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 Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Cowart M,Pratt JK,Stewart AO,Bennani YL,Esbenshade TA,Hancock AAdoi
10.1016/j.bmcl.2003.11.032subject
Has Abstractpub_date
2004-02-09 00:00:00pages
689-93issue
3eissn
0960-894Xissn
1464-3405pii
S0960894X03012216journal_volume
14pub_type
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