：113K
- 年卷期：v.51,no.18(September 25, 2008)
- ISSN：1520-4804
文摘
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.