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Bioorg Med Chem Lett. 2004 Feb 9;14(3):689-93.

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

Author information

1
Department of Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064-6123, USA. marlon.d.cowart@abbott.com

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.

PMID:
14741270
DOI:
10.1016/j.bmcl.2003.11.032
[Indexed for MEDLINE]

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