作为乙酰胆碱酯酶抑制剂的新型 1H-苯并[d]咪唑-1-基衍生物的设计、合成、表征和初步评估

Shuhad Yaseen, S. Z. Abdul-Majeed, Sarah Ashour Hamood
{"title":"作为乙酰胆碱酯酶抑制剂的新型 1H-苯并[d]咪唑-1-基衍生物的设计、合成、表征和初步评估","authors":"Shuhad Yaseen, S. Z. Abdul-Majeed, Sarah Ashour Hamood","doi":"10.54133/ajms.v7i1.794","DOIUrl":null,"url":null,"abstract":"Background: Alzheimer disease (AD) is the most common type of dementia, which is still a problem that everyone must deal with. In a continuous effort to find effective treatments, the new candidates for AD therapy have the capacity to scavenge excessive levels of free radicals and inhibit acetylcholinesterase (AChE). Objectives: This study focuses on synthesizing and biologically evaluating novel hybrid compounds (1-3) as acetylcholine esterase inhibitors. Methods: The benzimidazole has been added and then coupled with coumaric acid, cinnamic acid, and lipoic acid as conjugates, which are expected to have dual action as acetylcholinesterase inhibitors and antioxidants. The synthesis of benzimidazole derivatives (1-3) was accomplished and then characterized using 1H-NMR and elemental analysis. Additionally, their characteristics were assessed in vitro against the AChE enzyme. Results: The new compounds produced a potent inhibitory activity that may serve as a lead molecule for the synthesis of novel anti-AD molecules. Compound-1 has an inhibition percentage that is close to that of the authorized medication galantamine (95.386%), whereas compound-3 has the lowest inhibition percentage (88.647%). Conclusions: A very good yield was achieved during the synthesis of the benzimidazole derivatives (1-3) from the starting material. They can serve as potential candidates for acetylcholine esterase inhibitors.","PeriodicalId":105471,"journal":{"name":"Al-Rafidain Journal of Medical Sciences ( ISSN 2789-3219 )","volume":"42 6","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, Characterization and Preliminary Evaluation of New 1H-benzo[d]imidazole-1yl-derivatives as Acetylcholine Esterase Inhibitors\",\"authors\":\"Shuhad Yaseen, S. Z. Abdul-Majeed, Sarah Ashour Hamood\",\"doi\":\"10.54133/ajms.v7i1.794\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Background: Alzheimer disease (AD) is the most common type of dementia, which is still a problem that everyone must deal with. In a continuous effort to find effective treatments, the new candidates for AD therapy have the capacity to scavenge excessive levels of free radicals and inhibit acetylcholinesterase (AChE). Objectives: This study focuses on synthesizing and biologically evaluating novel hybrid compounds (1-3) as acetylcholine esterase inhibitors. Methods: The benzimidazole has been added and then coupled with coumaric acid, cinnamic acid, and lipoic acid as conjugates, which are expected to have dual action as acetylcholinesterase inhibitors and antioxidants. The synthesis of benzimidazole derivatives (1-3) was accomplished and then characterized using 1H-NMR and elemental analysis. Additionally, their characteristics were assessed in vitro against the AChE enzyme. Results: The new compounds produced a potent inhibitory activity that may serve as a lead molecule for the synthesis of novel anti-AD molecules. Compound-1 has an inhibition percentage that is close to that of the authorized medication galantamine (95.386%), whereas compound-3 has the lowest inhibition percentage (88.647%). Conclusions: A very good yield was achieved during the synthesis of the benzimidazole derivatives (1-3) from the starting material. They can serve as potential candidates for acetylcholine esterase inhibitors.\",\"PeriodicalId\":105471,\"journal\":{\"name\":\"Al-Rafidain Journal of Medical Sciences ( ISSN 2789-3219 )\",\"volume\":\"42 6\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-07-09\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Al-Rafidain Journal of Medical Sciences ( ISSN 2789-3219 )\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.54133/ajms.v7i1.794\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Al-Rafidain Journal of Medical Sciences ( ISSN 2789-3219 )","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.54133/ajms.v7i1.794","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

背景:阿尔茨海默病(AD)是最常见的痴呆症类型,至今仍是每个人必须面对的问题。在不断寻找有效治疗方法的过程中,治疗阿尔茨海默病的新候选药物具有清除过量自由基和抑制乙酰胆碱酯酶(AChE)的能力。研究目的本研究的重点是合成新型混合化合物(1-3)作为乙酰胆碱酯酶抑制剂,并对其进行生物学评估。方法:苯并咪唑添加后与香豆酸、肉桂酸和硫辛酸偶联成共轭物,有望作为乙酰胆碱酯酶抑制剂和抗氧化剂发挥双重作用。我们合成了苯并咪唑衍生物(1-3),并利用 1H-NMR 和元素分析对其进行了表征。此外,还针对 AChE 酶对它们的特性进行了体外评估。结果:新化合物具有很强的抑制活性,可作为合成新型抗 AChE 分子的先导分子。化合物-1的抑制率接近于授权药物加兰他敏(95.386%),而化合物-3的抑制率最低(88.647%)。结论从起始原料合成苯并咪唑衍生物(1-3)的收率非常高。它们可以作为乙酰胆碱酯酶抑制剂的潜在候选化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, Synthesis, Characterization and Preliminary Evaluation of New 1H-benzo[d]imidazole-1yl-derivatives as Acetylcholine Esterase Inhibitors
Background: Alzheimer disease (AD) is the most common type of dementia, which is still a problem that everyone must deal with. In a continuous effort to find effective treatments, the new candidates for AD therapy have the capacity to scavenge excessive levels of free radicals and inhibit acetylcholinesterase (AChE). Objectives: This study focuses on synthesizing and biologically evaluating novel hybrid compounds (1-3) as acetylcholine esterase inhibitors. Methods: The benzimidazole has been added and then coupled with coumaric acid, cinnamic acid, and lipoic acid as conjugates, which are expected to have dual action as acetylcholinesterase inhibitors and antioxidants. The synthesis of benzimidazole derivatives (1-3) was accomplished and then characterized using 1H-NMR and elemental analysis. Additionally, their characteristics were assessed in vitro against the AChE enzyme. Results: The new compounds produced a potent inhibitory activity that may serve as a lead molecule for the synthesis of novel anti-AD molecules. Compound-1 has an inhibition percentage that is close to that of the authorized medication galantamine (95.386%), whereas compound-3 has the lowest inhibition percentage (88.647%). Conclusions: A very good yield was achieved during the synthesis of the benzimidazole derivatives (1-3) from the starting material. They can serve as potential candidates for acetylcholine esterase inhibitors.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信