药效团
胆碱酯酶
丁酰胆碱酯酶
氨基甲酸酯
乙酰胆碱酯酶
药理学
化学
药品
组合化学
酶
生物化学
医学
阿切
作者
Lucia Ungvarská Maľučká,Jozef Csöllei
出处
期刊:Chemicke Listy
[Czech Chemical Society]
日期:2022-06-10
卷期号:116 (6): 372-380
摘要
The work deals with the design, synthesis and biological activity of new carbamate cholinesterase inhibitors. It is focused on selected syntheses of new carbamate derivatives, which were tested for their anticholinesterase activity against acetylcholinesterase as well as butyrylcholinesterase. Despite various theories in the pathogenesis of Alzheimer's disease, drugs that can inhibit these two enzymes still represent the major approach to the treatment of this neurodegenerative disease. Many of the newly synthesized compounds have unique chemical structure. Recently, the approach to the synthesis of new cholinesterase inhibitors has focused on the preparation of potential drugs, containing in their chemical structure fragments of already known drugs, commonly used in the pharmacotherapy of Alzheimer's disease, but also other diseases. The aim of preparing these compounds is to affect several biological systems simultaneously. These multipotent compounds have been termed "multi-target-directed ligands"; the molecules of drugs used to treat Alzheimer's disease always contain a pharmacophore acting as a cholinesterase inhibitor, which represents the mainstay of therapy.
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