85607-73-4Relevant articles and documents
1, 2, 4 - Oxadiazole Nrf2 activator - tacrine split product as well as preparation method and application thereof
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Paragraph 0022; 0025; 0069-0070; 0072; 0098; 0101, (2021/11/06)
The invention discloses 1,oxadiazole Nrf2 activator - tacrine split products as well as a preparation method and application thereof. The invention relates to an acetylcholinesterase inhibitory activity. Nrf2 Activation activity, selective screening and Morris water maze test was carried out to evaluate the compound of general formula I, II, III for the treatment of's disease (in particular, severe's disease), found to have good in vitro, in vivo activity and extremely high selectivity, and can be used as a precursor substance for further development through selective inhibition of acetylcholinesterase and activation Nrf2.
BIFUNCTION CHEMICAL EPIGENENTIC MODIFIERS AND METHODS OF USE
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, (2021/11/20)
The present disclosure relates to bifunctional chemical epigenetic modifiers, and methods of making, kits and using the bifunctional chemical epigenetic modifiers. The bifunctional chemical epigenetic modifiers can include a FK506 molecule or derivative thereof, a linker and a bifunctional ligand. The bifunctional ligand can be a histone deacetylase inhibitor.
Natural-Product-Inspired Aminoepoxybenzoquinones Kill Members of the Gram-Negative Pathogen Salmonella by Attenuating Cellular Stress Response
Mandl, Franziska A.,Kirsch, Volker C.,Ugur, Ilke,Kunold, Elena,Vomacka, Jan,Fetzer, Christian,Schneider, Sabine,Richter, Klaus,Fuchs, Thilo M.,Antes, Iris,Sieber, Stephan A.
, p. 14852 - 14857 (2016/11/23)
Gram-negative bacteria represent a challenging task for antibacterial drug discovery owing to their impermeable cell membrane and restricted uptake of small molecules. We herein describe the synthesis of natural-product-derived epoxycyclohexenones and explore their antibiotic activity against several pathogenic bacteria. A compound with activity against Salmonella Typhimurium was identified, and the target enzymes were unraveled by quantitative chemical proteomics. Importantly, two protein hits were linked to bacterial stress response, and corresponding assays revealed an elevated susceptibility to reactive oxygen species upon compound treatment. The consolidated inhibition of these targets provides a rationale for antibacterial activity and highlights epoxycyclohexenones as natural product scaffolds with suitable properties for killing Gram-negative Salmonella.