377767-11-8Relevant articles and documents
Discovery of novel triazole-containing pyrazole ester derivatives as potential antibacterial agents
Chu, Ming-Jie,Wang, Wei,Ren, Zi-Li,Liu, Hao,Cheng, Xiang,Mo, Kai,Wang, Li,Tang, Feng,Lv, Xian-Hai
, (2019/04/05)
To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound 4d exhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 μg/mL, 2 μg/mL, 4 μg/mL, and 0.5 μg/mL against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay 4d displayed the most potent topoisomerase II (IC50 = 13.5 μg/mL) and topoisomerase IV (IC50 = 24.2 μg/mL) inhibitory activity. Molecular docking was performed to position compound 4d into the topoisomerase II active site to determine the probable binding conformation. In summary, compound 4d may serve as potential topoisomerase II inhibitor.
Discovery of novel double pyrazole Schiff base derivatives as anti-tobacco mosaic virus (TMV) agents
Lv, Xian-Hai,Ren, Zi-Li,Li, Dong-Dong,Ruan, Ban-Feng,Li, Qing-Shan,Chu, Ming-Jie,Ai, Cheng-Ying,Liu, Dao-Hong,Mo, Kai,Cao, Hai-Qun
, p. 377 - 382 (2017/01/28)
Many pyrazole derivatives were reported to exhibit highly activity towards tobacco mosaic virus (TMV). In this work, an optimized pyrazole Schiff base scaffold was designed and introduced to derive novel potential TMV inhibitors. Thirty-six compounds were synthesized, characterized by elemental analysis, mass spectra and nuclear magnetic resonance (NMR) spectroscopy and evaluated by biological experiments. The bioassay results showed that some of the synthesized compounds exhibited excellent anti-TMV activities. Especially, 5-chloro-3-methyl-1H-pyrazole contained compound 4j showed ningnanmycin comparable inhibitory activity and can be considered as potential anti-TMV candidate agent. With molecular docking, compound 4j insert into nucleotide sequence (GAAGUU) of OriRNA stably which revealed nucleotide could be a target of these compounds.