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5-(苯并[d][1,3]二氧杂环戊烯-5-基)-3-叔丁基-1-取代-4,5-二氢吡唑的设计、合成及抗菌潜力

Design, synthesis and antibacterial potential of 5-(benzo[d][1,3]dioxol-5-yl)-3-tert-butyl-1-substituted-4,5-dihydropyrazoles.

作者信息

El-Behairy Mohammed F, Mazeed Tarek E, El-Azzouny Aida A, Aboul-Enein Mohamed N

机构信息

Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, 12622 Dokki, Giza, Egypt.

Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, 12622 Dokki, Giza, Egypt.

出版信息

Saudi Pharm J. 2015 Apr;23(2):202-9. doi: 10.1016/j.jsps.2014.07.009. Epub 2014 Jul 28.

Abstract

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 110 nM, respectively. While hydroxypiperidinoethanone derivative 6c showed MIC at 90 nM for Sarcina.

摘要

已合成了一系列5-(苯并[d][1,3]二氧杂环戊烯-5-基)-3-叔丁基-1-取代-4,5-二氢吡唑衍生物4a - e和6a - g,并对其进行了光谱表征。使用琼脂扩散试验筛选了这些新型候选物的抗菌活性。与标准抗菌药物相比,这些化合物对不同的革兰氏阳性菌和革兰氏阴性菌具有高抗菌活性。根据抑菌圈和最低抑菌浓度结果,八叠球菌和金黄色葡萄球菌是最敏感的细菌,其中吡咯烷甲酮衍生物4e对八叠球菌和金黄色葡萄球菌的最低抑菌浓度分别为80和110 nM。而羟基哌啶基乙酮衍生物6c对八叠球菌的最低抑菌浓度为90 nM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/663e/4421084/ec9725175f0e/gr1.jpg

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