- The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease
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A series of 2-acetylphenol-donepezil hybrids was designed and synthesized based on multi-target-directed ligands strategy. The biological activities were evaluated by AChE/BChE inhibition and MAO-A/MAO-B inhibition. The results revealed that the tertiary
- Zhu, Gaofeng,Wang, Keren,Shi, Jian,Zhang, Pengfei,Yang, Dan,Fan, Xiaotian,Zhang, Ziyi,Liu, Wenmin,Sang, Zhipei
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supporting information
(2019/08/26)
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- Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease
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A series of 2-acetyl-5-O-(amino-alkyl)phenol derivatives was designed, synthesized and evaluated as multi-function inhibitors for the treatment of Alzheimer's disease (AD). The results revealed that compound TM-3 indicated selective AChE inhibitory potenc
- Sang, Zhipei,Wang, Keren,Wang, Huifang,Wang, Huijuan,Ma, Qianwen,Han, Xue,Ye, Mengyao,Yu, Lintao,Liu, Wenmin
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supporting information
p. 5046 - 5052
(2017/10/20)
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- Chemical compounds
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There are provided compounds of formula I, STR1 wherein R1, R2, R3, R4, R5 and R7 may be the same or different, and are hydrogen, hydroxy, alkoxy, alkoxy substituted by phenyl, acyl, amino, acylamino, alkenyl, halogen, or alkyl, provided that at least one of R1, R2, R3 and R7 are other than hydrogen and hydroxy, Or an adjacent pair of R1, R2, R3 and R7 represent a chain --COCH=CH--O--, X is a hydrocarbon chain containing from 2 to 10 carbon atoms and optionally substituted by a hydroxy group, and E is a carboxy group or a tetrazole group, And pharmaceutically acceptable derivatives thereof. The compounds are indicated for use as antagonists of SRS-A.
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