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KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine
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Description
Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as a transition-state mimic. Using KMI-008 as a lead compound, a small-sized and highly potent BACE1 inhibitor KMI-370 (IC(50)=3.4 nM) was designed and synthesized.
Journal
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- Bioorganic & Medicinal Chemistry Letters
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Bioorganic & Medicinal Chemistry Letters 14 (6), 1527-1531, 2004-03
Elsevier BV