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  • Title: 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
    Author: Black LA, Nersesian DL, Sharma P, Ku YY, Bennani YL, Marsh KC, Miller TR, Esbenshade TA, Hancock AA, Cowart M.
    Journal: Bioorg Med Chem Lett; 2007 Mar 01; 17(5):1443-6. PubMed ID: 17169555.
    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.
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