Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 28, Issue 1, Pages 153-162Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2011.642375
Keywords
BACE-1; N-aryl-thiazoline-2-(thi)ones; ureas; thioureas; Alzheimer disease
Funding
- OSEO - ANVAR [A06 07 008 UAT]
- URMA (Unis pour la Recherche sur la Maladie d'Alzheimer) association
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We report the synthesis and the beta-site amyloid precursor protein cleaving enzyme-1 inhibitory properties of novel phenyl(thio) ureas bearing 2-(thio)oxothiazoline derivatives. A library of analogues was prepared according to specific synthetic schemes and the inhibitory activity was monitored using a fluorescence resonance energy transfer assay. Several analogues show potent inhibitory activities ranging between 1 and 0.01 mu M and the activity is related to the NH acidity of the (thio) urea motif. Our results illustrate once again the close relationship between molecular recognition, complexation of the active site in enzymatic system, and organocatalysis utilizing explicit hydrogen bonding.
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