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天然香料作为潜在杀菌剂候选物的开发:含 1,3,4-噁二唑/1,3-噻唑烷-4-酮片段的香草醛类似物的构建与生物评价。

Development of natural perfume as potential fungicide candidates: construction and biological evaluation of vanillin analogs bearing the 1,3,4-oxadiazole/1,3-thiazolidin-4-one fragments.

机构信息

Shanxi Key Laboratory of Integrated Pest Management in Agriculture, College of Plant Protection, Shanxi Agricultural University, Taigu 030801, China.

出版信息

J Asian Nat Prod Res. 2024 Sep;26(9):1094-1105. doi: 10.1080/10286020.2024.2346636. Epub 2024 May 16.

Abstract

Two series of vanillin derivatives containing 1,3,4-oxadiazole and 1,3-thiazolidin-4-one scaffolds were prepared and evaluated for their antifungal activity. The results revealed that compounds (29.73 μg/ml) and (38.15 μg/ml) displayed excellent inhibitory activity against the spore of . The inhibitory activity of compound (10.53 μg/ml) against the spore of was more than 42-fold that of vanillin. Compound (37.54 μg/ml) showed better antifungal activity against the spore of than positive controls. The cytotoxicity assay confirmed that compounds , , and showed good selectivity and less toxicity to normal mammalian cells.

摘要

两个含有 1,3,4-噁二唑和 1,3-噻唑烷-4-酮骨架的香草醛衍生物系列被制备并评估了它们的抗真菌活性。结果表明,化合物 (29.73μg/ml) 和 (38.15μg/ml) 对 的孢子显示出极好的抑制活性。化合物 (10.53μg/ml) 对 的孢子的抑制活性比香草醛高出 42 倍以上。化合物 (37.54μg/ml) 对 的孢子的抗真菌活性优于阳性对照。细胞毒性试验证实,化合物 、 和 对正常哺乳动物细胞具有良好的选择性和较低的毒性。

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