Design and synthesis of an aminopiperidine series of 纬-secretase modulators
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- 作者：Tomonori Kobayashi ; Seiji Iwama ; Akira Fusano ; Yoshihiro Kato ; Atsushi Ikeda ; Yasuhiro Teranishi ; Akemi Nishihara ; Masanori Tobe
- 关键词：Alzheimer&rsquo ; s disease ; 纬-Secretase modulator ; 纬-Secretase inhibitor ; Amyloid 尾 peptide ; Piperidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：1 January, 2014
- 年：2014
- 卷：24
- 期：1
- 页码：378-381
- 全文大小：1375 K
文摘
The design, synthesis, and SAR of cyclic diamines as novel 纬 secretase modulators (GSMs) are presented in this Letter. Starting from information in the literature and in-house cyclic diamines library, we have found a 3(S)-aminopiperidine as a potent structure for lowering A尾42 production both in vitro and in vivo.