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Merck
CN
  • Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr).

Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr).

Journal of medicinal chemistry (2011-08-27)
Christoph T Behrendt, Andrea Kunfermann, Victoria Illarionova, An Matheeussen, Miriam K Pein, Tobias Gräwert, Johannes Kaiser, Adelbert Bacher, Wolfgang Eisenreich, Boris Illarionov, Markus Fischer, Louis Maes, Michael Groll, Thomas Kurz
PMID21866890
摘要

Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.