Synthesis and biological evaluation of thiazolidine-2-one 1, 1-dioxide as inhibitors of Escherichia coli β-ketoacyl-ACP-synthase III (FabH)

…, M Kreishman-Deitrick, G Florova, KA Reynolds

文献索引：Alhamadsheh, Mamoun M.; Waters, Norman C.; Huddler, Donald P.; Kreishman-Deitrick, Mara; Florova, Galina; Reynolds, Kevin A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 4 p. 879 - 883

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被引用次数: 26

摘要

A series of cyclic sulfones has been synthesized and their activity against β-ketoacyl-ACP- synthase III (FabH) has been investigated. The compounds are selectively active against Escherichia coli FabH (ecFabH), but not Mycobacterium tuberculosis FabH (mtFabH) or Plasmodium falciparum KASIII (PfKASIII). The activity against ecFabH ranges from 0.9 to> 100μM and follows a consistent general SAR trend. Many of the compounds were shown ...