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Molecules 2017, 22(1), 172; doi:10.3390/molecules22010172

Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase

1
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines & Ministry of Health Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
2
Beijing Institutes For Drug Control, Beijing 100050, China
*
Author to whom correspondence should be addressed.
Academic Editors: Diego Muñoz-Torrero and Derek J. McPhee
Received: 19 October 2016 / Revised: 10 January 2017 / Accepted: 16 January 2017 / Published: 20 January 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [5468 KB, uploaded 20 January 2017]   |  

Abstract

Alzheimer’s disease (AD), the most common form of dementia in adults, is a progressive neurodegenerative disorder of the brain characterized by loss of memory and steady deterioration of cognition. Here, a series of symmetrical molecules containing biphenyl/bibenzyl scaffolds (1236) were designed, synthesized, and evaluated for their ability to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A biological evaluation showed that most of these biphenyl derivatives were potent AChE and BuChE inhibitors. Among them, compound 15 displayed the greatest ability to inhibit BuChE (IC50 = 0.74 µM) and was also a good AChE inhibitor (IC50 = 1.18 µM). Compound 19 was not only a potent AChE inhibitor (IC50 = 0.096 µM), but also a mild BuChE inhibitor (IC50 =1.25 µM). Overall, these results suggested that compound 19 may be a promising agent in the treatment of AD. View Full-Text
Keywords: Alzheimer’s disease; biphenyl/bibenzyl derivatives; acetylcholinesterase inhibitors; butyrylcholinesterase inhibitors; molecular docking Alzheimer’s disease; biphenyl/bibenzyl derivatives; acetylcholinesterase inhibitors; butyrylcholinesterase inhibitors; molecular docking
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Wang, D.-M.; Feng, B.; Fu, H.; Liu, A.-L.; Wang, L.; Du, G.-H.; Wu, S. Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase. Molecules 2017, 22, 172.

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