Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.

Ping Zhou,Yanfang Li,Yi Fan,Zheng Wang,Rajiv Chopra,Andrea Olland,Yun Hu,Ronald L Magolda,Menelas Pangalos,Peter H Reinhart,M James Turner,Jonathan Bard,Michael S Malamas,Albert J Robichaud

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

A novel class of pyridinyl aminohydantoins was designed and prepared as highly potent BACE1 inhibitors. Compound (S)-4g showed excellent potency with IC50 of 20nM for BACE1. X-ray crystallography indicated that the interaction between pyridine nitrogen and the tryptophan Trp76 was a key feature in the S2′ region of the enzyme that contributed to increased potency.

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关键词

Alzheimer’s disease,β-Secretase,BACE1,Pyridinyl aminohydantoins

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