Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic

作者：Wangsell Fredrik; Russo Francesco; Savmarker Jonas; Rosenquist Asa; Samuelsson Bertil; Larhed Mats^*

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(16): 4711-4714.

DOI：10.1016/j.bmcl.2009.06.065

• Alzheimer's disease
• BACE-1
• Enzyme inhibitor
• Transition state mimetic

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 IC(50) value of 0.23 mu M.

• 出版日期2009-8-15