New Series of Antiprion Compounds: Pyrazolone Derivatives Have the Potent Activity of Inhibiting Protease-Resistant Prion Protein Accumulation
Journal of Medicinal Chemistry2007Vol. 50(21), pp. 5053–5056
Citations Over TimeTop 10% of 2007 papers
Ayako Kimata, Hidehiko Nakagawa, Ryo Ohyama, Tomoko Fukuuchi, Shigeru Ohta, Takayoshi Suzuki, Naoki Miyata
Abstract
To find effective antiprion compounds, we synthesized and evaluated various pyrazolone derivatives. Seven of 19 compounds showed inhibition of PrP-res accumulation and the remarkably active compound 13 showed an IC50 value of 3 nM in both ScN2a and F3 cell lines. Findings from studies on physicochemical and biochemical properties suggest that the action mechanism of these compounds does not correlate with any antioxidant activities, any of hydroxyl radical scavenging activities, or any SOD-like activities.
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