Department of Pharmaceutical Chemistry, Anadolu University, Eskişehir, Turkey.
J Enzyme Inhib Med Chem. 2012 Dec;27(6):868-74. doi: 10.3109/14756366.2011.622273. Epub 2011 Oct 15.
In this work, some N-(9-Ethyl-9H-carbazole-3-yl)-2-(phenoxy)acetamide derivatives were synthesised and evaluated for their antimicrobial activity and cytotoxicity. The structural elucidation of the compounds was performed by IR, (1)H-NMR, (13)C-NMR and FAB(+)-MS spectral data and elemental analyses. The title compounds were obtained by reacting 2-chloro-N-(9-ethyl-9H-carbazole-3-yl)acetamide with some substituted phenols. The synthesised compounds were investigated for their antibacterial and antifungal activities against Micrococcus luteus, Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Listeria monocytogenes and Candida albicans. The compounds N-(9-Ethyl-9H-carbazole-3-yl)-2-(4-ethylphenoxy)acetamide (2c) and N-(9-Ethyl-9H-carbazole-3-yl)-2-(quinolin-8-yloxy)acetamide (2n) showed notable antimicrobial activity. The compounds were also studied for their cytotoxic effects using MTT assay, and it was seen that 2n had the lowest cytotoxic activity against NIH/3T3 cells.
在这项工作中,我们合成了一些 N-(9-乙基-9H-咔唑-3-基)-2-(苯氧基)乙酰胺衍生物,并评估了它们的抗菌活性和细胞毒性。通过 IR、(1)H-NMR、(13)C-NMR 和 FAB(+)-MS 光谱数据和元素分析对化合物的结构进行了阐明。标题化合物是通过将 2-氯-N-(9-乙基-9H-咔唑-3-基)乙酰胺与一些取代的苯酚反应得到的。我们研究了合成的化合物对微球菌、枯草芽孢杆菌、铜绿假单胞菌、金黄色葡萄球菌、大肠杆菌、单核细胞增生李斯特菌和白色念珠菌的抗菌和抗真菌活性。化合物 N-(9-乙基-9H-咔唑-3-基)-2-(4-乙基苯氧基)乙酰胺(2c)和 N-(9-乙基-9H-咔唑-3-基)-2-(喹啉-8-氧基)乙酰胺(2n)表现出显著的抗菌活性。我们还通过 MTT 测定法研究了这些化合物的细胞毒性作用,结果表明 2n 对 NIH/3T3 细胞的细胞毒性最低。