Wake promoting agents: Search for next generation modafinil, lessons learned: Part III

In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents were developed and evaluated in rat. Extensive pharmacokinetic studies of a potent member (compound 15) of the series revealed that the wake...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2012-06, Vol.22 (11), p.3751-3753
Hauptverfasser: Dunn, Derek, Hostetler, Greg, Iqbal, Mohamed, Marcy, Val R., Lin, Yin Guo, Jones, Bruce, Aimone, Lisa D., Gruner, John, Ator, Mark A., Bacon, Edward R., Chatterjee, Sankar
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Sprache:eng
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Zusammenfassung:In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents were developed and evaluated in rat. Extensive pharmacokinetic studies of a potent member (compound 15) of the series revealed that the wake promotion activity of the analog was likely due to an active metabolite (compound 3). In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents were developed and evaluated in rat. Extensive pharmacokinetic studies of a potent member of the series (compound 15) revealed that the wake promotion activity of the analog was likely due to an active metabolite (compound 3).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.04.031