Qiang Fei, Yanbi Luo, Haijiang Chen, Wenneng Wu, Su Xu
{"title":"阿魏酸酰胺衍生物的设计、合成、抗真菌和抗菌评价。","authors":"Qiang Fei, Yanbi Luo, Haijiang Chen, Wenneng Wu, Su Xu","doi":"10.1007/s11030-024-11076-4","DOIUrl":null,"url":null,"abstract":"<p><p>Natural compounds' derivatives as lead structures could effectively solve plant disease problems. In this article, amide compounds and amide ester compounds were synthetized through ferulic acid as the parent nucleus structure, and their biological activities in vitro and in vivo were evaluated. Compound 1q was screened out as the one with the best activity performance toward Xanthomonas axonopodis pv. citri (Xac), which displayed the inhibition rate of 100% and the EC<sub>50</sub> as low as 4.56 μg/mL. The results of in vivo experiments on citrus leaves infected with Xac showed that compound 1q had a protective efficacy of 60.98% and a curative efficacy of 26.56%. The mechanism of action as well as molecular docking was previously studied using extracellular polysaccharide (EPS) content, bacterial membrane permeability, and scanning electron microscopy (SEM) observations. Experimental results show that compound 1q can become an antibacterial agent for preventing and managing plant diseases.</p>","PeriodicalId":708,"journal":{"name":"Molecular Diversity","volume":" ","pages":""},"PeriodicalIF":3.9000,"publicationDate":"2024-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, synthesis, antifungal, and antibacterial evaluation of ferulic acid derivatives bearing amide moiety.\",\"authors\":\"Qiang Fei, Yanbi Luo, Haijiang Chen, Wenneng Wu, Su Xu\",\"doi\":\"10.1007/s11030-024-11076-4\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Natural compounds' derivatives as lead structures could effectively solve plant disease problems. In this article, amide compounds and amide ester compounds were synthetized through ferulic acid as the parent nucleus structure, and their biological activities in vitro and in vivo were evaluated. Compound 1q was screened out as the one with the best activity performance toward Xanthomonas axonopodis pv. citri (Xac), which displayed the inhibition rate of 100% and the EC<sub>50</sub> as low as 4.56 μg/mL. The results of in vivo experiments on citrus leaves infected with Xac showed that compound 1q had a protective efficacy of 60.98% and a curative efficacy of 26.56%. The mechanism of action as well as molecular docking was previously studied using extracellular polysaccharide (EPS) content, bacterial membrane permeability, and scanning electron microscopy (SEM) observations. Experimental results show that compound 1q can become an antibacterial agent for preventing and managing plant diseases.</p>\",\"PeriodicalId\":708,\"journal\":{\"name\":\"Molecular Diversity\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2024-12-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecular Diversity\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1007/s11030-024-11076-4\",\"RegionNum\":2,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, APPLIED\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Diversity","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1007/s11030-024-11076-4","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
Design, synthesis, antifungal, and antibacterial evaluation of ferulic acid derivatives bearing amide moiety.
Natural compounds' derivatives as lead structures could effectively solve plant disease problems. In this article, amide compounds and amide ester compounds were synthetized through ferulic acid as the parent nucleus structure, and their biological activities in vitro and in vivo were evaluated. Compound 1q was screened out as the one with the best activity performance toward Xanthomonas axonopodis pv. citri (Xac), which displayed the inhibition rate of 100% and the EC50 as low as 4.56 μg/mL. The results of in vivo experiments on citrus leaves infected with Xac showed that compound 1q had a protective efficacy of 60.98% and a curative efficacy of 26.56%. The mechanism of action as well as molecular docking was previously studied using extracellular polysaccharide (EPS) content, bacterial membrane permeability, and scanning electron microscopy (SEM) observations. Experimental results show that compound 1q can become an antibacterial agent for preventing and managing plant diseases.
期刊介绍:
Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including:
combinatorial chemistry and parallel synthesis;
small molecule libraries;
microwave synthesis;
flow synthesis;
fluorous synthesis;
diversity oriented synthesis (DOS);
nanoreactors;
click chemistry;
multiplex technologies;
fragment- and ligand-based design;
structure/function/SAR;
computational chemistry and molecular design;
chemoinformatics;
screening techniques and screening interfaces;
analytical and purification methods;
robotics, automation and miniaturization;
targeted libraries;
display libraries;
peptides and peptoids;
proteins;
oligonucleotides;
carbohydrates;
natural diversity;
new methods of library formulation and deconvolution;
directed evolution, origin of life and recombination;
search techniques, landscapes, random chemistry and more;