3,5-二甲基吡唑衍生物的合成与抑菌活性

Synthesis and Antibacterial Activity of 3,5-Dimethylpyrazole Derivatives

取代肼与乙酰丙酮在室温下反应直接合成了3种3,5-二甲基吡唑衍生物a~c,收率分别为45.6%~65.8%,目标产物经IR、1H NMR、13C NMR表证。通过对金黄色葡萄球菌(Staphylococcus aureus)粪肠球菌(Enterococcus faecalis)、肺炎链球菌(Streptococcus pneumoniae)、铜绿假单胞菌(Pseudomonas aeruginosa)、大肠埃希菌(Escherichia coli)、阴沟肠杆菌(Enterobacter cloacae) 6个菌种的体外抑菌活性试验,结果表明化合物c对铜绿假单胞菌有较强的抑菌活性,其最低抑菌浓度(MIC)为64μg/mL。

Three 3,5-dimethlprazole derivatives a~c were synthesized from substituted hydrazine and acetylacetone at room temperature with yields of 45.6%~65.8%. Their structures were confirmed by IR, 1H NMR and 13C NMR. Their antibacterial activity in vitro were tested for Staphylococcus aureus, Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas aeruginosa, Escherichia coli and Enterobacter cloacae, and the results showed that the compound c has strong antibacterial activity against Pseudomonas aeruginosa with a minimum inhibitory concentration(MIC) of 64 μg/mL.