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Paper | Regular issue | Vol 85, No. 8, 2012, pp.1933-1940
Published online, 15th June, 2012
DOI: 10.3987/COM-12-12506
Synthesis and Evaluation of 4-Aryl-2(1H)-quinolinones as Potent Amyloid β Fibrillogenesis Inhibitors

Yoko Shimokawa, Masamichi Nakakoshi, Setsu Saito, Hideharu Suzuki, Yuusaku Yokoyama, Akihito Ishigami, Hideo Nishioka, and Masayoshi Tsubuki*

*Institute of Medicinal Chemistry, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan

Abstract

4-Aryl-2(1H)-quinolinones were synthesized and evaluated in vitro as inhibitors of Aβ1-42 fibrillogenesis using a thioflavin T fluorescence method. The most potent anti-aggregating molecules (4b and 5c) were found among the derivatives bearing OH and/or OMe groups at C-4’ (R4) and/or C-6 (R2) of the 4-aryl-2(1H)-quinolinone moiety. Furthermore, the derivative bearing 4’-F substituent (4f) proved to be a very active inhibitor.