Journal of Medicinal Chemistry p. 2383 - 2400 (2017)
Update date:2022-08-15
Topics:
Bursavich, Matthew G.
Harrison, Bryce A.
Acharya, Raksha
Costa, Donald E.
Freeman, Emily A.
Hodgdon, Hilliary E.
Hrdlicka, Lori A.
Jin, Hong
Kapadnis, Sudarshan
Moffit, Jeffrey S.
Murphy, Deirdre A.
Nolan, Scott
Patzke, Holger
Tang, Cuyue
Wen, Melody
Koenig, Gerhard
Blain, Jean-Fran?ois
Burnett, Duane A.
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 Aβ42 reductions and subsequent Aβ37 increases in both rodent brain and CSF at 30 mg/kg dosed orally.
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