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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
α-Substituted β-oxa isosteres of fosmidomycin: Synthesis and biological evaluation
Journal of Medicinal Chemistry, Volume 55, No. 14, Year 2012
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Description
Specific inhibition of enzymes of the non-mevalonate pathway is a promising strategy for the development of novel antiplasmodial drugs. α-Aryl-substituted β-oxa isosteres of fosmidomycin with a reverse orientation of the hydroxamic acid group were synthesized and evaluated for their inhibitory activity against recombinant 1-deoxy-d-xylulose 5-phosphate reductoisomerase (IspC) of Plasmodium falciparum and for their in vitro antiplasmodial activity against chloroquine-sensitive and resistant strains of P. falciparum. The most active derivative inhibits IspC protein of P. falciparum (PfIspC) with an IC 50 value of 12 nM and shows potent in vitro antiplasmodial activity. In addition, lipophilic ester prodrugs demonstrated improved P. falciparum growth inhibition in vitro. © 2012 American Chemical Society.
Authors & Co-Authors
Brücher, Karin
Germany, Dusseldorf
Heinrich-heine-universität Düsseldorf
Illarionov, Boris A.
Germany, Hamburg
Universität Hamburg
Held, Jana
Germany, Tubingen
Eberhard Karls Universität Tübingen
Tschan, Serena C.
Germany, Tubingen
Eberhard Karls Universität Tübingen
Kunfermann, Andrea
Germany, Munich
Technische Universität München
Pein-Hackelbusch, Miriam
Germany, Dusseldorf
Heinrich-heine-universität Düsseldorf
Bacher, Adelbert
Germany, Munich
Technische Universität München
Gräwert, Tobias W.
Germany, Hamburg
Universität Hamburg
Maes, Louis J.R.M.
Belgium, Antwerpen
Universiteit Antwerpen
Mordmüller, Benjamin G.
Germany, Tubingen
Eberhard Karls Universität Tübingen
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Fischer, Markus
Germany, Hamburg
Universität Hamburg
Kurz, Thomas
Germany, Dusseldorf
Heinrich-heine-universität Düsseldorf
Statistics
Citations: 29
Authors: 12
Affiliations: 6
Identifiers
Doi:
10.1021/jm300652f
ISSN:
00222623
e-ISSN:
15204804