Microwave-assisted Synthesis of Novel Pyrazole Derivatives and their Biological Evaluation as Anti-Bacterial Agents.

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING(2021)

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摘要
AIMS AND OBJECTIVES:Microwave-assisted condensation of acetophenone 1 and aromatic aldehydes 2 gave chalcone analogs 3, which were cyclized to pyrazole derivatives 6a-f via the reaction with hydrazine hydrate and oxalic acid in the presence of the catalytic amount of acetic acid in ethanol. MATERIALS AND METHODS:The structural features of the synthesized compounds were characterized by melting point, FT-IR, 1H, 13C NMR and elemental analysis. RESULTS:The antibacterial activities of the synthesized pyrazoles were evaluated against three gram-positive bacteria, such as Enterococcus durans, Staphylococcus aureus, Bacillus subtilis and two gram-negative bacteria such as Escherichia coli and Salmonella typhimurium. CONCLUSION:All the synthesized pyrazoles showed relatively high antibacterial activity against S. aureus strain, and none of them demonstrated antibacterial activity against E. coli.
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关键词
Pyrazole, chalcone, microwave assisted, antibacterial, FT-IR, H-1 NMR, C-13 NMR
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