| Title : Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease - Xiao_2017_Bioorg.Med.Chem_25_1030 |
| Author(s) : Xiao G , Li Y , Qiang X , Xu R , Zheng Y , Cao Z , Luo L , Yang X , Sang Z , Su F , Deng Y |
| Ref : Bioorganic & Medicinal Chemistry , 25 :1030 , 2017 |
| Abstract : A series of 4'-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50=4.91muM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic analysis of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Abeta1-42 aggregation and Cu2+-induced Abeta1-42 aggregation by 89.5% and 79.7% at 25muM respectively, as well as acted as a selective monoamine oxidase B inhibitor (IC50=0.29muM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer's disease. |
| ESTHER : Xiao_2017_Bioorg.Med.Chem_25_1030 |
| PubMedSearch : Xiao_2017_Bioorg.Med.Chem_25_1030 |
| PubMedID: 28011206 |
Xiao G, Li Y, Qiang X, Xu R, Zheng Y, Cao Z, Luo L, Yang X, Sang Z, Su F, Deng Y (2017)
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease
Bioorganic & Medicinal Chemistry
25 :1030
Xiao G, Li Y, Qiang X, Xu R, Zheng Y, Cao Z, Luo L, Yang X, Sang Z, Su F, Deng Y (2017)
Bioorganic & Medicinal Chemistry
25 :1030