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Tacrines as Therapeutic Agents for Alzheimer's Disease. V. Recent Developments
The Chemical Record ( IF 6.6 ) Pub Date : 2020-11-10 , DOI: 10.1002/tcr.202000107
Óscar M Bautista-Aguilera 1 , Lhassane Ismaili 2 , Isabel Iriepa 1, 3 , Daniel Diez-Iriepa 1 , Fakher Chabchoub 4 , José Marco-Contelles 5 , Marta Pérez 6
Affiliation  

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 Thus, the drug was withdrawn from the clinics administration.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.

中文翻译:

Tacrines作为阿尔茨海默氏病的治疗剂。五,最新动态

本文中,我们回顾了我们在鉴定新的他克林类似物用于阿尔茨海默氏病(AD)治疗方面的最新进展。他克林是首个获准用于AD治疗的胆碱酯酶抑制剂,并未停止AD的进展,仅产生了一些认知改善,但主要由于其肝毒性而表现出次要作用。因此,该药物从诊所行政部门撤回。从那时起,许多出版物描述了非肝毒性他克瑞,此外,人们还通过结合胆碱酯酶抑制谱和与AD相关的其他生物靶标的调节,来设计多目标他克瑞。
更新日期:2020-11-10
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