Antioxidant and cytotoxic activities of 2-oxo-1,2,3,4-tetrahydropyrimidines

IF 2.5 Q2 CHEMISTRY, MULTIDISCIPLINARY
Sarosh Iqbal , Shahida Perveen , M. Iqbal Choudhary , Musarrat Jabeen , Shumaila Kiran , Faiza Qayyum , Khalid Mohammed Khan
{"title":"Antioxidant and cytotoxic activities of 2-oxo-1,2,3,4-tetrahydropyrimidines","authors":"Sarosh Iqbal ,&nbsp;Shahida Perveen ,&nbsp;M. Iqbal Choudhary ,&nbsp;Musarrat Jabeen ,&nbsp;Shumaila Kiran ,&nbsp;Faiza Qayyum ,&nbsp;Khalid Mohammed Khan","doi":"10.1016/j.rechem.2024.101891","DOIUrl":null,"url":null,"abstract":"<div><div>Oxidative stress (OS) is an imbalance between ROS and antioxidants which is caused by increased synthesis and buildup of reactive oxygen species as well as a reduced ability to detoxify them. It contributes to the onset and progression of chronic inflammation, cancers, diabetes mellitus, atherosclerosis, Alzheimer’s disease, ocular disease, nephropathy, and premature aging. The molecules known as antioxidants contribute significantly to both the prevention and exaggeration of ailments. In the present study, heterocyclic ethyl esters of 2-oxo-1,2,3,4-tetrahydropyrimidines <strong>1</strong>–<strong>25</strong> were assessed for their antioxidant activity by employing two robust <em>in vitro</em> bioassays; superoxide anion, and DPPH radical scavenging assays. Cytotoxicity was also performed to evaluate the cytotoxicity on PC3 cells. Out of twenty-five, twenty-two compounds exhibited IC<sub>50</sub> values in the range of 3.32 ± 0.08 – 167 ± 0.7 µM in superoxide anion assay. Compound <strong>2</strong> (IC<sub>50</sub> = 3.32 ± 0.08 µM) remained the most potent as compared to quercetin dihydrate (IC<sub>50</sub> = 94.1 ± 1.1 µM). Whereas, compound <strong>10,</strong> possessing a catechol moiety was identified as an excellent dual radical scavenger. Hence, this study identified 2-oxo-1,2,3,4-tetrahydropyrimidines ethyl esters as non-cytotoxic, potent ROS scavengers that can be studied further to treat oxidative stress and related pathologies.</div></div>","PeriodicalId":420,"journal":{"name":"Results in Chemistry","volume":"13 ","pages":"Article 101891"},"PeriodicalIF":2.5000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Results in Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2211715624005873","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0

Abstract

Oxidative stress (OS) is an imbalance between ROS and antioxidants which is caused by increased synthesis and buildup of reactive oxygen species as well as a reduced ability to detoxify them. It contributes to the onset and progression of chronic inflammation, cancers, diabetes mellitus, atherosclerosis, Alzheimer’s disease, ocular disease, nephropathy, and premature aging. The molecules known as antioxidants contribute significantly to both the prevention and exaggeration of ailments. In the present study, heterocyclic ethyl esters of 2-oxo-1,2,3,4-tetrahydropyrimidines 125 were assessed for their antioxidant activity by employing two robust in vitro bioassays; superoxide anion, and DPPH radical scavenging assays. Cytotoxicity was also performed to evaluate the cytotoxicity on PC3 cells. Out of twenty-five, twenty-two compounds exhibited IC50 values in the range of 3.32 ± 0.08 – 167 ± 0.7 µM in superoxide anion assay. Compound 2 (IC50 = 3.32 ± 0.08 µM) remained the most potent as compared to quercetin dihydrate (IC50 = 94.1 ± 1.1 µM). Whereas, compound 10, possessing a catechol moiety was identified as an excellent dual radical scavenger. Hence, this study identified 2-oxo-1,2,3,4-tetrahydropyrimidines ethyl esters as non-cytotoxic, potent ROS scavengers that can be studied further to treat oxidative stress and related pathologies.

Abstract Image

求助全文
约1分钟内获得全文 求助全文
来源期刊
Results in Chemistry
Results in Chemistry Chemistry-Chemistry (all)
CiteScore
2.70
自引率
8.70%
发文量
380
审稿时长
56 days
×
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:481959085
Book学术官方微信