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[摘要]:4-Aryl-2(1H)-quinolinones were synthesized and evaluated in vitro as inhibitors of A beta(1-42) 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' (R-4) and/or C-6 (R-2) of the 4-aryl-2(1H)-quinolinone moiety. Furthermore, the derivative bearing 4'-F substituent (4f) proved to be a very active inhibitor. |
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