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- W2132720896 abstract "1,4-Oxazines are presented, which show good in vitro inhibition in enzymatic and cellular BACE1 assays. We describe lead optimization focused on reducing the amidine pKa while optimizing interactions in the BACE1 active site. Our strategy permitted modulation of properties such as permeation and especially P-glycoprotein efflux. This led to compounds which were orally bioavailable, centrally active, and which demonstrated robust lowering of brain and CSF Aβ levels, respectively, in mouse and dog models. The amyloid lowering potential of these molecules makes them valuable leads in the search for new BACE1 inhibitors for the treatment of Alzheimer's disease." @default.
- W2132720896 created "2016-06-24" @default.
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- W2132720896 date "2015-10-10" @default.
- W2132720896 modified "2023-10-18" @default.
- W2132720896 title "1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads" @default.
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- W2132720896 doi "https://doi.org/10.1021/acs.jmedchem.5b01101" @default.
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