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Träfflista för sökning "WFRF:(Dharavath Shyamraj) "

Sökning: WFRF:(Dharavath Shyamraj)

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1.
  • Jansson, Anna, 1979-, et al. (författare)
  • DXR Inhibition by Potent Mono- and Disubstituted Fosmidomycin Analogues
  • 2013
  • Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 56:15, s. 6190-6199
  • Tidskriftsartikel (refereegranskat)abstract
    • The antimalarial compound fosmidomycin targets DXR, the enzyme that catalyzes the first committed step in the MEP pathway producing the universally essential isoprenoid precursors, isopentenyl diphosphate and dimethylallyl diphosphate. The MEP pathway is used by a number of pathogens, including Mycobacterium tuberculosis and apicomplexan parasites, and differs from the classical mevalonate pathway that is essential in humans. Using a structure-based approach, we designed a number of analogues of fosmidomycin, including a series that are substituted in both the Cα and the hydroxamate positions. The latter proved to be a stable framework for the design of inhibitors that extend from the cramped substrate-binding site and can, for the first time, bridge the substrate and cofactor binding sites. A number of these compounds are more potent than fosmidomycin in terms of killing Plasmodium falciparum in an in vitro assay; the best has an IC50 of 40 nM.
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2.
  • Suresh, Surisetti, et al. (författare)
  • Synthesis of antimalarial compounds fosmidomycin and FR900098 through N- or P-alkylation reactions
  • 2013
  • Ingår i: Tetrahedron. - : Elsevier BV. - 0040-4020 .- 1464-5416. ; 69:3, s. 1183-1188
  • Tidskriftsartikel (refereegranskat)abstract
    • Two straightforward and convenient routes for the synthesis of the antimalarial agents FR900098 and fosmidomycin are described. In the key steps N- or P-alkylation reactions are used. The best overall yields of FR900098 and fosmidomycin in 15 mmol scale are 83% and 68%, respectively. These routes utilize readily available materials and avoid harsh conditions.
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