合成及体外微生物评价一系列生物可裂解的 2-吗啉基-N-(4,6-二芳基嘧啶-2-基)乙酰胺。
Synthesis and in vitro microbiological evaluation of an array of biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides.
机构信息
Synthetic Organic Chemistry Laboratory, Department of Chemistry, Annamalai University, Annamalainagar 608 002, Tamil Nadu, India.
出版信息
Eur J Med Chem. 2010 Apr;45(4):1583-9. doi: 10.1016/j.ejmech.2009.12.068. Epub 2010 Jan 14.
Biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides 34-42 have been synthesized and evaluated for their in vitro antibacterial and antifungal activities. The minimum inhibitory concentration tested for the same compounds against the same set of bacterial and fungal strains shows that the compounds 36 and 38 against beta-Heamolytic streptococcus and Klebsiella pneumonia, 40 against Escherichia coli and Pseudomonas, have excellent antibacterial activity. Compounds 36, 38 and 42 show inhibition against Aspergillus flavus, compound 41 against Microsporum gypsuem, 42 against Mucor, and compounds 39 and 40 against Rhizopus.
生物不稳定的 2-吗啉基-N-(4,6-二芳基嘧啶-2-基)乙酰胺 34-42 已被合成并评估其体外抗菌和抗真菌活性。针对相同化合物对相同的细菌和真菌菌株的最小抑菌浓度测试表明，化合物 36 和 38 对β-溶血性链球菌和肺炎克雷伯菌、40 对大肠杆菌和假单胞菌具有极好的抗菌活性。化合物 36、38 和 42 对黄曲霉有抑制作用，化合物 41 对石膏样小孢子菌有抑制作用，42 对毛霉有抑制作用，化合物 39 和 40 对根霉有抑制作用。
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