Tacrines as Therapeutic Agents for Alzheimer's Disease. V. Recent Developments

被引：20

作者：

Bautista-Aguilera, Oscar M. ^{[1
]}

Ismaili, Lhassane ^{[2
]}

Iriepa, Isabel ^{[1
,3
]}

Diez-Iriepa, Daniel ^{[1
]}

Chabchoub, Fakher ^{[4
]}

Marco-Contelles, Jose ^{[5
]}

Perez, Marta ^{[6
]}

机构：

[1] Univ Alcala, Dept Quim Organ & Quim Inorgan, Ctra Madrid Barcelona,Km 33,6, Madrid 28871, Spain

[2] Univ Bourgogne Franche Comte, Lab Chim Organ & Therapeut, Neurosci Integrat & Clin EA 481, UFR Sante, 19 Rue Ambroise Pare, F-25000 Besancon, France

[3] Alcala Univ, Inst Chem Res Andres M del Rio, Madrid 28805, Spain

[4] Univ Sfax, Lab Chim Appl Heterocycles Corps Gras & Polymeres, Fac Sci Sfax, BP 802, Sfax 3000, Tunisia

[5] CSIC, Lab Med Chem IQOG, Juan de la Cierva 3, Madrid 28006, Spain

[6] Univ Basque Country, Publ Hlth Dept, Fac Med & Nursing, Leioa, Spain

来源：

CHEMICAL RECORD | 2021年 / 21卷 / 01期

关键词：

Alzheimer' s disease; Cholinesterase inhibition; Friedlä nder reaction; Hepatotoxicity; Tacrine derivatives; BIOLOGICAL ASSESSMENT; DIRECTED LIGANDS; SENILE DEMENTIA; ACETYLCHOLINESTERASE; INHIBITORS; DRUGS; FLUORESCEIN; MELATONIN; HYBRIDS; DESIGN;

D O I：

10.1002/tcr.202000107

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Herein we have reviewed our recent developments for the identification of new tacrine analogues for Alzheimer's disease (AD) therapy. Tacrine, the first cholinesterase inhibitor approved for AD treatment, did not stop the progression of AD, producing only some cognitive improvements, but exhibited secondary effects mainly due to its hepatotoxicity. Thus, the drug was withdrawn from the clinics administration. Since then, many publications have described non-hepatotoxic tacrines, and in addition, important efforts have been made to design multitarget tacrines by combining their cholinesterase inhibition profile with the modulation of other biological targets involved in AD.

引用

页码：162 / 174

页数：13

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