Title : Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.

Pub. Date : 2018 Jul 12

PMID : 29775538






2 Functional Relationships(s)
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1 Changing to a pyrazine followed by optimization of substituents on both the oxazine and the pyrazine culminated in 24 with robust Abeta reduction in vivo at low doses as well as reduced CYP2D6 inhibition. Pyrazines cytochrome P450 family 2 subfamily D member 6 Homo sapiens
2 Changing to a pyrazine followed by optimization of substituents on both the oxazine and the pyrazine culminated in 24 with robust Abeta reduction in vivo at low doses as well as reduced CYP2D6 inhibition. Pyrazines cytochrome P450 family 2 subfamily D member 6 Homo sapiens