首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis, antiproliferative and antimicrobial activity of new Mannich bases bearing 1,2,4-triazole moiety
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Synthesis, antiproliferative and antimicrobial activity of new Mannich bases bearing 1,2,4-triazole moiety

机译:新曼尼希碱轴承1,2,4-三唑部分的合成,抗增殖和抗微生物活性

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摘要

This study presents the synthesis, antiproliferative and antimicrobial evaluation of a new series of Mannich base derivatives containing 1,2,4-triazole system. New compounds were prepared by the reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with formaldehyde and various amines. The structures of the prepared compounds were confirmed by means of H-1 NMR, C-13 NMR and elemental analyses. Twelve compounds were evaluated for their in vitro antiproliferative activities against six chosen cancer cell lines. All synthesized compounds were screened for their in vitro antimicrobial activity by using the agar dilution technique. For 17 potentially active compounds, their antibacterial activity was confirmed on the basis of MIC (minimal inhibitory concentration) by broth microdilution method using the reference Grampositive and Gram-negative bacterial strains.
机译:本研究介绍了含有1,2,4-三唑体系的新系列曼尼希碱衍生物的合成,抗增殖和抗微生物评价。 通过将4,5-二取代的1,2,4-三唑-3-酮与甲醛和各种胺的反应制备新化合物。 通过H-1 NMR,C-13 NMR和元素分析证实制备的化合物的结构。 评估12种化合物,对其对六种选择的癌细胞系进行体外抗增殖活动。 通过使用琼脂稀释技术筛选所有合成的化合物对其体外抗微生物活性进行筛选。 对于17个潜在的活性化合物,通过使用参考晶体和革兰氏阴性细菌菌株的肉汤微冰氧化方法基于MIC(最小抑制浓度)来确认它们的抗菌活性。

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