标题：Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASH) System Enzymes as Potential Antibacterial Agents
作者：Yi Wang;Shutao Ma
作者机构：[Wang, Y] Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong U 更多
通讯作者地址：[Ma, ST]Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, 44 West Culture Rd, Jinan 250012, Peoples R China.
关键词：acyl carrier protein;antibacterial agents;inhibitors;fatty acid synthesis type II;medicinal chemistry
摘要：Bacterial infections are a constant and serious threat to iiuman health. With the increase of multidrug resistance of clinically pathogenic bacteria, common antibiotic therapies have been less effective. Fatty acid synthesis type II (FASH) system enzymes are essential for bacterial membrane lipid biosynthesis and represent increasingly promising targets for the discovery of antibacterial agents with new mechanisms of action. This review highlights recent advances in inhibitors of bacterial FASH as potential antibacterial agents, paying special attention to the activities, mechanisms, and structure-activity relationships of those inhibitors that mainly target β-ketoacyl-ACP synthase, β-ketoacyl-ACP reductase, β-hydroxyacyl-ACP dehydratase, and enoyl-ACP reductase. Although inhibitors with low nanomolar and selective activity against various bacterial FASH have entered clinical trials, further research is needed to expand upon both available and yet unknown scaffolds to identify new FASH inhibitors that may have antibacterial potential, particularly against resistant bacterial strains.