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Fatty acid biosynthesis is essential for bacterial survival. In recent years, components of this biosynthetic pathway have aroused wide concern. β-Ketoacyl-acyl carrier protein synthase III (FabH) is a particularly attractive target which catalyzes the initial step of fatty acid biosynthesis. In this review, fatty acid biosynthesis, recent advances in the research of FabH as well as related inhibitors are reviewed. Finally, we also discuss the prospect and developmental trend of FabH inhibitors as anti-bacterial agents.