Momin Khan, Munir Ur Rehman, Aftab Alam, Muhammad Ashraf, Uzma Salar, Khalid Mohammed Khan, Abdullah F. AlAsmari, Fawaz Alasmari
{"title":"探索 5-亚芳基-N,N-二乙基硫代巴比妥酸盐的 DPPH 自由基清除潜力","authors":"Momin Khan, Munir Ur Rehman, Aftab Alam, Muhammad Ashraf, Uzma Salar, Khalid Mohammed Khan, Abdullah F. AlAsmari, Fawaz Alasmari","doi":"10.1134/S1068162024050017","DOIUrl":null,"url":null,"abstract":"<p><b>Objective:</b> To screen the synthesized analogues for their <i>in vitro</i> DPPH free radical scavenging activity. Due to their high efficacy and inexpensiveness compared to natural antioxidants, synthetic antioxidants are frequently used. The current work is primarily concerned with investigating the free radical scavenging activity of derivatives of thiobarbituric acid, based on the findings of the literature review. <b>Methods:</b> A series of <i>N</i>,<i>N</i>-diethylthiobarbiturates (<b>I–XVII</b>) were synthesized, and screened for their DPPH radical scavenging activity. <b>Results and discussion:</b> Limited structure-activity relationship has been established on the basis of different substituents and their varying positions. These synthetic compounds showed varying degree of inhibition in the range of IC<sub>50</sub> values 20.28 ± 0.15 to 286.19 ± 0.16 μM. Limited structure-activity relationship was revealed that hydroxyl containing compounds (<b>V</b>) (IC<sub>50</sub> = 20.28 ± 0.15 μM), (<b>IV</b>) (IC<sub>50</sub> = 22.89 ± 0.19 μM), and (<b>I</b>) (IC<sub>50</sub> = 26.34 ± 0.03 μM) showed comparable free radical scavenging activities with standard quercetin (IC<sub>50</sub> = 16.96 ± 0.14 μM). <b>Conclusions:</b> The study indicates that <i>N</i>,<i>N</i>-diethylthiobarbiturate derivatives have the potential to be synthetic antioxidants since they have strong DPPH radical scavenging action. Additionally, molecules with hydroxyl substituting demonstrate efficacy that is comparable to that of the natural antioxidant quercetin.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 5","pages":"1928 - 1934"},"PeriodicalIF":1.1000,"publicationDate":"2024-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Exploring the DPPH Radical Scavenging Potential in 5-Arylidene-N,N-diethylthiobarbiturates\",\"authors\":\"Momin Khan, Munir Ur Rehman, Aftab Alam, Muhammad Ashraf, Uzma Salar, Khalid Mohammed Khan, Abdullah F. AlAsmari, Fawaz Alasmari\",\"doi\":\"10.1134/S1068162024050017\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><b>Objective:</b> To screen the synthesized analogues for their <i>in vitro</i> DPPH free radical scavenging activity. Due to their high efficacy and inexpensiveness compared to natural antioxidants, synthetic antioxidants are frequently used. The current work is primarily concerned with investigating the free radical scavenging activity of derivatives of thiobarbituric acid, based on the findings of the literature review. <b>Methods:</b> A series of <i>N</i>,<i>N</i>-diethylthiobarbiturates (<b>I–XVII</b>) were synthesized, and screened for their DPPH radical scavenging activity. <b>Results and discussion:</b> Limited structure-activity relationship has been established on the basis of different substituents and their varying positions. These synthetic compounds showed varying degree of inhibition in the range of IC<sub>50</sub> values 20.28 ± 0.15 to 286.19 ± 0.16 μM. Limited structure-activity relationship was revealed that hydroxyl containing compounds (<b>V</b>) (IC<sub>50</sub> = 20.28 ± 0.15 μM), (<b>IV</b>) (IC<sub>50</sub> = 22.89 ± 0.19 μM), and (<b>I</b>) (IC<sub>50</sub> = 26.34 ± 0.03 μM) showed comparable free radical scavenging activities with standard quercetin (IC<sub>50</sub> = 16.96 ± 0.14 μM). <b>Conclusions:</b> The study indicates that <i>N</i>,<i>N</i>-diethylthiobarbiturate derivatives have the potential to be synthetic antioxidants since they have strong DPPH radical scavenging action. Additionally, molecules with hydroxyl substituting demonstrate efficacy that is comparable to that of the natural antioxidant quercetin.</p>\",\"PeriodicalId\":758,\"journal\":{\"name\":\"Russian Journal of Bioorganic Chemistry\",\"volume\":\"50 5\",\"pages\":\"1928 - 1934\"},\"PeriodicalIF\":1.1000,\"publicationDate\":\"2024-10-09\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Russian Journal of Bioorganic Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1134/S1068162024050017\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of Bioorganic Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1068162024050017","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Exploring the DPPH Radical Scavenging Potential in 5-Arylidene-N,N-diethylthiobarbiturates
Objective: To screen the synthesized analogues for their in vitro DPPH free radical scavenging activity. Due to their high efficacy and inexpensiveness compared to natural antioxidants, synthetic antioxidants are frequently used. The current work is primarily concerned with investigating the free radical scavenging activity of derivatives of thiobarbituric acid, based on the findings of the literature review. Methods: A series of N,N-diethylthiobarbiturates (I–XVII) were synthesized, and screened for their DPPH radical scavenging activity. Results and discussion: Limited structure-activity relationship has been established on the basis of different substituents and their varying positions. These synthetic compounds showed varying degree of inhibition in the range of IC50 values 20.28 ± 0.15 to 286.19 ± 0.16 μM. Limited structure-activity relationship was revealed that hydroxyl containing compounds (V) (IC50 = 20.28 ± 0.15 μM), (IV) (IC50 = 22.89 ± 0.19 μM), and (I) (IC50 = 26.34 ± 0.03 μM) showed comparable free radical scavenging activities with standard quercetin (IC50 = 16.96 ± 0.14 μM). Conclusions: The study indicates that N,N-diethylthiobarbiturate derivatives have the potential to be synthetic antioxidants since they have strong DPPH radical scavenging action. Additionally, molecules with hydroxyl substituting demonstrate efficacy that is comparable to that of the natural antioxidant quercetin.
期刊介绍:
Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.