Synthesis and evaluation of 4-aryl-2(1H)-quinolinones as potent amyloid β fibrillogenesis inhibitors

Article abstract of DOI:10.3987/COM-12-12506

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.