98%
921
2 minutes
20
Sulfonamide derivatives have been widely used for pesticide research in recent years. Herein, 1,3,4-oxadiazole sulfonamide derivatives containing a pyrazole structure were synthesized, and their structure-activity relationship was studied. Bioactivity tests showed the remarkable efficacy of most synthesized compounds. Especially for pv , A23 exhibited 100% inhibition at 100 mg/L, surpassing bismerthiazol (99.3%), and 90% inhibition at 50 mg/L, outperforming thiodiazole copper (84.5%), with an EC of 5.0 mg/L, markedly more active than bismerthiazol (23.9 mg/L) and thiodiazole copper (63.5 mg/L). Initial investigations into antimicrobial mechanisms involved a series of biochemical analyses, including bacterial growth rate analysis, scanning electron microscopy, bacterial biofilm formation experiments, and molecular docking analyses. Notably, A23 considerably inhibited the formation of biofilms, disrupting the integrity of bacterial cell membranes. Co-analysis of transcriptomics and proteomics revealed the capability of A23 to regulate pathways such as tryptophan metabolism and phenylpropanoid biosynthesis, enhancing the innate immunity of rice and activating its disease resistance. Thus, A23 emerges as a potential immunoinducible pesticide lead compound for the discovery of highly active immune-inducing agents.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1021/acs.jafc.4c05674 | DOI Listing |
Pestic Biochem Physiol
November 2025
Shenyang Agricultural University, College of Plant Protection, Shenyang, Liaoning 110866, PR China. Electronic address:
As the weed Echinochloa phyllopogon has rapidly developed multi- and cross-resistance to several herbicides, we aimed to determine the mechanism underlying penoxsulam resistance in weeds. There was no target mutation in the tested population, and P450 enzyme activity was significantly higher in the penoxsulam-treated resistant population, confirming that non-target-site resistance was dominant. The antioxidant enzyme activity of the resistant population was higher than that of the sensitive population following the application of the penoxsulam and cleared HO faster.
View Article and Find Full Text PDFMol Divers
September 2025
Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
Tilorone, a 9-fluorenone scaffold-based molecule, is a known broad-spectrum antiviral with an IC of 180 nM against SARS-CoV-2, but its mechanism is not known. In the present study, we found it to have weak activity against PLpro (IC = 30.7 ± 7.
View Article and Find Full Text PDFBioorg Chem
August 2025
Department of Chemistry, Faculty of Science, Atatürk University, 25240 Erzurum, Türkiye. Electronic address:
Compounds that possess a benzene sulfonamide structure are utilized in a wide range of fields. Benzene bissulfonamides are also important compounds in the field of organic and medicinal chemistry. Based on these features, a series of benzene bissulfonamides were synthesized in moderate yields starting from 3-methylanisole.
View Article and Find Full Text PDFBioorg Chem
August 2025
Wenzhou Medical University, Wenzhou 325035, PR China; Zhejiang Cancer Hospital, Hangzhou 310022, PR China. Electronic address:
Transcriptional enhanced associate domain (TEAD), overexpressed in hepatocellular carcinoma (HCC) and inversely correlated to prognosis, has emerged as a promising target for HCC therapy. To date, no small-molecule inhibitors targeting TEAD have been reported for HCC treatment. In this study, a bioinformatic analysis has been performed and has demonstrated that TEAD is a promising target for therapeutic intervention in HCC.
View Article and Find Full Text PDFJ Viral Hepat
October 2025
Clinical and Health Sciences, University of South Australia, Adelaide, South Australia, Australia.
Direct-acting antivirals (DAAs) have transformed hepatitis C virus (HCV) treatment in Australia since their inclusion on the Pharmaceutical Benefits Scheme (PBS) in 2016. Treatment has shifted from genotype-specific to pan-genotypic regimens, with glecaprevir/pibrentasvir and sofosbuvir/velpatasvir now recommended in clinical guidelines. This study examined trends in DAA dispensing in light of evolving treatment regimens.
View Article and Find Full Text PDF