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2005
Oxazine derivatives
R 0595
A Novel Series of Potent γ-Secretase Inhibitors Based on a BenzobicycCore. — Lead optimization studies on the screening hit (Ia) based on
20- 160 lo[4.2.1]nonane
a benzobicyclononane core lead to the development of a series of potent γ-secretase
inhibitors. In particular, derivatives bearing a terminal N-morpholino substituent in the
p-position of the aromatic ring give rise to very potent compounds. — (LEWIS*, S.
J.; et al.; Bioorg. Med. Chem. Lett. 15 (2005) 2, 373-378; Merck Sharp Dohme Res.
Lab., Dep. Med. Chem., Neurosci. Res. Cent., Harlow, Essex CM20 2QR, UK; Eng.)
— R. Staver
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