Design, synthesis, and evaluation of tetrasubstituted pyridines as potent 5-HT2CReceptor agonists

ROUQUET, Guy, MOORE, Dianna E., SPAIN, Malcolm, ALLWOOD, Daniel, BATTILOCCHIO, Claudio, BLAKEMORE, David C., FISH, Paul V., JENKINSON, Stephen, JESSIMAN, Alan S., LEY, Steven V., MCMURRAY, Gordon and STORER, R. Ian (2015). Design, synthesis, and evaluation of tetrasubstituted pyridines as potent 5-HT2CReceptor agonists. ACS Medicinal Chemistry Letters, 6 (3), 329-333.

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Official URL: http://pubs.acs.org/doi/abs/10.1021/ml500507v
Link to published version:: https://doi.org/10.1021/ml500507v
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    Abstract

    A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties commensurate with an orally available and CNS penetrant profile. The synthesis of a novel bicyclic tetrasubstituted pyridine core template is outlined, including rationale to account for the unexpected formation of aminopyridine 13 resulting from an ammonia cascade cyclization.

    Item Type: Article
    Research Institute, Centre or Group - Does NOT include content added after October 2018: Biomolecular Sciences Research Centre
    Identification Number: https://doi.org/10.1021/ml500507v
    Page Range: 329-333
    Depositing User: Users 3084 not found.
    Date Deposited: 13 Aug 2015 09:06
    Last Modified: 13 Jun 2017 13:31
    URI: http://shura.shu.ac.uk/id/eprint/10759

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