Peptidomimetics based on natural cinnamic acid scaffold: Synthesis, bio-evaluation and structure-activity relationships

文献类型： 外文期刊

第一作者： Guo, Lirong

作者： Guo, Lirong;Wang, Hexiang;Liu, Fang;Bao, Longzhu;Wu, Zhaoyuan;Ye, Ting;Zhang, Yani;Wang, Yueying;Fang, Wei;Ke, Shaoyong;Guo, Lirong;Wang, Hexiang;Cao, Xiufang;Duan, Liping;Duan, Liping;Duan, Liping;Duan, Liping

作者机构：

关键词： Natural product; Peptidomimetics; Cinnamic acid; Conjugates; Biological activity; SARs

期刊名称：PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY （ 影响因子：4.0； 五年影响因子：4.5 ）

ISSN： 0048-3575

年卷期： 2025 年 213 卷

页码：

收录情况： SCI

摘要： A total of twenty-one peptidomimetics based on cinnamic acid scaffold were synthesized through structureactivity relationship driven (SAR-driven) optimization of natural molecule (CSDK450160). Systematic bioevaluation against twelve phytopathogenic fungi for these compounds revealed structure-dependent antifungal specificity, with cinnamic acid-peptide conjugates demonstrating pronounced inhibitory efficacy against Botrytis cinerea and Sclerotinia sclerotiorum. In planta antifungal assays showed that compound I-1 exhibited superior inhibitory potency against S. sclerotiorum. Scanning electron microscopy (SEM) analysis confirmed significant morphological disruption of S. sclerotiorum hyphae by I-1, including mycelial collapse and septation defects, effectively arresting mycelial proliferation. The mechanism of interaction between compound I-1 and potential target protein was described by integrating molecular docking technology and quantum chemistry theory. The theoretical results show that compound I-1 exhibits unique spatial structure specificity and achieves accurate recognition and highly selective binding with target proteins through it-it stacking.

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