Song_2018_Bioorg.Med.Chem_26_6115

Reference

Title : Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease - Song_2018_Bioorg.Med.Chem_26_6115
Author(s) : Song Q , Li Y , Cao Z , Liu H , Tian C , Yang Z , Qiang X , Tan Z , Deng Y
Ref : Bioorganic & Medicinal Chemistry , 26 :6115 , 2018
Abstract :

A series of 2,5-dihydroxyterephthalamide derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease. In vitro assays demonstrated that most of the derivatives exhibited good multifunctional activities. Among them, compound 9d showed the best inhibitory activity against both RatAChE and EeAChE (IC50=0.56muM and 5.12muM, respectively). Moreover, 9d exhibited excellent inhibitory effects on self-induced Abeta1-42 aggregation (IC50=3.05muM) and Cu(2+)-induced Abeta1-42 aggregation (71.7% at 25.0muM), and displayed significant disaggregation ability to self- and Cu(2+)-induced Abeta1-42 aggregation fibrils (75.2% and 77.2% at 25.0muM, respectively). Furthermore, 9d also showed biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activities and appropriate BBB permeability. These multifunctional properties highlight 9d as promising candidate for further studies directed to the development of novel drugs against AD.

PubMedSearch : Song_2018_Bioorg.Med.Chem_26_6115
PubMedID: 30470598

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Citations formats

Song Q, Li Y, Cao Z, Liu H, Tian C, Yang Z, Qiang X, Tan Z, Deng Y (2018)
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease
Bioorganic & Medicinal Chemistry 26 :6115

Song Q, Li Y, Cao Z, Liu H, Tian C, Yang Z, Qiang X, Tan Z, Deng Y (2018)
Bioorganic & Medicinal Chemistry 26 :6115