百里酚及其衍生物的抗菌活性及机制研究

700,000 people die of antibiotic-resistant infections every year in the world. The infections caused by methicillin-resistant Staphylococcus aureus (MRSA) pose a serious threat to human life and health, and have become a serious public health problem. Therefore, it is urgent to develop new antibiotics effective against MRSA. In this paper, we chose thymol which has certain anti-MRSA ability to modify, in order to improve its antibacterial ability and explore its antibacterial mechanism. Thy3 - TPP series compounds were synthesized by structural modification of thymol, and their anti-MRSA activities were detected to be more than 100 times higher than that of thymol. Among them, Thy3d has the best activity-toxicity window, has excellent anti-gram-positive bacteria and gram-negative bacteria effects, has significant anti-persistent bacteria effects at high concentrations, and is not easy to generate drug resistance. Using a series of methods, we demonstrated that Thy3d exerts its antibacterial effect by disrupting the bacterial cell membrane, and this drug acting on non-target proteins is not easy to induce bacterial resistance. In conclusion, Thy3d has the ability to resist multi-drug resistant bacteria and has the potential to be developed as a new antibacterial drug.