The first oxidative chloro- and bromodifluoromethylation of phenols with (CH)SiCFX and CuX (X = Cl or Br) in the presence of Selectfluor under mild reaction conditions was developed. This protocol provided a practical and efficient method for the synthesis of a diverse range of biologically valuable and synthetically challenging chloro- and bromodifluoromethyl aryl ethers. Preliminary mechanistic studies suggest that this reaction proceeded through a difluorocarbene-involved oxidative coupling process.
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http://dx.doi.org/10.1021/jacs.3c08858 | DOI Listing |
Front Immunol
January 2025
Department of Biophysics and Cell Biology, Faculty of Medicine, University of Debrecen, Debrecen, Hungary.
The human voltage-gated proton channel (H1) provides an efficient proton extrusion pathway from the cytoplasm contributing to the intracellular pH regulation and the oxidative burst. Although its pharmacological inhibition was previously shown to induce cell death in various cell types, no such effects have been examined in polarized macrophages albeit H1 was suggested to play important roles in these cells. This study highlights that 5-chloro-2-guanidinobenzimidazole (ClGBI), the most widely applied H1 inhibitor, reduces the viability of human THP-1-derived polarized macrophages at biologically relevant doses with M1 macrophages being the most, and M2 cells the least sensitive to this compound.
View Article and Find Full Text PDFSe Pu
January 2025
School of Public Health, Nanjing Medical University, Nanjing 211166, China.
Chlorinated coumarins, which are as cytotoxic as highly toxic halobenzoquinones toward CHO-K1 cells, have recently been identified as disinfection byproducts in drinking water disinfection processes. Therefore, detecting coumarins in water samples collected at various stages from drinking water treatment plants helps assess the formation of chlorinated coumarins in drinking water. Hence, a simple, rapid, accurate, and sensitive method for quantifying coumarins in water samples is required.
View Article and Find Full Text PDFActa Crystallogr E Crystallogr Commun
October 2024
Department of Inorganic Chemistry and Technology, Jožef Stefan Institute, Jamova 39, 1000 Ljubljana, Slovenia.
The crystal structure of the title organic-inorganic hybrid salt, (CHN)[CdCl], (I), has been reported with four mol-ecules in the asymmetric unit in a monoclinic cell [Vassilyeva (2021 ▸). , , 7713-7722]. While using two different aldehydes in the oxidative cyclization-condensation involving CHNH·HCl to prepare a new monovalent cation with the imidazo[1,5-]pyridinium skeleton, a new polymorph was obtained for (I) in space group 1 and a unit cell with approximately half the volume of the monoclinic form.
View Article and Find Full Text PDFArch Pharm (Weinheim)
January 2025
Shanghai Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Shanghai, China.
Bacteria biofilm infection seriously challenges clinical drug therapy. Nitric oxide (NO) was reported to disperse biofilm, eliminate bacteria resistance and kill bacteria. In this study, on the basis of membrane targeting of α-mangostin (α-MG) and the dispersion effect of NO on bacteria biofilms, we designed and synthesized 30 NO donors that α-MG was conjugated with a nitrobenzene or a nitrate and other four representative reference derivatives.
View Article and Find Full Text PDFBiosens Bioelectron
December 2024
Institute of Agricultural Engineering, ARO, Volcani Institute, Rishon LeZion, 7505101, Israel. Electronic address:
Botulinum neurotoxins (BoNT), the agent causing botulism, exhibit the highest potency among bacterial toxins and pose a significant threat to both humans and animals. The current in vivo method (mouse lethality assay, MLA) is inappropriate for real-time and pen-side assessment of the occurring outbreak or case. Herein, we describe a reflective-based biosensor capable of detecting the toxin's type and activity state by competitive immunoassay and endopeptidase activity, respectively.
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