一些新型 N'-(喹啉-4-亚甲基)丙酰肼的合成及其对阿尔茨海默病的胆碱酯酶抑制和抗氧化能力研究

IF 3.5 4区 医学 Q2 CHEMISTRY, MEDICINAL
Burcu Kilic, Deniz S. Dogruer
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引用次数: 0

摘要

阿尔茨海默病(AD)是过去几十年来最严重的长期健康问题之一。遗憾的是,目前治疗和护理阿尔茨海默病的选择并不充分,因此成为药物开发研究的热门课题。有关 AD 药物开发的研究主要集中在多靶点定向配体的使用上。根据这一策略,我们设计了具有额外抗氧化和金属螯合作用的新型 ChE 抑制剂。在这项研究中,我们合成并鉴定了 8 种新型 N'-(喹啉-4-基亚甲基)丙烷肼衍生物。然后,我们评估了所有最终化合物对胆碱酯酶的抑制效力。结果发现,4e(IC50 乙酰胆碱酯酶[AChE] = 0.69 µM,丁酰胆碱酯酶[BChE] = 26.00 µM)和 4h(IC50 的 AChE= 7.04 µM,BChE= 16.06 µM)分别是最有效的 AChE 和 BChE 抑制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis and investigation of the cholinesterase inhibitory and antioxidant capacities of some novel N'-(quinolin-4-ylmethylene)propanehydrazides against Alzheimer's disease

Synthesis and investigation of the cholinesterase inhibitory and antioxidant capacities of some novel N'-(quinolin-4-ylmethylene)propanehydrazides against Alzheimer's disease

One of the worst long-term health issues of the past few decades is Alzheimer's disease (AD). Unfortunately, there are currently insufficient choices for treating and caring for AD, which makes it a popular subject for drug development research. Studies on the development of drugs for AD have primarily concentrated on the use of multitarget directed ligands. Following this strategy, we designed new ChE inhibitors with additional antioxidant and metal chelator effects. In this research, eight novel N’-(quinolin-4-ylmethylene)propanehydrazide derivatives were synthesized and characterized. We then evaluated the inhibition potency of all the final compounds for cholinesterase enzymes. Among them, 4e (IC50 acetylcholinesterase [AChE] = 0.69 µM and butyrylcholinesterase [BChE]= 26.00 µM) and 4h (IC50's AChE= 7.04 µM and BChE= 16.06 µM) were found to be the most potent AChE and BChE inhibitors, respectively.

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来源期刊
CiteScore
6.40
自引率
2.60%
发文量
104
审稿时长
6-12 weeks
期刊介绍: Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.
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