Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.

Jiang, Xueyang; Zhou, Junting; Wang, Yang; Chen, Lei; Duan, Yan; Huang, Jianping; Liu, Chang; Chen, Yao; Liu, Wenyuan; Sun, Haopeng; Feng, Feng; Qu, Wei

Jiang, Xueyang; Zhou, Junting; Wang, Yang; Chen, Lei; Duan, Yan; Huang, Jianping; Liu, Chang; Chen, Yao; Liu, Wenyuan; Sun, Haopeng; Feng, Feng; Qu, Wei.

Afiliação

Jiang X; Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 211198, China.
Zhou J; Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 211198, China.
Wang Y; Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, 211198, China.
Chen L; School of Pharmacy, Gannan Medical University, Ganzhou, 341000, China.
Duan Y; School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.
Huang J; School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.
Liu C; Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, 211198, China.
Chen Y; School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Liu W; Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, 211198, China.
Sun H; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 211198, China.
Feng F; Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 211198, China; Jiangsu Food and Pharmaceutical Science College, No.4 Meicheng Road, Huai'an, 223003, China.
Qu W; Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 211198, China. Electronic address: popoqzh@126.com.

Eur J Med Chem ; 207: 112751, 2020 Dec 01.

Article em En | MEDLINE | ID: mdl-32950908

Assuntos

Acetilcolinesterase/metabolismo; Acridinas/química; Acridinas/farmacologia; Doença de Alzheimer/tratamento farmacológico; Desenho de Fármacos; Quinase 3 da Glicogênio Sintase/antagonistas & inibidores; Tiazóis/química; Acridinas/metabolismo; Acridinas/uso terapêutico; Doença de Alzheimer/metabolismo; Animais; Barreira Hematoencefálica/metabolismo; Inibidores da Colinesterase/química; Inibidores da Colinesterase/metabolismo; Inibidores da Colinesterase/farmacologia; Inibidores da Colinesterase/uso terapêutico; Relação Dose-Resposta a Droga; Camundongos; Simulação de Acoplamento Molecular; Terapia de Alvo Molecular; Teste do Labirinto Aquático de Morris/efeitos dos fármacos; Fosforilação/efeitos dos fármacos; Conformação Proteica; Proteínas tau/metabolismo

Palavras-chave

Acetylcholinesterase; Alzheimer's disease; Glycogen synthase kinase3ß; Multi-target-directed ligands

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Acetilcolinesterase / Tiazóis / Acridinas / Desenho de Fármacos / Quinase 3 da Glicogênio Sintase / Doença de Alzheimer Idioma: En Ano de publicação: 2020 Tipo de documento: Article

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