Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Eur J Med Chem. 2009 Nov;44(11):4522-7. doi: 10.1016/j.ejmech.2009.06.020. Epub 2009 Jun 26.
In the present investigation a series of novel 2-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazol-4-yl]-5-(substituted-phenyl)-[1,3,4]oxadiazoles (4a-j) were synthesized by cyclization of substituted-benzoic acid N'-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazole-4-carbonyl]-hydrazide by using phosphorousoxychloride at 120 degrees C. The chemical structure of the newly synthesized compounds was characterized by analytical and spectral (IR, (1)H NMR, (13)C NMR and LC-MS) methods. The title compounds were screened for qualitative (zone of inhibition) and quantitative antibacterial activity (MIC) by agar cup plate and microtitration methods, respectively. Among the synthesized compounds in this series compound 2-[1-(5-chloro-2-methoxyphenyl)-5-methyl-1H-pyrazol-4-yl]-5-(4-fluorophenyl)-1,3,4-oxadiazole (4b) was found to exhibit significant antibacterial activity with MICs of 22.4, 29.8, 29.6 and 30.0 microg/mL against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae, respectively. The other compounds exhibited moderate activity when compared to standard substance Ampicillin.
在本研究中,通过用亚磷酰氯在 120°C 下环化取代苯甲酰基 N'-[1-(5-氯-2-甲氧基苯基)-5-甲基-1H-吡唑-4-羰基]-肼,合成了一系列新型 2-[1-(5-氯-2-甲氧基苯基)-5-甲基-1H-吡唑-4-基]-5-(取代苯基)-[1,3,4]恶二唑(4a-j)。新合成化合物的化学结构通过分析和光谱(IR、(1)H NMR、(13)C NMR 和 LC-MS)方法进行了表征。通过琼脂杯盘法和微量滴定法分别对标题化合物进行定性(抑菌圈)和定量(MIC)抗菌活性筛选。在所合成的化合物中,化合物 2-[1-(5-氯-2-甲氧基苯基)-5-甲基-1H-吡唑-4-基]-5-(4-氟苯基)-1,3,4-恶二唑(4b)表现出显著的抗菌活性,对枯草芽孢杆菌、金黄色葡萄球菌、大肠杆菌和肺炎克雷伯菌的 MIC 分别为 22.4、29.8、29.6 和 30.0μg/mL。与标准物质氨苄西林相比,其他化合物的活性中等。