954104-96-2Relevant academic research and scientific papers
Synthesis of antimalarial compounds fosmidomycin and FR900098 through N- or P-alkylation reactions
Suresh, Surisetti,Shyamraj, Dharavath,Larhed, Mats
, p. 1183 - 1188 (2013/03/14)
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 a
Novel deoxyxylulosephosphate-reductoisomerase inhibitors: Fosmidomycin derivatives with spacious acyl residues
Ortmann, Regina,Wiesner, Jochen,Silber, Katrin,Klebe, Gerhard,Jomaa, Hassan,Schlitzer, Martin
, p. 483 - 490 (2008/12/21)
1-Deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr) represents an essential enzyme of the mevalonate-independent pathway of the isoprenoid biosynthesis. Using fosmidomycin as a specific inhibitor of Dxr, this enzyme was previously validated as target for the treatment of malaria and bacterial infections. The replacement of the formyl residue of fosmidomycin by spacious acyl residues yielded inhibitors active in the micromolar range. As predicted by flexible docking, evidence was obtained for the formation of a hydrogen bond between an appropriately placed carbonyl group in the acyl residue and the main-chain NH of Met214 located in the flexible catalytic loop of the enzyme.
