Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC50 value of 0.23 μM. © 2009 Elsevier Ltd. All rights reserved.
CITATION STYLE
Wångsell, F., Russo, F., Sävmarker, J., Rosenquist, Å., Samuelsson, B., & Larhed, M. (2009). Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic. Bioorganic and Medicinal Chemistry Letters, 19(16), 4711–4714. https://doi.org/10.1016/j.bmcl.2009.06.065
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