| Title : Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and beta-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease - Xu_2018_Bioorg.Med.Chem_26_1885 |
| Author(s) : Xu R , Xiao G , Li Y , Liu H , Song Q , Zhang X , Yang Z , Zheng Y , Tan Z , Deng Y |
| Ref : Bioorganic & Medicinal Chemistry , 26 :1885 , 2018 |
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Abstract :
A series of 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives were designed, synthesized and evaluated as potential multifunctional agents for the treatment of Alzheimer's disease (AD). The in vitro assays indicated that most of these derivatives were selective AChE inhibitors with good multifunctional properties. Among them, compounds 11b and 11d displayed comprehensive advantages, with good AChE (IC50=0.29+/-0.01muM and 0.46+/-0.02muM, respectively), MAO-A (IC50=8.2+/-0.08muM and 7.9+/-0.07muM, respectively) and MAO-B (IC50=20.1+/-0.16muM and 43.8+/-2.0% at 10muM, respectively) inhibitory activities, moderate self-induced Abeta1-42 aggregation inhibitory potency (35.4+/-0.42% and 48.0+/-1.53% at 25muM, respectively) and potential antioxidant activity. In addition, the two representative compounds displayed high BBB permeability in vitro. Taken together, these multifunctional properties make 11b and 11d as a promising candidate for the development of efficient drugs against AD. |
| PubMedSearch : Xu_2018_Bioorg.Med.Chem_26_1885 |
| PubMedID: 29500132 |
Xu R, Xiao G, Li Y, Liu H, Song Q, Zhang X, Yang Z, Zheng Y, Tan Z, Deng Y (2018)
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and beta-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease
Bioorganic & Medicinal Chemistry
26 :1885
Xu R, Xiao G, Li Y, Liu H, Song Q, Zhang X, Yang Z, Zheng Y, Tan Z, Deng Y (2018)
Bioorganic & Medicinal Chemistry
26 :1885