444646-05-3Relevant academic research and scientific papers
Design, Synthesis and Structure-Activity Relationships of Dual Inhibitors of Acetylcholinesterase and Serotonin Transporter as Potential Agents for Alzheimer's Disease
Toda, Narihiro,Tago, Keiko,Marumoto, Shinji,Takami, Kazuko,Ori, Mayuko,Naho, Yamada,Koyama, Kazuo,Naruto, Shunji,Abe, Kazumi,Yamazaki, Reina,Hara, Takao,et al.
, p. 1936 - 1956 (2007/10/03)
We have designed and synthesized a dual inhibitor of acetylcholinesterase (AChE) and serotonin transporter (SERT) as a novel class of treatment drugs for Alzheimer's disease on the basis of a hypothetical model of the AChE active site. Dual inhibitions of AChE and SERT would bring about greater therapeutic effects than AChE inhibition alone and avoid adverse peripheral effects caused by excessive AChE inhibition. Compound (S)-6j exhibited potent inhibitory activities against AChE (IC50 = 101 nM) and SERT (IC50 = 42 nM). Furthermore, (S)-6j showed inhibitory activities of both AChE and SERT in mice brain following oral administration.
BENZYLAMINE ANALOGUE
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Page/Page column 72, (2008/06/13)
A compound of the formula (I): [wherein R1 represents a C1-C6 alkyl group etc., R2 and R3 are the same or different and represent a hydrogen atom etc., Ra represents a C1-C6 alkyl group etc., Arom represents an aryl group etc., A represents a C1-C6 alkylene group, E represents a single bond, an oxygen atom, a sulfur atom etc., X1 and X2 are the same or different and represent an oxygen atom or a sulfur atom] or a pharmacologically acceptable salt or ester thereof.
