Journal
CHEMMEDCHEM
Volume 8, Issue 10, Pages 1589-1608Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201300209
Keywords
acyl carrier protein; antibacterial agents; inhibitors; fatty acid synthesis typeII; medicinal chemistry
Categories
Funding
- National Natural Science Foundation of China [20872081, 21072114]
- Natural Science Foundation of Shandong [ZR2010HM092]
- Chinese State Education Ministry through the Scientific Research Foundation for Returned Overseas Chinese Scholars
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Bacterial infections are a constant and serious threat to human health. With the increase of multidrug resistance of clinically pathogenic bacteria, common antibiotic therapies have been less effective. Fatty acid synthesis typeII (FASII) 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 FASII as potential antibacterial agents, paying special attention to the activities, mechanisms, and structure-activity relationships of those inhibitors that mainly target -ketoacyl-ACP synthase, -ketoacyl-ACP reductase, -hydroxyacyl-ACP dehydratase, and enoyl-ACP reductase. Although inhibitors with low nanomolar and selective activity against various bacterial FASII have entered clinical trials, further research is needed to expand upon both available and yet unknown scaffolds to identify new FASII inhibitors that may have antibacterial potential, particularly against resistant bacterial strains.
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