Skeletal editing of single-atom insertion to basic chemicals has been demonstrated as an efficient strategy for the discovery of structurally diversified compounds. Previous endeavors in skeletal editing have successfully facilitated the insertion of boron, nitrogen, and carbon atoms. Given the prevalence of oxygen atoms in biologically active molecules, the direct oxygenation of C-C bonds through single-oxygen-atom insertion like Baeyer-Villiger reaction is of particular significance.
View Article and Find Full Text PDF(1) Background: Scopoletin and scoparone, two naturally occurring coumarins, have garnered considerable attention and have been introduced to the market in China due to their high insecticidal efficacy and low toxicity. To investigate the structure-activity relationship of these coumarins, a series of scopoletin derivatives with aryl sulfate at C7 and different substitutes at C3 were designed and synthesized, and their insecticidal activity was studied. (2) Methods: A total of 28 new scopoletin derivatives were designed and synthesized.
View Article and Find Full Text PDFABTRACTThis study aims to design and synthesize a series of N-Acyl-N-(m-fluoro- benzyl)-6- amino-coumarins through the principle of active substructure stitching, which are based on the core structure of N-(m-fluoro-benzyl)-6-amino-coumarin. The structures of target compounds have been characterized by H NMR, C NMR, ESI-MS and elemental analysis. Meanwhile, their agricultural activity have been evaluated in two weeds ( and ) and four widespread noxious pathogens ( and ).
View Article and Find Full Text PDFSeries of thioether derivatives containing 4-methylumbelliferone fused oxazole moiety were designed and synthesised, their structures were fully characterized by H NMR, C NMR and HR-ESI-MS as well. Moreover, the antifungal potency of the title compounds were preliminarily evaluated for their possible use as a fungicide. Meanwhile, ethyl thioethers and displayed remarkable inhibitory effect against the mycelium growth of and with EC of 12-16 μg/mL.
View Article and Find Full Text PDFIn our research, a series of 8-substituted coumarin derivatives were synthesized, and their structures were confirmed by FT-IR, H-NMR, and MS (or HRMS). In activity screening, the synthesized compounds exhibited potent antifungal activity against 4 phytopathogenic fungi: , , , and . Notably, 8-chloro coumarin and ethyl 8-chloro-coumarin3-carboxylate showed the strongest fungus inhibition with EC of 0.
View Article and Find Full Text PDFA series of novel trifluoromethylcoumarinyl urea derivatives were designed, synthesized, and characterized by ¹H-NMR, C-NMR, and HR-ESI-MS. The fluorescence spectra of the target compounds were recorded. The spectra show that most of the title compounds glow green with λ of 500-517 nm, while compounds , , , and (compounds named by authors) glow violet with λ of 381-443 nm.
View Article and Find Full Text PDFA series of novel 4-methylumbelliferone amide derivatives were designed, synthesized and characterized by ¹H NMR, C NMR and HR-ESI-MS. The structures of compounds and (compounds named by authors) were further confirmed by X-ray single crystal diffraction. The acaricidal, herbicidal and antifungal activities of the synthesized compounds were assayed for their potential use as pesticide.
View Article and Find Full Text PDFTwelve angular oxazole-fused coumarin derivatives were designed, synthesised and characterised by H NMR, C NMR and HRMS. The structure of compound 4a was further confirmed by X-ray single-crystal diffraction. The bioassay experiment results indicated that compounds 4f and 4l have high antifungal activity on the mycelium growth of 4 plant disease fungi.
View Article and Find Full Text PDFEnvironmentally friendly hypervalent iodine reagents are unusually effective promoters of asymmetric α-functionalization of carbonyl compounds. By using hypervalent iodine reagents, various substituents can be introduced into the α-position of carbonyl compounds. In the present review, we briefly survey the asymmetric α-functionalization of carbonyl compound reactions catalyzed by these hypervalent iodine reagents.
View Article and Find Full Text PDFRecently our group has demonstrated that cellular triglyceride (TG) levels play an important role in rotavirus replication. In this study, we further examined the roles of the key enzymes for TG synthesis (lipogenesis) in the replication of rotaviruses by using inhibitors of fatty acid synthase, long chain fatty acid acyl-CoA synthetase (ACSL), and diacylglycerol acyltransferase and acyl-CoA:cholesterol acyltransferase in association with lipid droplets of which TG is a major component. Triacsin C, a natural ACSL inhibitor from Streptomyces aureofaciens, was found to be highly effective against rotavirus replication.
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