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    Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.

    The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine.

    Welch JT, Lim DS.

    Department of Chemistry, University at Albany, SUNY, Albany, NY 12222, USA. jwelch@uamail.albany.edu

    The trifluoromethyl group of fluoxetine 1 and fenfluramine and norfenfluramine, 2 and 3, was substituted by the pentafluorosulfanyl group. On examination of the efficacy of the pentafluorosulfanyl containing compounds as inhibitors of 5-hydroxytryptamine receptors, it was found that substitution could lead to enhanced selectivity and in the case of the pentafluorosulfanyl analog of fenfluramine, 18, it significantly enhanced potency against the 5-HT(2b), 5-HT(2c), and 5-HT(6) receptors.

    PMID: 17765553 [PubMed - indexed for MEDLINE]

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