{"title":"合成、抗氧化活性","authors":"a","doi":"10.3987/com-23-14915","DOIUrl":null,"url":null,"abstract":"<span>3-[2-(5-Aryl-3-phenyl-4,5-dihydro-1</span><span>H</span><span>-pyrazol-1-yl)thiazol-4-yl]-4- hydroxy-6-methyl-2</span><span>H</span><span>-pyran-2-ones </span><span>6a-h</span><span> were synthesized </span><span>via</span><span> the ring closure reactions of 3-phenyl-5-aryl-4,5-dihydropyrazole-1-carbothioamides </span><span>3a-h</span><span> with 3-(bromoacetyl)-4-hydroxy-6-methyl-2</span><span>H</span><span>-pyran-2-one </span><span>5</span><span>. The new synthesized thiazolyl-pyrazolinyl-pyran-2-one compounds were evaluated for their potential antioxidant activity by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical method. The molecular docking of the synthesized compounds on DPPH oxidase protein showed a high binding affinity, confirming the experimental results recorded. The synthesized compounds deserve a consideration for further analyses regarding the control of oxidative stress and their use as possible antioxidant agents in the pharmaceutical industry.<br/></span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.8000,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, Antioxidant Activity\",\"authors\":\"a\",\"doi\":\"10.3987/com-23-14915\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<span>3-[2-(5-Aryl-3-phenyl-4,5-dihydro-1</span><span>H</span><span>-pyrazol-1-yl)thiazol-4-yl]-4- hydroxy-6-methyl-2</span><span>H</span><span>-pyran-2-ones </span><span>6a-h</span><span> were synthesized </span><span>via</span><span> the ring closure reactions of 3-phenyl-5-aryl-4,5-dihydropyrazole-1-carbothioamides </span><span>3a-h</span><span> with 3-(bromoacetyl)-4-hydroxy-6-methyl-2</span><span>H</span><span>-pyran-2-one </span><span>5</span><span>. The new synthesized thiazolyl-pyrazolinyl-pyran-2-one compounds were evaluated for their potential antioxidant activity by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical method. The molecular docking of the synthesized compounds on DPPH oxidase protein showed a high binding affinity, confirming the experimental results recorded. The synthesized compounds deserve a consideration for further analyses regarding the control of oxidative stress and their use as possible antioxidant agents in the pharmaceutical industry.<br/></span>\",\"PeriodicalId\":13166,\"journal\":{\"name\":\"Heterocycles\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.8000,\"publicationDate\":\"2023-11-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Heterocycles\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.3987/com-23-14915\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Heterocycles","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.3987/com-23-14915","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
3-[2-(5-Aryl-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4-yl]-4- hydroxy-6-methyl-2H-pyran-2-ones 6a-h were synthesized via the ring closure reactions of 3-phenyl-5-aryl-4,5-dihydropyrazole-1-carbothioamides 3a-h with 3-(bromoacetyl)-4-hydroxy-6-methyl-2H-pyran-2-one 5. The new synthesized thiazolyl-pyrazolinyl-pyran-2-one compounds were evaluated for their potential antioxidant activity by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical method. The molecular docking of the synthesized compounds on DPPH oxidase protein showed a high binding affinity, confirming the experimental results recorded. The synthesized compounds deserve a consideration for further analyses regarding the control of oxidative stress and their use as possible antioxidant agents in the pharmaceutical industry.
期刊介绍：
Since its inception in 1973 HETEROCYCLES has provided a platform for the rapid exchange of research in the areas of organic, pharmaceutical, analytical, and medicinal chemistry of heterocyclic compounds in addition to communications, papers, reviews, a special section of the journal presents newly-discovered natural products whose structure has recently been established.
Another section is devoted to the total synthesis of previously documented natural products with heterocyclic ring systems.
Due to the fact that the journal is able to publish articles within two months of receipt of the manuscripts, researchers in this field can obtain up-to-date information on heterocyclic research by reading Heterocycles regularly.
Audience: Organic and Physical Organic Chemists, Biochemists, Pharmacologists and Scientists studying heterocyclic compounds
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