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

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2024-05-15 DOI:10.1080/10286020.2024.2346636

引用次数: 0

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 6j (29.73 μg/ml) and 7a (38.15 μg/ml) displayed excellent inhibitory activity against the spore of Fusarium solani. The inhibitory activity of compound 7d (10.53 μg/ml) against the spore of Alternaria solani was more than 42-fold that of vanillin. Compound 7a (37.54 μg/ml) showed better antifungal activity against the spore of B. cinerea than positive controls. The cytotoxicity assay confirmed that compounds 6k, 7a, and 7d showed good selectivity and less toxicity to normal mammalian cells.

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开发天然香水作为潜在的杀真菌剂候选物：含有 1,3,4-oxadiazole/1,3-thiazolidin-4-one 片段的香兰素类似物的构建和生物学评价。

研究人员制备了两个系列的香兰素衍生物，分别含有 1,3,4-恶二唑和 1,3-噻唑啉-4-酮支架，并对其抗真菌活性进行了评估。结果表明，化合物 6j（29.73 μg/ml）和 7a（38.15 μg/ml）对禾谷镰刀菌孢子具有很好的抑制活性。化合物 7d（10.53 μg/ml）对茄属真菌孢子的抑制活性是香兰素的 42 倍以上。化合物 7a（37.54 μg/ml）对 B. cinerea 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 6k、7a 和 7d 具有良好的选择性，对正常哺乳动物细胞的毒性较小。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Asian Natural Products Research 医学-药学

CiteScore

3.20

自引率

5.90%

发文量

审稿时长

2.3 months

期刊介绍： The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures. All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.