Della G T Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa E Mathew, Sanal Dev, Balasubramanain Lakshminarayanan, Omnia M Hendawy, Bijo Mathew
{"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":"<p><strong>Background: </strong>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).</p><p><strong>Methods: </strong>The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.</p>","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}
引用次数: 3
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.
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.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
