169899-58-5Relevant articles and documents
Novel coumarin-thiazolyl ester derivatives as potential DNA gyrase Inhibitors: Design, synthesis, and antibacterial activity
Cheng, Xiang,Chu, Zhi-Wen,Hu, Rui,Liu, Hao,Lv, Xian-Hai,Xia, Dong-Guo
, (2020)
The design and synthesis of novel coumarin-thiazolyl ester derivatives of potent DNA gyrase inhibitory activity were the main aims of this study. All the novel synthesized compounds were examined for their antibacterial activity against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli and Salmonella. Compound 8p exhibited excellent antibacterial activity against four bacteria strains with MIC values of 0.05, 0.05, 8, and 0.05 μg/mL, respectively. In vitro drug-resistant bacterial inhibition experiments indicated that compound 8p exhibited the best bacteriostatic effect in the selected compounds and four positive control drugs with MIC values of 4 μg/mL. In vitro enzyme inhibitory assay showed that compound 8p exhibited potent inhibition against DNA gyrase with IC50 values of 0.13 μM. The molecular docking model indicated that compounds 8p can bind well to the DNA gyrase by interacting with amino acid residues. This study demonstrated that the compound 8p can act as the most potent DNA gyrase inhibitor in the reported series of compounds and provide valuable information for the commercial DNA gyrase inhibiting bactericides.
Coumarin derivative as - well as preparation method and application thereof (by machine translation)
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Paragraph 0037; 0040, (2020/01/03)
The coumarin-thiazole ester derivative has a broad-spectrum antibacterial activity, and the coumarin,thiazole ester derivative has, a broad-spectrum antibacterial activity, so that 4 the coumarin 7-thiazole, ester derivative has a DCC, DMAP, broad 0 °C-spectrum 10 - 15 antibacterial activity, and the application is a novel antibacterial, agent developed with coumarin-thiazole ester, derivatives as active ingredients 24. (by machine translation)
Thiazolium-catalyzed additions of acylsilanes: A general strategy for acyl anion addition reactions
Mattson, Anita E.,Bharadwaj, Ashwin R.,Zuhl, Andrea M.,Scheidt, Karl A.
, p. 5715 - 5724 (2007/10/03)
A strategy utilizing N-heterocyclic carbenes (NHCs) derived from thiazolium salts has been developed for the generation of carbonyl anions from acylsilanes. Synthetically useful 1,4-diketones and N-phosphinoyl-α- aminoketones have been prepared in good to excellent yields via NHC-catalyzed additions of acylsilanes to the corresponding α,β-unsaturated systems and N-phosphinoylimines. These organocatalytic reactions are air- and water-tolerant methods to execute robust carbonyl anion addition reactions. Additionally, polysubstituted aromatic furans and pyrroles have been efficiently synthesized in a one-pot process using this carbonyl anion methodology. The addition of alcohols to the reaction renders the process catalytic in thiazolium salt. In an effort to synthesize a potential intermediate along the proposed reaction pathway, silylated thiazolium carbinols have been identified to provide good yields of carbonyl anion addition products when subjected to the standard reaction conditions in the presence of suitable electrophiles.