Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Aβ 1–42 aggregation …

…, JH Yang, TY Shin, DK Kim, BS Chae, JY Leem…

Index: Kwon, Young Ee; Park, Jung Youl; No, Kyung Tai; Shin, Jae Hong; Lee, Sung Kwang; Eun, Jae Soon; Yang, Jae Heon; Shin, Tae Yong; Kim, Dae Keun; Chae, Byung Sook; Leem, Jae-Yoon; Kim, Kuk Hwan Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 20 p. 6596 - 6607

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Citation Number: 69

Abstract

With the goal of developing Alzheimer's disease therapeutics, we have designed and synthesized new piperidine derivatives having dual action of acetylcholinesterase (AChE) and beta-amyloid peptide (Aβ) aggregation inhibition. For binding with the catalytic site of AChE, an ester with aromatic group was designed, and for the peripheral site, another aromatic group was considered. And for intercalating amyloid-beta oligomerization, long ...