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

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.

journal_name

Bioorg Med Chem Lett

authors

Cowart M,Pratt JK,Stewart AO,Bennani YL,Esbenshade TA,Hancock AA

doi

10.1016/j.bmcl.2003.11.032

subject

Has Abstract

pub_date

2004-02-09 00:00:00

pages

689-93

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960894X03012216

journal_volume

14

pub_type

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