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    Bioorg Med Chem Lett. 2009 Feb 1;19(3):903-7. doi: 10.1016/j.bmcl.2008.11.114. Epub 2008 Dec 6.

    Novel imidazole-based histamine H3 antagonists.

    Jablonowski JA, Ly KS, Bogenstaetter M, Dvorak CA, Boggs JD, Dvorak LK, Lord B, Miller KL, Mazur C, Wilson SJ, Lovenberg TW, Carruthers NI.

    Source

    Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. jjablono@its.jnj.com

    Abstract

    A novel series of imidazole containing histamine H(3) receptor ligands were investigated and found to be potent functional antagonists. After improving the stability of these molecules towards liver microsomes, these compounds were found to have no appreciable affinity for CYP P450s. Subsequent in vivo experiments showed significant brain uptake of (4-chloro-phenyl)-[2-(1-isopropyl-piperidin-4-ylmethoxy)-3-methyl-3H-imidazol-4-yl]-methanone 22.

    PMID:
    19119007
    [PubMed - indexed for MEDLINE]

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