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

Department of Chemistry and Institute of Catalysis Science and Technology, Technion-Israel Institute of Technology, Haifa.

Bioorganic & medicinal chemistry 1999 Dec

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The design and two synthetic pathways to aminophosphonate 4 which mimics the ionic and steric properties of putative oxocarbenium intermediate 3 in the Kdo8P synthase-catalyzed reaction are reported. It was found that 4 is a slow-binding, most potent inhibitor of the enzyme yet tested, with a Ki value of 0.4 microM.

Citation

S Du, H Faiger, V Belakhov, T Baasov. Towards the development of novel antibiotics: synthesis and evaluation of a mechanism-based inhibitor of Kdo8P synthase. Bioorganic & medicinal chemistry. 1999 Dec;7(12):2671-82