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Abeta Aggregation inhibitors. Part I: Synthesis and biological activity of phenylazo benzenesulfonamides

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Abeta Aggregation inhibitors. Part I: Synthesis and

biological activity of phenylazo benzenesulfonamides

楊禮明;林淑娟

Lin SJ;Shiao YJ;Chi CW;Yang LM

Abstract

Phenylazo benzenesulfonamides were designed and synthesized as beta-amyloid (Abeta40) fibril assembly inhibitors, and evaluated for inhibition of Abeta40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe(2) group on the end of the phenylazo moiety may play an important role in preventing Abeta40 fibril formation. LB-152 provides a new lead for further development of potential beta-amyloid aggregation inhibitors to treat AD.

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