首页> 外文期刊>Saudi Pharmaceutical Journal >Design, synthesis and antibacterial potential of 5-(benzo[d][1,3]dioxol-5-yl)-3-tert-butyl-1-substituted-4,5-dihydropyrazoles
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Design, synthesis and antibacterial potential of 5-(benzo[d][1,3]dioxol-5-yl)-3-tert-butyl-1-substituted-4,5-dihydropyrazoles

机译:5-(苯并[d] [1,3]二恶酚-5-基)-3-叔丁基-1-取代的4,5-二氢吡唑的设计,合成及抗菌潜力

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A series of 5-(benzo[d][1,3]dioxol-5-yl)-3-tert-butyl-1-substituted-4,5-dihydropyrazole derivatives 4a-e and 6a-g have been synthesized and spectrally characterized. The antibacterial activity of the novel candidates has been screened using the agar diffusion test. These compounds were endowed with high antibacterial activity against different Gram +ve and Gram -ve bacteria when compared with standard antibacterial drugs. In the light of zone of inhibition and MIC results, Sarcina and Staphylococcus aureus are the most sensitive bacteria where pyrrolidinomethanone derivative 4e showed MICs at 80 and 110nM, respectively. While hydroxypiperidinoethanone derivative 6c showed MIC at 90nM for Sarcina.
机译:合成了一系列5-(苯并[d] [1,3]二氧杂-5-基)-3-叔丁基-1-取代的4,5-二氢吡唑衍生物4a-e和6a-g,并进行了光谱分析表征。使用琼脂扩散试验已经筛选出了新候选药物的抗菌活性。与标准抗菌药物相比,这些化合物具有对不同革兰氏+ ve和革兰氏-ve细菌的高抗菌活性。根据抑制区和MIC结果,Sarcina和金黄色葡萄球菌是最敏感的细菌,吡咯烷二甲酮衍生物4e分别显示80nM和110nM的MIC。羟哌啶酮乙酮衍生物6c对Sarcina的MIC为90nM。

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