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- W2021283318 abstract "Starting from advanced pyrrolidin-2-one lead compounds, this novel series of small-molecule orexin receptor antagonists was further optimized by fine-tuning of the C-3 substitution at the γ-lactam ring. We discuss our design to align in vitro potency with metabolic stability and improved physicochemical/pharmacokinetic properties while avoiding P-glycoprotein-mediated efflux. These investigations led to the identification of the orally active 3-hydroxypyrrolidin-2-one 46, a potent and selective orexin-2 receptor antagonist, that achieved good brain exposure and promoted physiological sleep in rats." @default.
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- W2021283318 date "2015-05-01" @default.
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- W2021283318 title "Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2" @default.
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- W2021283318 doi "https://doi.org/10.1016/j.bmcl.2015.03.035" @default.
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