Parallel synthesis of DAPT derivatives and their γ-secretase-inhibitory activity

…, Y Morohashi, H Natsugari, T Tomita, T Iwatsubo…

Index: Kan, Toshiyuki; Tominari, Yusuke; Rikimaru, Kentaro; Morohashi, Yuichi; Natsugari, Hideaki; Tomita, Taisuke; Iwatsubo, Takeshi; Fukuyama, Tohru Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 8 p. 1983 - 1985

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Citation Number: 34

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).