Rational modification of lactams for improved efficacy in home care applications

除了去除污垢外，家庭和个人护理配方，如洗衣粉、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益处。这些好处目前是通过化学抗菌剂实现的，这些抗菌剂对已建立的生物膜效果有限。对600多种呋喃酮类内酰胺类药物的文库进行筛选后，发现了在模拟环境中扰乱群体感知和生物膜生长的变异。这一可行性项目旨在通过合理修改现有的主要类似物来提高内酰胺类药物在家庭护理应用中的生物利用度和有效性。衍生化的可能路线包括引入可溶解的带电基团，增强活性部位的功能，以及将含有内酰胺类的复杂聚合物材料定向输送到表面和生物膜上。将构建、合成约10种新型类似物的焦点文库，并将在一系列家庭和工业表面以真实生物膜为对照进行研究。将评估改进内酰胺类药物在家庭护理中的平台机会。

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.