选定的卤代噻吩查尔酮胆碱酯酶抑制活性。

Q3 Psychology

Central nervous system agents in medicinal chemistry Pub Date : 2019-01-01 DOI:10.2174/1871524918666181119114016

Della G T Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa E Mathew, Sanal Dev, Balasubramanain Lakshminarayanan, Omnia M Hendawy, Bijo Mathew

{"title":"选定的卤代噻吩查尔酮胆碱酯酶抑制活性。","authors":"Della G T Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa E Mathew, Sanal Dev, Balasubramanain Lakshminarayanan, Omnia M Hendawy, Bijo Mathew","doi":"10.2174/1871524918666181119114016","DOIUrl":null,"url":null,"abstract":"Background: Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).Methods: The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.Results: Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.Conclusion: Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"3","resultStr":"{\"title\":\"Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.\",\"authors\":\"Della G T Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa E Mathew, Sanal Dev, Balasubramanain Lakshminarayanan, Omnia M Hendawy, Bijo Mathew\",\"doi\":\"10.2174/1871524918666181119114016\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Background: Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).Methods: The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.Results: Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.Conclusion: Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.\",\"PeriodicalId\":9799,\"journal\":{\"name\":\"Central nervous system agents in medicinal chemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2019-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Central nervous system agents in medicinal chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1871524918666181119114016\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Psychology\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Central nervous system agents in medicinal chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1871524918666181119114016","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Psychology","Score":null,"Total":0}

引用次数: 3

摘要

背景:双作用人单胺氧化酶B (hMAO-B)和胆碱酯酶(ChE)抑制剂治疗阿尔茨海默病(AD)比经典的单药单靶点治疗更有效。方法:对几种已知选择性hMAO-B抑制剂的卤代噻吩查尔酮类分子的ChE抑制能力进行了评价。结果:根据IC50值，所选化合物对ChE有中等抑制作用，IC50值在14 ~ 70µM范围内。合成的分子中，T8和T6分别对AChE和BChE表现出最强的抑制活性。结论:综上所述，T8可进一步优化以增强其AChE抑制活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文本刊更多论文

Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.

Background: Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).

Methods: The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.

Results: Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.

Conclusion: Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.

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

Central nervous system agents in medicinal chemistry Psychology-Neuropsychology and Physiological Psychology

CiteScore

2.10

自引率

0.00%

发文量

期刊介绍： Central Nervous System Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new central nervous system agents. Containing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Central Nervous System Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.