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Silica Supported Synthesis and Quorum Quenching Ability of Isoxazolones Against Both Gram Positive and Gram Negative Bacterial Pathogens

机译:二氧化硅支持革兰氏阳性和革兰氏阴性细菌病原体的二氧化唑的合成和法规淬灭能力

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摘要

Isoxazolones are synthesised using easily available, economical and reusable silica(TLC grade)catalyst. High yields are obtained in aqueous reaction system with substrate tolerance without affecting the yield. This multigram scale, purification free method exhibits prospects for a large scale use in future. These compounds were screened for their potential application as quorum quenchers in pathogenic bacteria. The prepared compounds were analysed for quorum quenching(QQ)activity on Gram negative bioreporter strain Chromobacterium violaceum by inhibiting its pigment production i. e. violacein production in a concentration dependent manner. Some Isoxazolone derivatives showed very good quorum quenching activity. Moreover these derivatives also showed very good antibiofilm activity against both Gram negative(Pseudomonas aeruginosa ATCC 27853)and Gram positive(Staphylococcus aureus ATCC 6538)bacterial human pathogens through Quorum Quenching mechanism. Isoxazolones thus have enormous potential to be exploited in the medical field against bacterial infections caused by both Gram negative and Gram positive bacterial human pathogens.
机译:使用易于可用,经济和可重复使用的二氧化硅(TLC级)催化剂合成异恶唑酮。在具有底物耐受性的水性反应系统中获得了高产量,而不会影响产量。这种多元量表,无纯化方法展示了将来大规模使用的前景。这些化合物被筛选为在致病细菌中作为法定淬火剂的潜在应用。通过抑制其色素的产生i,分析了制备的化合物在革兰氏阴性生物孢子菌菌株中的群体淬火(QQ)活性。 e。以集中依赖的方式产生紫oup。一些异恶唑酮衍生物表现出非常好的Quorum淬火活性。此外,这些衍生物还显示出对革兰氏阴性(铜绿假单胞菌ATCC 27853)和革兰氏阳性(金黄色葡萄球菌ATCC 6538)细菌性人类病原体的抗体性抗体活性非常好。因此,依氧唑酮具有在医疗领域利用巨大的潜力,以抵抗由革兰氏阴性和革兰氏阳性细菌人体病原体引起的细菌感染。

著录项

  • 来源
    《Chemistry Select》 |2021年第43期|11718-11728|共11页
  • 作者单位

    K. Salkar, Dr. M. M. Naik, Dr. L. Charya Department of Microbiology, Goa University, Taleigao Plateau, Goa-403206, India;

    Post-graduate department of Chemistry, St. Xavier’s College, Mapusa, Goa-403507, India;

    School of Chemical Sciences, Goa University, Taleigao Plateau, Goa-403206, India;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 英语
  • 中图分类 Online;
  • 关键词

    ISOXAZOLONE; silicon dioxide; ChickpeaQuorum Quenching;

    机译:异恶唑酮;二氧化硅;鹰嘴豆淬火;

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