Parallel synthesis of DAPT derivatives and their gamma-secretase-inhibitory activity |
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| Authors: | Kan Toshiyuki Tominari Yusuke Rikimaru Kentaro Morohashi Yuichi Natsugari Hideaki Tomita Taisuke Iwatsubo Takeshi Fukuyama Tohru |
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| Affiliation: | Graduate School of Pharmaceutical Sciences, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan. |
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| Abstract: | Parallel synthesis of the C-terminal-modified DAPT (1) derivatives was accomplished utilizing our novel resin 7. Condensation reaction of the N-acylamino acid 10 with the amines 11a-o proceeded smoothly to give the corresponding amides 6a-o without any epimerization. Among the analogues, the benzophenonemethyl amide derivative 6o showed 30 times more potent activity than the original DAPT (1). |
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