Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374584 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
A novel class of pyridinyl aminohydantoins was designed and prepared as highly potent BACE1 inhibitors. Compound (S)-4g showed excellent potency with IC50 of 20 nM 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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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,