Carbohydroxamido-oxazolidines: antibacterial agents that target lipid A biosynthesis |
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| Authors: | Chen M H Steiner M G de Laszlo S E Patchett A A Anderson M S Hyland S A Onishi H R Silver L L Raetz C R |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA. |
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| Abstract: | A series of carbohydroxamido-oxazolidine inhibitors of UDP-3-O-R-3-hydroxymyristoyl]-GlcNAc deacetylase, the enzyme responsible for the second step in lipid A biosynthesis, was identified. The most potent analog L-161,240 showed an IC50 = 30 nM in the DEACET assay and displayed an MIC of 1-3 microg/mL against wild-type E. coli. |
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