Design, Synthesis and Antifungal Activity of Azole-Modified Sclerotiorin Derivatives

doi:10.6023/cjoc202605013

Chinese Journal of Organic Chemistry

ARTICLE

唑类修饰核丛青霉素衍生物的合成及其抗菌活性研究

李佚琳^†, 刘铃铃^†, 贾豪, 黎嘉琳, 龙玉华^*

华南师范大学化学学院广州 510006

收稿日期:2026-05-14 修回日期:2026-08-03
作者简介:^†共同第一作者
基金资助:
广东省自然科学基金(No. 2025A1515012235)资助项目.

Design, Synthesis and Antifungal Activity of Azole-Modified Sclerotiorin Derivatives

Yilin Li^†, Linlin Liu^†, Hao Jia, Jialin Li, Yuhua Long^*

School of Chemistry, South China Normal University, Guangzhou, 510006

Received:2026-05-14 Revised:2026-08-03
Contact: ^*E-mail: longyh@scnu.edu.cn
About author:^†These authors contributed equally to this work
Supported by:
Natural Science Foundation of Guangdong Province (No. 2025A1515012235).

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Abstract

Azaphilone derivatives have a wide range of pharmacological activities. Inspired by the application of various derivatives of natural products with broad-spectrum antiphytopathogenic activity, 17 novel Azole-Modified sclerotiorin derivatives with nitrogen-containing heterocyclic substitutions were designed and synthesized, and their antifungal activities against five plant pathogenic fungi were evaluated.The results of the in vitro antifungal test showed that compound Sc-17 exhibited the highest inhibitory activity against Botrytis cinerea, with its minimum inhibitory concentration (MIC) being 25 μg/mL.Furthermore, compounds Sc-2, Sc-9 and Sc-10 exhibited stronger inhibitory activity against the Colletotrichum litchi Trag than the parent compound sclerotiorin. The minimum inhibitory concentration (MIC) of all three compounds was 25 μg/mL. The in vivo test results indicated that compound Sc-17 shows significant post-harvest protection and treatment effects on the three types of fruits.Further studies on the initial mechanism of compound Sc-17's effect on Botrytis cinerea revealed that compound Sc-17 can exhibit concentration-dependent inhibition of the activity of Botrytis cinerea.SEM and TEM observations revealed that the compound Sc-17 could achieve antifungal effects by damaging the cell membrane and cell wall, causing the leakage of intracellular substances and the dissolution of organelles.

Key words: Sclerotiorin, Botrytis cinerea, Colletotrichum litchi Trag, antifungal activity

Cite this article

Yilin Li, Linlin Liu, Hao Jia, Jialin Li, Yuhua Long. Design, Synthesis and Antifungal Activity of Azole-Modified Sclerotiorin Derivatives[J]. Chinese Journal of Organic Chemistry, doi: 10.6023/cjoc202605013.

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唑类修饰核丛青霉素衍生物的合成及其抗菌活性研究

Design, Synthesis and Antifungal Activity of Azole-Modified Sclerotiorin Derivatives

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