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Synthesis and Evaluation of Antimicrobial and Antibiofilm Properties of A-Type Procyanidin Analogues against Resistant Bacteria in Food

机译:一种抗菌药物和抗菌药物对食物抗性细菌的抗菌药物和抗菌性能的合成与评价

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摘要

Natural A-type procyanidins have shown very interesting biological activities, such as their proven antiadherence properties against pathogenic bacteria. In order to find the structural features responsible for their activities, we describe herein the design and synthesis of six A-type procyanidin analogues and the evaluation of their antimicrobial and antibiofilm properties against 12 resistant bacteria, both Gram positive and Gram negative, isolated from organic foods. The natural A-type procyanidin A-2, which had known antiadherence activity, was also tested as a reference compound for the comparative studies. Within the series, analogue 4, which had a NO2 group on ring A, showed the highest antimicrobial activity (MIC of 10 mu g/mL) and was one of the best molecules at preventing biofilm formation (up to 40% decreases at 100 mu g/mL) and disrupting preformed biofilms (up to 40% reductions at 0.1 mu g/mL). Structure-activity relationships are also analyzed.
机译:天然A型Procyanidins已经表现出非常有趣的生物活性,例如对致病细菌的证明抗钝性。 为了找到负责其活动的结构特征,我们描述了六种型原霉素类似物的设计和合成,以及对12个抗菌细菌的抗微生物和抗生素性能的评价,克阳性和革兰氏阴性,来自有机的蛋白 食物。 已知抗钝性活性的天然A型Procyanidin A-2也被测试为对比例的参考化合物。 在系列中,在环A上具有NO2组的模拟4显示出最高的抗微生物活性(10μg/ ml的MIC),并且是在预防生物膜形成时的最佳分子之一(高达40%在100亩下降 g / ml)和破坏预制的生物膜(高达40%的降低0.1μg/ ml)。 还分析了结构 - 活动关系。

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