Jian-Song An , Shu-Hui Hu , Hai-Jiang Chen , Qiang Fei , Wen-Neng Wu
{"title":"含1,3,4-噻二唑和1,2,4-三唑硫醚的三氟甲基嘧啶衍生物的合成、抑菌和抗菌评价","authors":"Jian-Song An , Shu-Hui Hu , Hai-Jiang Chen , Qiang Fei , Wen-Neng Wu","doi":"10.1080/10426507.2025.2481121","DOIUrl":null,"url":null,"abstract":"<div><div>In this study, twentythree trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties were designed and synthesized. These compounds were confirmed structurally through IR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, and HRMS analyses. Bioassay results revealed that some of the synthesized compounds exhibited higher antifungal activity compared to commercial drug. Particularly, compounds <strong>7s</strong> and <strong>7t</strong> demonstrated antifungal rates of 80.13% and 81.70% against <em>Sclerotinia sclerotiorum</em> at 50 <em>μ</em>g/mL, outperforming the control agent Pyrimethanil (68.39%). Furthermore, their EC<sub>50</sub> values of 14.68 and 13.06 <em>μ</em>g/mL, respectively, were better than that of Pyrimethanil (46.94 <em>μ</em>g/mL). These findings suggest that compounds <strong>7s</strong> and <strong>7t</strong> hold promise for future drug development due to their efficient synthesis and notable biological activities.</div></div>","PeriodicalId":20056,"journal":{"name":"Phosphorus, Sulfur, and Silicon and the Related Elements","volume":"200 4","pages":"Pages 372-382"},"PeriodicalIF":1.4000,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties\",\"authors\":\"Jian-Song An , Shu-Hui Hu , Hai-Jiang Chen , Qiang Fei , Wen-Neng Wu\",\"doi\":\"10.1080/10426507.2025.2481121\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>In this study, twentythree trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties were designed and synthesized. These compounds were confirmed structurally through IR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, and HRMS analyses. Bioassay results revealed that some of the synthesized compounds exhibited higher antifungal activity compared to commercial drug. Particularly, compounds <strong>7s</strong> and <strong>7t</strong> demonstrated antifungal rates of 80.13% and 81.70% against <em>Sclerotinia sclerotiorum</em> at 50 <em>μ</em>g/mL, outperforming the control agent Pyrimethanil (68.39%). Furthermore, their EC<sub>50</sub> values of 14.68 and 13.06 <em>μ</em>g/mL, respectively, were better than that of Pyrimethanil (46.94 <em>μ</em>g/mL). These findings suggest that compounds <strong>7s</strong> and <strong>7t</strong> hold promise for future drug development due to their efficient synthesis and notable biological activities.</div></div>\",\"PeriodicalId\":20056,\"journal\":{\"name\":\"Phosphorus, Sulfur, and Silicon and the Related Elements\",\"volume\":\"200 4\",\"pages\":\"Pages 372-382\"},\"PeriodicalIF\":1.4000,\"publicationDate\":\"2025-04-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Phosphorus, Sulfur, and Silicon and the Related Elements\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/org/science/article/pii/S1042650725000255\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Phosphorus, Sulfur, and Silicon and the Related Elements","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S1042650725000255","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties
In this study, twentythree trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties were designed and synthesized. These compounds were confirmed structurally through IR,1H NMR,13C NMR, and HRMS analyses. Bioassay results revealed that some of the synthesized compounds exhibited higher antifungal activity compared to commercial drug. Particularly, compounds 7s and 7t demonstrated antifungal rates of 80.13% and 81.70% against Sclerotinia sclerotiorum at 50 μg/mL, outperforming the control agent Pyrimethanil (68.39%). Furthermore, their EC50 values of 14.68 and 13.06 μg/mL, respectively, were better than that of Pyrimethanil (46.94 μg/mL). These findings suggest that compounds 7s and 7t hold promise for future drug development due to their efficient synthesis and notable biological activities.
期刊介绍:
Phosphorus, Sulfur, and Silicon and the Related Elements is a monthly publication intended to disseminate current trends and novel methods to those working in the broad and interdisciplinary field of heteroatom chemistry.