Towards the development of novel antibiotics: synthesis and evaluation of a mechanism-based inhibitor of Kdo8P synthase Original Research Article

The design and two synthetic pathways to aminophosphonate which mimics the ionic and steric properties of putative oxocarbenium intermediate in the Kdo8P synthase-catalyzed reaction are reported. It was found that is a slow-binding, most potent inhibitor of the enzyme yet tested, with a Ki value of 0.4 μM.