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Progress in Chemistry 2009, Vol. 21 Issue (09): 1930-1938 Previous Articles   Next Articles

• Review •

Advances in the Research of β-Ketoacyl-ACP Synthase Ⅲ(FabH) Inhibitors

Liu Xiaobo|Li Yuyan|You Qidong*   

  1. (Department of Medicinal Chemistry, China Pharmacerutical University, Nanjing 210009, China)
  • Received: Revised: Online: Published:
  • Contact: You Qidong E-mail:youqidong@gmail.com
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Fatty acid biosynthesis is essential for bacterial survival. In recent years, components of this biosynthetic pathway have aroused wide concern. One fatty acid synthase, FabH (β-Ketoacyl-acyl carrier protein synthase Ⅲ), is a particularly attractive target which catalyzes the initial step of fatty acid biosynthesis. The pivotal role of this essential enzyme combined with its ubiquitous occurrence in bacteria and no homologous protein in human being has made it an attractive new target for the development of new antibacterial agents. Small molecules that inhibit FabH enzymatic activity have the potential to be candidates within a novel class of selective, nontoxic, broad-spectrum antibacterials. In this paper, fatty acid biosynthesis, recent advances in the research of FabH as well as related inhibitors are reviewed.

Contents
1 Introduction
2 Structure of FabH
2.1 FabH
2.2 mtFabH
3 FabH Inhibitors
3.1 Thiolactomycin(TLM)
3.2 Platensimycin and platencin
3.3 Indole compounds
3.4 Benzoylaminobenzoic acid derivatives
3.5 Alkylsulfonyl substituents
3.6 1,2-dithiole-3-ones
3.7 Thiazolidine-2-One 1,1-dioxide
3.8 Alkyl-CoA disulfides
4 Conclusion and perspective

Key words: fatty acid synthase(FAS), FabH, FabH inhibitors, mycobacterium tuberculosis

CLC Number: 

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