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新型脂肪族磺酰胺的合成、表征及抗菌活性

Synthesis, characterization and antimicrobial activity of new aliphatic sulfonamide.

作者信息

Ozbek Neslihan, Katircioğlu Hikmet, Karacan Nurcan, Baykal Tülay

机构信息

Ahi-Evran University, Kirsehir Education Faculty, Kirsehir [corrected] Turkey.

出版信息

Bioorg Med Chem. 2007 Aug 1;15(15):5105-9. doi: 10.1016/j.bmc.2007.05.037. Epub 2007 May 18.

Abstract

A series of novel aliphatic sulfonamide derivatives (1-7) were synthesized and characterized by elemental analyses, FT-IR, (1)H NMR, (13)C NMR and LC-MS techniques. All the synthesized compounds were evaluated in vitro as antimicrobial agents against representative strains of Gram-positive (Staphylococcus aureus ATCC 25953, Bacillus cereus ATCC 6633 and Listeria monocytogenes ATCC Li6 (isolate), Gram-negative bacteria (Escherichia coli ATCC 11230) and antifungal agent against Candida albicans (clinical isolate) by both disc diffusion and minimal inhibition concentration (MIC) methods. All these bacteria and fungus studied were screened against some antibiotics to compare with our chemicals' zone diameters. Our aliphatic sulfonamides have highest powerful antibacterial activity for Gram-negative bacteria than Gram-positive bacteria and antibacterial activity decreases as the length of the carbon chain increases.

摘要

合成了一系列新型脂肪族磺酰胺衍生物(1-7),并通过元素分析、傅里叶变换红外光谱(FT-IR)、核磁共振氢谱(¹H NMR)、核磁共振碳谱(¹³C NMR)和液相色谱-质谱(LC-MS)技术对其进行了表征。通过纸片扩散法和最低抑菌浓度(MIC)法,对所有合成化合物进行了体外抗菌活性评价,测试其对革兰氏阳性菌(金黄色葡萄球菌ATCC 25953、蜡样芽孢杆菌ATCC 6633和单核细胞增生李斯特菌ATCC Li6(分离株))、革兰氏阴性菌(大肠杆菌ATCC 11230)的抗菌活性以及对白色念珠菌(临床分离株)的抗真菌活性。针对所有这些研究的细菌和真菌,筛选了一些抗生素以与我们化合物的抑菌圈直径进行比较。我们的脂肪族磺酰胺对革兰氏阴性菌的抗菌活性比对革兰氏阳性菌的抗菌活性更强,并且随着碳链长度的增加,抗菌活性降低。

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