{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Wu J"],"funding":["Shanghai Sailing Program"],"pagination":["1337"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC10974209"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["29(6)"],"pubmed_abstract":["The meta-diamide (<i>m</i>-diamide) insecticide, Broflanilide, was characterized by its high efficiency, low toxicity and lack of cross-resistance with traditional GABA receptors. In accordance with the principles of drug molecular design, easily derivable sulfur with diverse bioactivities was introduced while leading with the parent Broflanilide. Twelve novel <i>m</i>-diamide target compounds containing sulfide derivatives were synthesized through exploration guided by the literature. Their structures were confirmed by melting points, <sup>1</sup>H NMR, <sup>13</sup>C NMR and HRMS. Insecticidal activity assessments revealed that most target compounds <b>A</b>-<b>D</b> exhibited 100% lethality against <i>Plutella xylostella</i> (<i>P. xylostella</i>) and <i>Aphis craccivora Koch</i> (<i>A. craccivora</i>) at 500 mg·L<sup>-1</sup>. Notably, for <i>P. xylostella</i>, compounds <b>C-2</b>, <b>C-3</b>, <b>C-4</b> and <b>D-2</b> demonstrated 60.00-100.00% insecticidal activity even at a concentration as low as 0.625 mg·L<sup>-1</sup>. As determined by structure-activity relationship (SAR) analysis, compounds with R<sub>1</sub> = CH<sub>3</sub> and R<sub>2</sub> = Br (<b>B-1</b>, <b>C-2</b> and <b>D-2</b>) and sulfoxide compound <b>C-3</b> contained 100.00% lethality against <i>A. craccivora</i> at 500 mg·L<sup>-1</sup>, surpassing the lethality when leading with the parent Broflanilide in terms of efficacy. Consequently, it can be inferred that the sulfoxide compound (<b>C-3</b>) requires further investigation as a potential active molecule for new insecticides. These explorations provide valuable references for future research on the synthesis and insecticidal activities of sulfide-containing <i>m</i>-diamide compounds."],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["Novel Meta-Diamide Compounds Containing Sulfide Derivatives Were Designed and Synthesized as Potential Pesticides."],"pmcid":["PMC10974209"],"funding_grant_id":["21YF1414400"],"pubmed_authors":["Wu J","Zhang Y","Zhou S","Dang S"],"additional_accession":[]},"is_claimable":false,"name":"Novel Meta-Diamide Compounds Containing Sulfide Derivatives Were Designed and Synthesized as Potential Pesticides.","description":"The meta-diamide (<i>m</i>-diamide) insecticide, Broflanilide, was characterized by its high efficiency, low toxicity and lack of cross-resistance with traditional GABA receptors. In accordance with the principles of drug molecular design, easily derivable sulfur with diverse bioactivities was introduced while leading with the parent Broflanilide. Twelve novel <i>m</i>-diamide target compounds containing sulfide derivatives were synthesized through exploration guided by the literature. Their structures were confirmed by melting points, <sup>1</sup>H NMR, <sup>13</sup>C NMR and HRMS. Insecticidal activity assessments revealed that most target compounds <b>A</b>-<b>D</b> exhibited 100% lethality against <i>Plutella xylostella</i> (<i>P. xylostella</i>) and <i>Aphis craccivora Koch</i> (<i>A. craccivora</i>) at 500 mg·L<sup>-1</sup>. Notably, for <i>P. xylostella</i>, compounds <b>C-2</b>, <b>C-3</b>, <b>C-4</b> and <b>D-2</b> demonstrated 60.00-100.00% insecticidal activity even at a concentration as low as 0.625 mg·L<sup>-1</sup>. As determined by structure-activity relationship (SAR) analysis, compounds with R<sub>1</sub> = CH<sub>3</sub> and R<sub>2</sub> = Br (<b>B-1</b>, <b>C-2</b> and <b>D-2</b>) and sulfoxide compound <b>C-3</b> contained 100.00% lethality against <i>A. craccivora</i> at 500 mg·L<sup>-1</sup>, surpassing the lethality when leading with the parent Broflanilide in terms of efficacy. Consequently, it can be inferred that the sulfoxide compound (<b>C-3</b>) requires further investigation as a potential active molecule for new insecticides. These explorations provide valuable references for future research on the synthesis and insecticidal activities of sulfide-containing <i>m</i>-diamide compounds.","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Mar","modification":"2025-04-22T21:29:42.78Z","creation":"2025-04-22T21:29:42.78Z"},"accession":"S-EPMC10974209","cross_references":{"pubmed":["38542973"],"doi":["10.3390/molecules29061337"]}}