A new class of potent non-imidazole H 3 antagonists: 2-aminoethylbenzofurans

…, YL Bennani, TA Esbenshade, AA Hancock

文献索引：Cowart, Marlon; Pratt, John K.; Stewart, Andrew O.; Bennani, Youssef L.; Esbenshade, Timothy A.; Hancock, Arthur A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 3 p. 689 - 693

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被引用次数: 83

摘要

2-Aminoethylbenzofurans constitute a new class of H3 antagonists that are more rotationally constrained than most previously reported H3 antagonists. They retain high potency at human and rat receptors, with efficient CNS penetration observed in 35. The SAR of the basic amine moiety was compared in three different series of analogues. The greatest potency was found in analogues bearing a 2-methylpyrrolidine, a 2, 5-dimethylpyrrolidine, ...