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Bioorg Med Chem Lett. 2007 Mar 1;17(5):1443-6. Epub 2006 Dec 1.

4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.

Author information

1
Neuroscience Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA. larry.a.black@abbott.com

Abstract

4-[6-(2-Tertiaryaminoethyl)naphthalen-2-yl]benzonitriles are conformationally constrained histamine H3 receptor antagonists with high potency and selectivity. The analogs were designed around a naphthalene core, with the goal of enhancing lipophilicity and CNS penetration, as compared to a previously reported benzofuran series. The SAR of the tertiary amine moiety is similar to that reported for the benzofuran series, with analogs bearing a 2-methylpyrrolidine substituent possessing the greatest rat and human H3 receptor binding affinities.

PMID:
17169555
DOI:
10.1016/j.bmcl.2006.11.073
[Indexed for MEDLINE]

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