Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer’s Disease
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https://figshare.com/articles/dataset/Design_Synthesis_and_Evaluation_of_a_Novel_Series_of_Oxadiazine_Gamma_Secretase_Modulators_for_Familial_Alzheimer_s_Disease/4743562
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资源简介：
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.
创建时间：
2017-03-10
