کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373524 | 981901 | 2010 | 4 صفحه PDF | دانلود رایگان |
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.
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.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 21, 1 November 2010, Pages 6222–6225