Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease

Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease

Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer’s disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the synthesised compounds, 15b and 15j showed submicromolar IC50...

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Bibliographic Details
Main Authors: Jun Mo, Tingkai Chen, Hongyu Yang, Yan Guo, Qi Li, Yuting Qiao, Hongzhi Lin, Feng Feng, Wenyuan Liu, Yao Chen, Zongliang Liu, Haopeng Sun
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
alzheimer’s disease
cholinesterase inhibitor
1,3-dimethylbenzimidazolinone derivatives
molecular docking
structural modification
structure-activity relationship
Online Access:http://dx.doi.org/10.1080/14756366.2019.1699553

Internet

http://dx.doi.org/10.1080/14756366.2019.1699553

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