Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 6, Pages 2383-2400Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01620
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Herein we describe the design, synthesis, and evaluation of a novel series of oxadiazine-based gamma secretase modulators obtained via isosteric amide replacement and critical consideration of conformational restriction. Oxadiazine lead 47 possesses good in vitro potency with excellent predicted CNS drug-like properties and desirable ADME/PK profile. This lead compound demonstrated robust A beta(42) reductions and subsequent A beta(37) increases in both rodent brain and CSF at 30 mg/kg dosed orally.
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