TY - JOUR
T1 - Synthesis and antiplasmodial activity of highly active reverse analogues of the antimalarial drug candidate fosmidomycin
AU - Behrendt, Christoph T.
AU - Kunfermann, Andrea
AU - Illarionova, Victoria
AU - Matheeussen, An
AU - Gräwert, Tobias
AU - Groll, Michael
AU - Rohdich, Felix
AU - Bacher, Adelbert
AU - Eisenreich, Wolfgang
AU - Fischer, Markus
AU - Maes, Louis
AU - Kurz, Thomas
PY - 2010/10/4
Y1 - 2010/10/4
N2 - Inhibition of enzymes involved in the nonmevalonate pathway of isoprenoid biosynthesis represents a promising strategy for the development of novel antimalarial agents. A small series of reverse hydroxamate-based fosmidomycin analogues was synthesized and evaluated for their inhibitory activity against the recombinant 1-deoxy-D-xylulose 5-phosphate reductoisomerases (DXRs) of Escherichia coli and Plasmodium falciparum, as well as for their in vitro antiplasmodial activity and cytotoxicity.
AB - Inhibition of enzymes involved in the nonmevalonate pathway of isoprenoid biosynthesis represents a promising strategy for the development of novel antimalarial agents. A small series of reverse hydroxamate-based fosmidomycin analogues was synthesized and evaluated for their inhibitory activity against the recombinant 1-deoxy-D-xylulose 5-phosphate reductoisomerases (DXRs) of Escherichia coli and Plasmodium falciparum, as well as for their in vitro antiplasmodial activity and cytotoxicity.
KW - Antiprotozoal agents
KW - DOXP reductoisomerase
KW - Fosmidomycin
KW - MEP pathway
KW - Reverse analogues
UR - http://www.scopus.com/inward/record.url?scp=77957653130&partnerID=8YFLogxK
U2 - 10.1002/cmdc.201000276
DO - 10.1002/cmdc.201000276
M3 - Article
C2 - 20718073
AN - SCOPUS:77957653130
SN - 1860-7179
VL - 5
SP - 1673
EP - 1676
JO - ChemMedChem
JF - ChemMedChem
IS - 10
ER -