Reverse Fosmidomycin Derivatives against the Antimalarial Drug Target IspC (Dxr)
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- 作者：Christoph T. Behrendt ; Andrea Kunfermann ; Victoria Illarionova ; An Matheeussen ; Miriam K. Pein ; Tobias Gr盲wert ; Johannes Kaiser ; Adelbert Bacher ; Wolfgang Eisenreich ; Boris Illarionov ; Markus Fischer ; Louis Maes ; Michael Groll ; Thomas Kurz
- 刊名：Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：October 13, 2011
- 年：2011
- 卷：54
- 期：19
- 页码：6796-6802
- 全文大小：979K
- 年卷期：v.54,no.19(October 13, 2011)
- ISSN：1520-4804
文摘
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.