Discovery of novel quinolin-2-one derivatives as potential GSK-3β inhibitors for treatment of Alzheimer's disease: Pharmacophore-based design, preliminary SAR, in vitro and in vivo biological evaluation.

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第一作者： Esraa,Abdo Moustafa

第一单位： Egyptian Drug Authority (EDA), 51 Wezaret El-Zeraa St., Giza 35521, Egypt.

作者： Esraa,Abdo Moustafa ^[1] ; Heba,Abdelrasheed Allam ^[2] ; Marwa A,Fouad ^[3] ; Ahmed M,El Kerdawy ^[4] ; Nahed,Nasser Eid El-Sayed ^[1] ; Christoph,Wagner ^[5] ; Hatem A,Abdel-Aziz ^[6] ; Manal,Abdel Fattah Ezzat ^[7]

作者单位： Egyptian Drug Authority (EDA), 51 Wezaret El-Zeraa St., Giza 35521, Egypt. ^[1] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, 11562 Cairo, Egypt. ^[2] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, 11562 Cairo, Egypt; Pharmaceutical Chemistry Department, School of Pharmacy, Newgiza University, Newgiza, km 22 Cairo- Alexandria Desert Road, Cairo, Egypt. ^[3] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, 11562 Cairo, Egypt; School of Pharmacy, College of Health and Science, University of Lincoln, Joseph Banks Laboratories, Green Lane, Lincoln, United Kingdom. ^[4] Institut für Chemie, Naturwissenschaftliche FakultätII, Universität Halle, Kurt-Mothes-Str. 206120, Halle, Germany. ^[5] Department of Applied Organic Chemistry, National Research Center, Dokki, Giza, P.O. Box 12622, Egypt. ^[6] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, 11562 Cairo, Egypt. Electronic address: Manal.salem@pharma.cu.edu.eg. ^[7]

关键词 Alzheimer’s disease Glycogen synthase kinase inhibitor Quinolin-2-one Tau hyperphosphorylation, ADME

主题词人类(Humans);动物(Animals);小鼠(Mice);阿尔茨海默病(Alzheimer Disease);神经母细胞瘤(Neuroblastoma);磷酰化(Phosphorylation);tau蛋白质类(tau Proteins)

DOI 10.1016/j.bioorg.2024.107324

PMID 38569322

发布时间 2024-04-15

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