Design, Synthesis and Antibacterial Evaluation of Some New 2-Phenyl-quinoline-4-carboxylic Acid Derivatives.
Design, Synthesis and Antibacterial Evaluation of Some New 2-Phenyl-quinoline-4-carboxylic Acid Derivatives.
复制标题
一些新型2-苯基喹啉-4-羧酸衍生物的设计、合成及抗菌评价
DOI：
10.3390/molecules21030340
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发表时间：
2016-03-10
期刊：
影响因子：
--
通讯作者：
He M
中科院分区：
文献类型：
--
作者：
Wang X;Xie X;Cai Y;Yang X;Li J;Li Y;Chen W;He M
以苯胺、2-硝基苯甲醛、丁二酸为原料，经Doebner反应、酰胺化、还原、酰化、胺化等反应合成了一系列新的2-苯基喹啉-4-羧酸衍生物。所有新合成的化合物均通过1H-NMR、13 C-NMR和高分辨质谱进行了表征。这些化合物对革兰氏阴性杆菌的抗菌活性（大肠杆菌、铜绿假单胞菌）和革兰氏阳性菌采用琼脂扩散法对金黄色葡萄球菌、枯草芽孢杆菌和一株耐甲氧西林金黄色葡萄球菌（MRSA）进行了评价（抑菌圈法）和肉汤稀释法（最小抑菌浓度（MIC）），并对它们的构效关系进行了讨论。结果表明，部分化合物对金黄色葡萄球菌具有较好的抑菌活性，其中化合物5a 4和5a 7对金黄色葡萄球菌和大肠杆菌的MIC分别为64 μg/mL和128 μg/mL。MTT测定的结果说明化合物5a 4的低细胞毒性。
A series of new 2-phenyl-quinoline-4-carboxylic acid derivatives was synthesized starting from aniline, 2-nitrobenzaldehyde, pyruvic acid followed by Doebner reaction, amidation, reduction, acylation and amination. All of the newly-synthesized compounds were characterized by 1H-NMR, 13C-NMR and HRMS. The antibacterial activities of these compounds against Gram-negative (Escherichia coli, Pseudomonas aeruginosa) and Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis), as well as one strain of methicillin-resistant Staphylococcus aureus (MRSA) bacteria were evaluated by the agar diffusion method (zone of inhibition) and a broth dilution method (minimum inhibitory concentration (MIC)), and their structure-activity relationships were obtained and discussed. The results revealed that some compounds displayed good antibacterial activity against Staphylococcus aureus, and Compounds 5a4 and 5a7 showed the best inhibition with an MIC value of 64 μg/mL against Staphylococcus aureus and with an MIC value of 128 μg/mL against Escherichia coli, respectively. The results of the MTT assay illustrated the low cytotoxicity of Compound 5a4.
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影响因子：
6.7
作者：
Jordao, Alessandro K.;Novais, Juliana;Ferreira, Vitor F.
通讯作者：
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DOI：
10.3390/molecules20023170
发表时间：
2015-02-13
期刊：
Molecules (Basel, Switzerland)
影响因子：
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影响因子：
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作者：
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影响因子：
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作者：
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通讯作者：
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