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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2017
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Abstract
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 potency (eeAChE, IC = 0.69 μM, selective index (SI) = 32.7). Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-3 could simultaneously bind to the catalytic active site and peripheral anionic site of AChE. And TM-3 was also a highly selective MAO-B inhibitor (IC = 6.8 μM). Moreover, TM-3 could act as antioxidant (ORAC value was 1.5eq) and neuroprotectant, as well as a selective metal chelating agent. More interestingly, compound TM-3 could cross the blood-brain barrier (BBB) in vitro and abided by Lipinski's rule of five. Therefore, compound TM-3, a promising multi-targeted active molecule, offers an attractive starting point for further lead optimization in the drug-discovery process against AD.
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Autoren Sang, Zhipei;Wang, Keren;Wang, Huifang;Wang, Huijuan;Ma, Qianwen;Han, Xue;Ye, Mengyao;Yu, Lintao;Liu, Wenmin;
Zeitschrift Bioorganic & medicinal chemistry letters
Jahr 2017
DOI
S0960-894X(17)30966-6
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Schlüsselwörter
alzheimer’s disease blood-brain barrier 2-acetyl-5-o-(amino-alkyl)phenol derivatives designed multi-target inhibitor synthesized

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