Journal of Medicinal Chemistry p. 8216 - 8235 (2015)
Update date:2022-08-15
Topics:
Rombouts, Frederik J. R.
Tresadern, Gary
Delgado, Oscar
Martínez-Lamenca, Carolina
Van Gool, Michiel
García-Molina, Aránzazu
Alonso De Diego, Sergio A.
Oehlrich, Daniel
Prokopcova, Hana
Alonso, José Manuel
Austin, Nigel
Borghys, Herman
Van Brandt, Sven
Surkyn, Michel
De Cleyn, Michel
Vos, Ann
Alexander, Richard
Macdonald, Gregor
Moechars, Dieder
Gijsen, Harrie
Trabanco, Andrés A.
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 permi
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