| Title : Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties - Li_2017_Bioorg.Med.Chem_25_714 |
| Author(s) : Li Y , Qiang X , Luo L , Yang X , Xiao G , Zheng Y , Cao Z , Sang Z , Su F , Deng Y |
| Ref : Bioorganic & Medicinal Chemistry , 25 :714 , 2017 |
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Abstract :
A series of homoisoflavonoid Mannich base derivatives were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease. It demonstrated that most of the derivatives were selective AChE and MAO-B dual inhibitors with good multifunctional properties. Among them, compound 10d displayed the comprehensive advantages, with excellent AChE and MAO-B inhibitory activities (IC50=2.49+/-0.08nM and 1.74+/-0.0581muM, respectively), good self- and Cu2+-induced Abeta1-42 aggregation inhibitory potency, antioxidant activity, biometal chelating ability and high BBB permeability. These multifunctional properties make 10d as an excellent candidate for the development of efficient drugs against AD. |
| PubMedSearch : Li_2017_Bioorg.Med.Chem_25_714 |
| PubMedID: 27923535 |
Li Y, Qiang X, Luo L, Yang X, Xiao G, Zheng Y, Cao Z, Sang Z, Su F, Deng Y (2017)
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties
Bioorganic & Medicinal Chemistry
25 :714
Li Y, Qiang X, Luo L, Yang X, Xiao G, Zheng Y, Cao Z, Sang Z, Su F, Deng Y (2017)
Bioorganic & Medicinal Chemistry
25 :714