Molecules · 2014 · 18 citations · 33 references
Target EnzymeBioorganic ChemistrySynthetic Fosmidomycin AnaloguesAntimicrobial ChemotherapyChemical Biology1-Deoxy-d-xylulose 5-Phosphate ReductoisomerasePharmaceutical ChemistryDrug ResistanceMedicinal ChemistryM. Tuberculosis DxrPlasmodium Falciparum GrowthAntimicrobial ResistanceBiochemistryAntibacterial AgentAntimicrobial CompoundDrug DevelopmentPharmacologyNatural SciencesHydroxamate FunctionalityMedicineDrug Discovery
Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. This study further underlines the importance of the hydroxamate functionality and illustrates that identifying effective alternative bidentate ligands for this target enzyme is challenging.
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The global distribution of clinical episodes of Plasmodium falciparum malaria
Robert W. Snow, Carlos A. Guerra, Abdisalan M. Noor et al. · Nature · 2005 · 2.7K citations · Full text
Inhibitors of the Nonmevalonate Pathway of Isoprenoid Biosynthesis as Antimalarial Drugs
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