1. Academic Validation
  2. Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)

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

  • J Med Chem. 2011 Oct 13;54(19):6796-802. doi: 10.1021/jm200694q.
Christoph T Behrendt 1 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
Affiliations

Affiliation

  • 1 Institut für Pharmazeutische und Medizinische Chemie, Heinrich Heine Universität, Universitätsstrasse 1, 40225 Düsseldorf, Germany.
Abstract

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.

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