合成及脲和硫脲的氮丙啶衍生物的生物活性评价。
Synthesis and Evaluation of Biological Activities of Aziridine Derivatives of Urea and Thiourea.
机构信息
Department of Microbial Genetics, Faculty of Biology and Environmental Protection, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland.
Department of Organic and Applied Chemistry, Faculty of Chemistry, University of Lodz, Tamka 12, 91-403 Lodz, Poland.
出版信息
Molecules. 2017 Dec 25;23(1):45. doi: 10.3390/molecules23010045.
In the present paper, we report the synthesis and evaluation of in vitro antimicrobial activities of aziridine-thiourea derivatives. A series of aziridines in reaction with isocyanates and isothiocyanates to obtain urea and thiourea derivatives were used. The structures of all new products were confirmed based on spectroscopic data (¹H-NMR, C-NMR, HR-MS). These compounds were screened for their in vitro antimicrobial activity against a panel of Gram-positive and Gram-negative strains of bacteria. Six of the tested compounds appeared to be promising agents against reference strains of , and . Subsequently, compounds exhibiting promising antibacterial activity were tested against twelve clinical isolates of from three different sources of infection. The most bactericidal compounds (MIC = 16-32 µg/mL) showed better antibacterial activity against MRSA than ampicillin and streptomycin. The in vitro cytotoxicity analysis on L929 murine fibroblast and HeLa human tumor cell line using the MTT assay allowed us to select the least toxic compounds for future investigation.
在本论文中，我们报告了氮丙啶-硫脲衍生物的合成与体外抗菌活性评价。我们使用一系列氮丙啶与异氰酸酯和异硫氰酸酯反应，得到脲和硫脲衍生物。所有新产物的结构均基于光谱数据（1H-NMR、C-NMR、HR-MS）得到确认。这些化合物对一组革兰氏阳性和革兰氏阴性细菌菌株进行了体外抗菌活性筛选。测试的六种化合物对参考菌株 、 和 表现出有希望的抗菌作用。随后，对来自三种不同感染源的十二株临床分离的 进行了抗菌活性测试。具有最杀菌活性的化合物（MIC = 16-32 µg/mL）对 MRSA 的抗菌活性优于氨苄西林和链霉素。使用 MTT 测定法对 L929 鼠成纤维细胞和 HeLa 人肿瘤细胞系进行体外细胞毒性分析，使我们能够选择毒性最低的化合物进行进一步研究。
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