Copper Complexes with Antibacterial Activity

具有抗菌活性的铜配合物

• 批准号: 2744812
• 金额: --
• 依托单位: Durham University
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2022
• 资助国家: 英国
• 起止时间: 2022 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2744812
• 关键词: Copper; Complexes; Antibacterial; Activity

Antibiotic resistance is a major issue worldwide, leading to many deaths, particularly in developing countries. An enzyme family, the metallo-beta-carbapenemases, have recently been identified as a an important target to overcome antibiotic resistance. Copper complexes are effective at inhibiting this enzyme through transmetallation. In this PhD project, we will design, synthesise and analyse series of copper pyrithione complexes, which are proposed to be effective inhibitors of the carbapenemase enzymes. We will develop structure to activity relationships and identify important properties of the complexes, such as solubility, lipophilicity, bacterial cell uptake and biological activity against the resistant bacteria. The project combines synthetic chemistry with aspects of biochemistry. Our collaborators in India will be involved with the bacterial testing against antibiotic resistant bacteria.

抗生素耐药性是世界范围内的一个主要问题，导致许多人死亡，特别是在发展中国家。金属-β-碳青霉烯酶是一个重要的酶家族，近年来被认为是克服抗生素耐药性的重要靶标。铜络合物通过transmetabolic有效抑制这种酶。在这个博士项目中，我们将设计，合成和分析一系列的铜吡啶络合物，这被认为是碳青霉烯酶的有效抑制剂。我们将开发结构与活性的关系，并确定复合物的重要性质，例如溶解度、亲脂性、细菌细胞吸收和针对耐药细菌的生物活性。该项目将合成化学与生物化学的各个方面结合起来。我们在印度的合作者将参与针对抗生素耐药性细菌的细菌测试。