AI Article Synopsis

  • - The study improves pesticide discovery by using an active splicing strategy that enhances bioactivity and antifungal effectiveness, focusing on simple molecules with chloro-substituted benzyl esters.
  • - An analysis of the structure-activity relationship revealed that fatty acid fragment esters are more potent than those with aromatic or naphthenic acids, with certain compounds showing high curative and fungicidal activities.
  • - One compound stands out as cost-effective and exhibits potential for disease control by targeting cell membrane integrity, potentially through a novel mechanism that leads to cell damage.

Article Abstract

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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Source
http://dx.doi.org/10.1021/acs.jafc.4c01033DOI Listing

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