Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A 1-adenosine receptor

…, MA Tabrizi, JC Shryock, E Leung, R Romagnoli

文献索引：Baraldi, Pier Giovanni; Zaid, Abdel Naser; Lampronti, Ilaria; Fruttarolo, Francesca; Pavani, Maria Giovanna; Tabrizi, Mojgan Aghazadhe; Shryock, John C.; Leung, Edward; Romagnoli, Romeo Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 17 p. 1953 - 1957

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被引用次数: 73

摘要

New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1- adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 μM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor. Compounds 4e and 4o appeared to be ...