Carbohydroxamido-oxazolidines: antibacterial agents that target lipid A biosynthesis
- Bioorg Med Chem Lett. 1999 Feb 8;9(3):313-8. doi: 10.1016/s0960-894x(98)00749-5.
- 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
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.