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• W1991069944 abstract "We have identified macrocyclic inhibitors of the aspartic protease BACE, implicated in the etiology of Alzheimer's disease. An X-ray structure of screening hit 1 in the BACE active site revealed a hairpin conformation suggesting that constrained macrocyclic derivatives may also bind there. Several of the analogs we prepared were >100x more potent than 1, such as 7 (5 nM K(i))." @default.
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• W1991069944 date "2010-05-01" @default.
• W1991069944 modified "2023-10-16" @default.
• W1991069944 title "Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads" @default.
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• W1991069944 doi "https://doi.org/10.1016/j.bmcl.2010.03.097" @default.
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