4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1

Ajit Dhananjay Jagtap,Nagendra B. Kondekar,Pei-Yun Hung,Chen-En Hsieh,Chia-Ron Yang,Grace Shiahuy Chen,Ji-Wang Chern

Bioorganic Chemistry（2020）

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摘要

•A novel class of dihydroquinazolines was designed and synthesized to inhibit BACE1.•Key strategy: Relocating the hairpin side-chain α-hydrophobic moiety to position C4 on dihydroquinazolines.•Compound 22a and 22b strongly inhibited BACE1 (CFA, IC50 = 0.38 and 0.49 μM; WCA IC50 = 0.14 and 0.14 μM).

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关键词

Alzheimer’s disease,BACE-1,Non-peptidic aspartyl protease inhibitors,2-amino-3,4-dihydroquinazolines,Structure-activity relationship

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