| Title : Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl\/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase - Wang_2017_Molecules_22_ |
| Author(s) : Wang DM , Feng B , Fu H , Liu AL , Wang L , Du GH , Wu S |
| Ref : Molecules , 22 : , 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 (12-36) 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 microM) and was also a good AChE inhibitor (IC50 = 1.18 microM). Compound 19 was not only a potent AChE inhibitor (IC50 = 0.096 microM), but also a mild BuChE inhibitor (IC50 =1.25 microM). Overall, these results suggested that compound 19 may be a promising agent in the treatment of AD. |
| PubMedSearch : Wang_2017_Molecules_22_ |
| PubMedID: 28117700 |
Wang DM, Feng B, Fu H, Liu AL, Wang L, Du GH, Wu S (2017)
Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl\/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase
Molecules
22 :
Wang DM, Feng B, Fu H, Liu AL, Wang L, Du GH, Wu S (2017)
Molecules
22 :