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ID: ALA1147428
Journal: Bioorg Med Chem Lett
Title: A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.
Authors: Cowart M, Pratt JK, Stewart AO, Bennani YL, Esbenshade TA, Hancock AA.
Abstract: 2-aminoethylbenzofurans constitute a new class of H(3) antagonists that are more rotationally constrained than most previously reported H(3) 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, or a 2,6-dimethylpiperidine.
CiteXplore: 14741270