51649-80-0Relevant articles and documents
Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
Dos Santos, Maurício Silva,Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo
, p. 335 - 343 (2021/09/07)
Hybrid systems containing pyrazole moiety show a wide spectrum of biological activities. To access novel hybrids with pyrazole ring, in this work we synthesized twenty pyrazole-carboxylic acids and twenty pyrazole-carboxamides, using simple synthetic methods, to be used as building blocks in the development of new structures.
Discovery of novel multi-substituted benzo-indole pyrazole schiff base derivatives with antibacterial activity targeting DNA gyrase
Cao, Hai-Qun,Chu, Zhi-Wen,Liu, Hao,Lv, Xian-Hai,Xia, Dong-Guo
, (2020/04/08)
The design and synthesis of novel multi-substituted benzo-indole pyrazole Schiff base derivatives of potent DNA gyrase inhibitory activity were the main aims of this study. All the novel synthesized compounds were examined for their antibacterial activities against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella. In addition, we selected 20 compounds for the in vitro antibacterial activities assay of 6 drug-resistant bacteria strains. The result revealed compound 8I-w exhibited excellent antibacterial activity against 4 drug-resistant E. coli bacteria strains with IC50 values of 7.0, 17.0, 13.5, and 1.0 μM, respectively. In vitro enzyme inhibitory assay showed that compound 8I-w displayed potent inhibition against DNA gyrase with IC50 values of 0.10 μM. The molecular docking model indicated that compounds 8I-w can bind well to the DNA gyrase by interacting with various amino acid residues. This study demonstrated that the compound 8I-w 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.
Pyrazolo pyrimidine derivative and its preparation method and application (by machine translation)
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, (2019/10/23)
The invention discloses a pyrazolo pyrimidine ketone derivatives, wherein R1 For nicotinic acid, isonicotinic acid, 2 - chloro nicotinic acid, 6 - chloro nicotinic acid, 2 - bromo nicotinic acid, 6 - bromo nicotinic acid, 2 - fluoro nicotinic acid, 6 - fluoro nicotinic acid, 6 - methoxy nicotinic acid or 2 - methoxy nicotinic acid; R2 Hydrogen, fluoro, chloro or methyl; R3 Is hydrogen or methyl. Also disclosed the preparation method of the derivative and application, by chemical synthetic way to synthesize 40 for the purpose of the compound, and further by the introduction of the the purpose of the chiral compound to the secondary structure is optimized, so that the preparation of the pyrazole and pyrimidinone derivatives with broad-spectrum of cooperativity antifungal activity, in particular to the apple rot bacteria and germ inhibiting activity represent significant; the application in order to develop pyrazolo pyrimidine compound derivatives as the active ingredient to provide the basis for a novel bactericide. (by machine translation)