Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties

IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Phosphorus, Sulfur, and Silicon and the Related Elements Pub Date : 2025-04-03 Epub Date: 2025-03-15 DOI:10.1080/10426507.2025.2481121
Jian-Song An , Shu-Hui Hu , Hai-Jiang Chen , Qiang Fei , Wen-Neng Wu
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Abstract

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.
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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
本研究设计合成了23个含有1,3,4-噻二唑和1,2,4-三唑硫醚基团的三氟甲基嘧啶衍生物。这些化合物通过IR、1H NMR、13C NMR和HRMS进行了结构鉴定。生物测定结果表明,与市售药物相比,合成的一些化合物具有更高的抗真菌活性。其中,化合物7s和7t在50 μg/mL浓度下对菌核菌的抑菌率分别为80.13%和81.70%,优于吡虫胺(68.39%)。其EC50值分别为14.68和13.06 μg/mL,优于嘧虫胺(46.94 μg/mL)。这些发现表明,化合物7s和7t由于其高效的合成和显著的生物活性,在未来的药物开发中具有广阔的前景。
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来源期刊
CiteScore
2.60
自引率
7.70%
发文量
103
审稿时长
2.1 months
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.
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