TY - JOUR
T1 - Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)
AU - Behrendt, Christoph T.
AU - Kunfermann, Andrea
AU - Illarionova, Victoria
AU - Matheeussen, An
AU - Pein, Miriam K.
AU - Gräwert, Tobias
AU - Kaiser, Johannes
AU - Bacher, Adelbert
AU - Eisenreich, Wolfgang
AU - Illarionov, Boris
AU - Fischer, Markus
AU - Maes, Louis
AU - Groll, Michael
AU - Kurz, Thomas
PY - 2011/10/13
Y1 - 2011/10/13
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=80053909858&partnerID=8YFLogxK
U2 - 10.1021/jm200694q
DO - 10.1021/jm200694q
M3 - Article
C2 - 21866890
AN - SCOPUS:80053909858
SN - 0022-2623
VL - 54
SP - 6796
EP - 6802
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 19
ER -