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    Bioorg Med Chem Lett. 2010 Sep 1;20(17):5069-73. Epub 2010 Jul 11.

    Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.

    Gianotti M, Corti C, Delle Fratte S, Di Fabio R, Leslie CP, Pavone F, Piccoli L, Stasi L, Wigglesworth MJ.

    Source

    Neurosciences CEDD, GlaxoSmithKline, Medicines Research Centre, Verona, Italy. massimo.gianotti@aptuit.com

    Abstract

    A novel imidazobenzazepine template (5a) with potent dual H(1)/5-HT(2A) antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R(1)-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]-2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H(1)/5-HT(2A) receptor antagonist activities and good developability profiles.

    Copyright 2010 Elsevier Ltd. All rights reserved.

    PMID:
    20674357
    [PubMed - indexed for MEDLINE]

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