| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376279 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
A novel norstatine derivative, phenylthionorstatine [(2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid; Ptns], containing a hydroxymethylcarbonyl (HMC) isostere was designed, synthesized, and stereochemically determined. Then, Ptns was introduced into the structure of BACE1 inhibitors at the P1 position. Finally, Ptns was found as a suitable P1 moiety for potent BACE1 inhibitor design.
Graphical abstractA novel norstatine derivative, phenylthionorstatine [(2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid; Ptns], was designed and synthesized. Then, Ptns was introduced into the structure of designed BACE1 inhibitors at the P1 position.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zyta Ziora, Soko Kasai, Koushi Hidaka, Ayaka Nagamine, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso,