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The synthesis of coumarin thiazoles containing a trifluoromethyl group and their antifungal activities
Arabian Journal of Chemistry ( IF 5.3 ) Pub Date : 2021-01-01 , DOI: 10.1016/j.arabjc.2020.10.027
Guoyu Yang , Lijun Shi , Zhenliang Pan , Lulu Wu , Liangxin Fan , Caixia Wang , Cuilian Xu , Jun Liang

Abstract A series of novel coumarin thiazoles containing trifluoromethyl group 3a-3l were prepared through a one-pot reaction and 3-(trifluoroacetyl)coumarin as a starting material in solvent-free conditions. Their structures were confirmed using IR, 1H NMR, 13C NMR, HRMS and X-ray single crystal diffraction, and their antifungal activity against Fusarium. moniliforme(F. moniliforme), Fusarium. graminearum(F. graminearum), and Curvularia. lunata(C. lunata) was evaluated. Among the synthesized compounds, compound 3f showed the highest inhibitor rate of 74% at 0.5 mg/mL against F. moniliforme, and compound 3g exhibited the highest inhibitor rates of 89% and 93.4% at 0.5 mg/mL against F. graminearum and C. lunata, respectively. The introduction of trifluoromethyl group greatly improved the antifungal activity of counterpart 3g compared to the compound 4.

中文翻译:

含三氟甲基的香豆素噻唑类化合物的合成及其抗真菌活性

摘要 以3-(三氟乙酰基)香豆素为原料,在无溶剂条件下,通过一锅法反应制备了一系列含三氟甲基的新型香豆素噻唑类化合物3a-3l。使用 IR、1H NMR、13C NMR、HRMS 和 X 射线单晶衍射证实了它们的结构,以及它们对镰刀菌的抗真菌活性。念珠菌(F. moniliforme),镰刀菌。禾本科(F. graminearum)和弯孢属。lunata(C. lunata) 进行了评价。在合成的化合物中,化合物 3f 在 0.5 mg/mL 时对念珠菌的抑制率最高,为 74%,化合物 3g 在 0.5 mg/mL 时对禾谷镰刀菌和念珠菌的抑制率最高,分别为 89% 和 93.4% . lunata,分别。
更新日期:2021-01-01
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