Rational modification of lactams for improved efficacy in home care applications

合理修饰内酰胺以提高家庭护理应用的功效

• 批准号: 132182
• 金额: $ 3.18万
• 依托单位: UNILEVER U.K. CENTRAL RESOURCES LIMITED
• 依托单位国家: 英国
• 项目类别: Feasibility Studies
• 财政年份: 2016
• 资助国家: 英国
• 起止时间: 2016 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=132182
• 关键词: Rational; modification; lactams; improved; efficacy

Beyond removal of dirt, home and personal care formulations such as laundry detergents, kitchen and bathroomcleaners aim to deliver health and hygiene benefits in line with Unilever’s Sustainable Living Plan. These benefitsare currently delivered by chemical antimicrobials which have a limited efficacy on established biofilms. Thescreening of a library of over 600 furanone-derived lactams has revealed variants that disrupt quorum sensingand biofilm growth in model environments. This feasibility project aims to enhance the bioavailability andefficacy of lactams in home care applications via rational modification of existing principal analogues. Possibleroutes of derivatisation will range from introduction of charged groups for solubility, enhancing the 'active site'functionality, and grafting complex polymeric lactam-containing materials for targeted delivery to surfaces andbiofilms. A focused library of around 10 novel analogues will be constructed, synthesised, and their anti-biofilmefficacy will be explored against real biofilms on a range of home and industrial surfaces. The platformopportunity of improved lactams in home care will be assessed.

除了去除污垢，家庭和个人护理配方，如洗衣剂、厨房和浴室清洁剂，旨在提供符合联合利华可持续生活计划的健康和卫生效益。这些好处目前是由化学抗菌剂提供的，对已建立的生物膜的功效有限。筛选了600多个呋喃酮衍生内酰胺的文库，揭示了在模型环境中破坏群体感应和生物膜生长的变体。本可行性项目旨在通过对现有主要类似物进行合理修饰，提高内酰胺类药物在家庭护理中的生物利用度和有效性。衍生化的可能途径包括引入带电基团以提高溶解度，增强“活性位点”的功能，以及接枝含有复杂聚合物内酰胺的材料以靶向递送到表面和生物膜。将构建、合成一个大约10种新型类似物的重点库，并在一系列家庭和工业表面上探索其抗生物膜的功效。将评估改进内酰胺在家庭护理中的平台机会。