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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 12
BKCSDE 29(12)
December 20, 2008 

Synthesis of Thia(oxa)zolopyridines and Their Inhibitory Activities for β-Amyloid Fibrillization
Yeo Ran Lee, Dong Jin Kim, Inhee Mook Jung, Kyung Ho Yoo*
Alzheimer’s disease, β-Amyloid fibrillization, Thia(oxa)zolopyridines, Binding affinity
A series of thiazolo[5,4-b]pydine and oxazolo[5,4-b]pyridine derivatives 1a-o were designed. These fifteen compounds were evaluated by Aβ42 fibril formation inhibitory assay using thioflavin T as a dye. Thiazolo[5,4- b]pyridines 1a-g showed potent inhibitory activities for Aβ42 fibrillization at IC50 of 0.23-4.5 μM. Among them, compounds 1b and 1k having methoxy group at C-5 exhibited excellent activities (IC50 = 0.23 and 0.50 μM, respectively) than that of Curcumin (IC50 = 0.80 μM).
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