Bioorganic & Medicinal Chemistry Letters 2012-06-01

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

Derek Dunn, Greg Hostetler, Mohamed Iqbal, Val R. Marcy, Yin Guo Lin, Bruce Jones, Lisa D. Aimone, John Gruner, Mark A. Ator, Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Greg Hostetler, Mohamed Iqbal, Val R. Marcy, Yin Guo Lin, Bruce Jones, Lisa D. Aimone, John Gruner, Mark A. Ator, Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Greg Hostetler, Mohamed Iqbal, Val R. Marcy, Yin Guo Lin, Bruce Jones, Lisa D. Aimone, John Gruner, Mark A. Ator, Edward R. Bacon, Sankar Chatterjee

文献索引：Bioorg. Med. Chem. Lett. 22(11) , 3751-3, (2012)

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摘要

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).