期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 11, 页码 5377-5390出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00236
关键词
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资金
- National Institutes of Health [GM102864, AI044639]
beta-Ketoacyl-ACP synthases (KAS) are key enzymes involved in the type II bacterial fatty acid biosynthesis (FASII) pathway and are putative targets for antibacterial discovery. Several natural product KAS inhibitors have previously been reported, including thiolactomycin (TLM), which is produced by Nocardia spp. Here we describe the synthesis and characterization of optically pure 5R-thiolacto-mycin (TLM) analogues that show improved whole cell activity against bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA) and priority pathogens such as Francisella tularensis and Burkholderia pseudomallei. In addition, we identify TLM analogues with in vivo efficacy against MRSA and Klebsiella pneumoniae in animal models of infection.
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