title: Synthesis and evaluation of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) as effective inhibitor of metal-induced Aβ aggregation and antioxidant.
abstract: A series of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) at the 2-position were synthesized and evaluated for treatment of Alzheimer's disease. In vitro assays demonstrated that most of the target compounds exhibit significant inhibition of Cu(II)-induced Aβ1-42 aggregation, rapid H2O2 scavenging and glutathione peroxidise (GPx)-like catalytic activity. Among these molecules, compound 9a is the most potent peroxide scavenger that possesses the ability to scavenge most H2O2 within 200-220min and possesses GPx-like activity (v0=106.0μM·min(-1)), enabling modulation of metal-induced Aβ aggregation.
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
authors: Bo
authors: B
authors: Wang
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
authors: Zhiren
authors: Z
authors: Wang
authors: College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
authors: Hong
authors: H
authors: Chen
authors: College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China. Electronic address: luchuanjun@zjut.edu.cn.
authors: Chuan-Jun
authors: CJ
authors: Lu
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: lixsh@mail.sysu.edu.cn.
authors: Xingshu
authors: X
authors: Li
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000975:Antioxidants / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001812:Blood-Brain Barrier / Q000378:metabolism; D003300:Copper / Q000378:metabolism*; D015195:Drug Design; D006801:Humans; D006912:Hydroxyquinolines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D008567:Membranes, Artificial; D010446:Peptide Fragments / Q000037:antagonists & inhibitors / Q000378:metabolism*; D066329:Protein Aggregates / Q000187:drug effects*
chemical_list: D016229:Amyloid beta-Peptides; D000975:Antioxidants; D006912:Hydroxyquinolines; D008567:Membranes, Artificial; D010446:Peptide Fragments; D066329:Protein Aggregates; C075222:amyloid beta-protein (1-42); D003300:Copper
keywords: Alzheimer’s disease; Antioxidant activity; Aβ aggregation; GPx-like activity; Multitarget; Organoselenium