Screening cholinesterase inhibitory potential of selected amines

Açelya Mavideniz, Tuğba Erçetin, Aybike Yektaoglu, Zahra Nobavar, Jale Yuzugulen, Emine Dilek Özyılmaz, H. O. Gülcan
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Abstract

Cholinesterase inhibition has gained attention in the treatment of some disease states, covering cholinergic deficiency. Alzheimer’s disease (AD) can be counted as the most important one among them. Indeed, the current drugs used in the treatment of AD are cholinesterase inhibitor molecules, besides memantine, and biological new drugs. Many pharmacophores have been suggested so far for cholinesterase inhibition and many of them possess a basic center with an amine function. Within this work, we have selected some simple amines and investigated their potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes. The results indicated that simple amines by themselves don’t have strong potential unless they are used with other pharmacophores.
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筛选某些胺类的胆碱酯酶抑制潜力
胆碱酯酶抑制剂在治疗某些胆碱能缺乏的疾病方面受到了关注。阿尔茨海默病(AD)可以说是其中最重要的一种。事实上,目前用于治疗阿尔茨海默病的药物除了美金刚外,还有胆碱酯酶抑制剂分子和生物新药。迄今为止,已有许多抑制胆碱酯酶的药理作用被提出,其中许多药理作用都具有带胺功能的碱性中心。在这项工作中,我们选择了一些简单的胺,并研究了它们抑制乙酰胆碱酯酶和丁酰胆碱酯酶的潜力。结果表明,除非与其他药剂一起使用,否则单胺本身并不具有很强的潜力。
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