The active splicing strategy has witnessed improvement in bioactivity and antifungal spectra in pesticide discovery. Herein, a series of simple-structured molecules (-) containing chloro-substituted benzyl esters were designed using the above strategy. The structure-activity relationship (SAR) analysis demonstrated that the fatty acid fragment-structured esters were more effective than those containing an aromatic acid moiety or naphthenic acid part. Compounds and , which featured a thiazole-4-acid moiety and trifluoromethyl aliphatic acid part, respectively, exhibited excellent curative activity (89.4%, 100 mg/L ) and fungicidal activity (EC = 0.708 mg/L, ) against . Determination of antifungal spectra and analysis of scanning electron microscopy (SEM), membrane permeability, cell peroxidation, ergosterol content, oxalic acid pathways, and enzymatic assays were performed separately here. Compound is cost effective due to its simple structure and shows promise as a disease control candidate. In addition, might act on a novel target through a new pathway that disrupts the cell membrane integrity by inducing cell peroxidation.
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http://dx.doi.org/10.1021/acs.jafc.4c01033 | DOI Listing |
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