Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373524 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
In this Letter, an efficient strategy for the fast construction of 108 compounds library was developed using click chemistry. The fingerprint of inhibitory activity toward MAO-A/B against this library was obtained, and four hit compounds were identified as selective inhibitors toward MAO-A. Docking study was carried out to demonstrate the binding mode between a9 and MAO-A/B, and the result reveals that a9 localized in the ‘aromatic cage’ and oriented to establish π–π stacking interactions with Tyr407, Tyr444 and FAD in MAO-A rather than in MAO-B.
Graphical abstractAn efficient strategy for the fast construction of 108 compounds library was developed using click chemistry. The fingerprint of inhibitory activity toward MAO-A/B against this library was obtained, and four hit compounds were identified as selective inhibitors toward MAO-A. Docking study was carried out to demonstrate the binding mode between a9 and MAO-A/B, and the result reveals that a9 localized in the ‘aromatic cage’ and oriented to establish π–π stacking interactions with Tyr407, Tyr444 and FAD in MAO-A rather than in MAO-B.Figure optionsDownload full-size imageDownload as PowerPoint slide