Results 121 to 130 of about 1,235 (162)

Acyloxymethyl and alkoxycarbonyloxymethyl prodrugs of a fosmidomycin surrogate as antimalarial and antibacterial agents

open access: yesEuropean Journal of Medicinal Chemistry, 2023
Fosmidomycin is a natural antibiotic with potent IspC (DXR, 1-deoxy-d-xylulose-5-phosphate reductoisomerase) inhibitory activity. This enzyme catalyzes the first committed step of the non-mevalonate isoprenoid biosynthesis pathway, which is essential in most bacteria, including A. baumanii and M.
Serge Van Calenbergh   +2 more
exaly   +5 more sources
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Arylmethyl substituted derivatives of Fosmidomycin: Synthesis and antimalarial activity

European Journal of Medicinal Chemistry, 2006
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Rolf D Walter
exaly   +3 more sources

Fosmidomycin as an Antimalarial Drug: A Meta-Analysis of Clinical Trials

Future Microbiology, 2015
With first indications of resistance against artemisinin compounds, the development of novel alternative antimalarials remains an urgent need. One candidate is fosmidomycin (Fos), a phosphonic acid derivative. This PRISMA guideline-adhering and PROSPERO-registered systematic review and meta-analysis provides an overview of the state-of-the-art of the ...
Benjamin Mordmüller   +2 more
exaly   +4 more sources

Fosmidomycin for the treatment of malaria

Parasitology Research, 2003
In malaria parasites, isoprenoids are synthesised by the mevalonate independent 1-deoxy- D-xylulose 5-phosphate (DOXP) pathway. Fosmidomycin, a natural antibiotic originally developed for the treatment of bacterial infections, represents an inhibitor of DOXP reductoisomerase, an essential enzyme of this pathway.
Jochen, Wiesner   +2 more
openaire   +2 more sources

Prodrugs of Reverse Fosmidomycin Analogues

Journal of Medicinal Chemistry, 2015
Fosmidomycin inhibits IspC (Dxr, 1-deoxy-d-xylulose 5-phosphate reductoisomerase), a key enzyme in nonmevalonate isoprenoid biosynthesis that is essential in Plasmodium falciparum. The drug has been used successfully to treat malaria patients in clinical studies, thus validating IspC as an antimalarial target.
Brücher, Karin   +12 more
openaire   +4 more sources

Carboxylic Acid Analogues of Fosmidomycin

Zeitschrift für Naturforschung B, 2003
N-Alkylation of N-Boc-O-benzylhydroxylamine (1) with benzyl 4-bromobutyrate (2) in DMF gave N,O-bisprotected benzyl 4-hydroxyamino-butyrate (3), which was converted into 4-benzyloxyamino-butyric acid benzyl ester (4) with TFA in methylene chloride.
Thomas Kurz   +2 more
openaire   +1 more source

Hydroxyurea Analogues of Fosmidomycin

Zeitschrift für Naturforschung B, 2003
Abstract Benzyloxyureas (4) have been prepared by reactions of diethyl 3-benzyloxyamino-propyl-phosphonate (3) with isocyanates, potassium cyanate or 1,1’-carbonyldiimidazole / methylamine. Conversion of phosphonic esters 4 into phosphonic acids 6 by means of bromotrimethylsilane and catalytic hydrogenation of 4, 6 afforded the target ...
Thomas Kurz   +2 more
openaire   +1 more source

Comparison of the response ofEscherichia coli to fosfomycin and fosmidomycin

European Journal of Clinical Microbiology, 1987
The responses of Escherichia coli to fosfomycin and fosmidomycin were investigated by continuous turbidimetric monitoring of cultures exposed to the drugs and by microscopy. The activity of both agents was potentiated by glucose-6-phosphate, suggesting that they share the inducible hexose phosphate transport system in Escherichia coli, but several ...
Y, Kanimoto, D, Greenwood
openaire   +2 more sources

Fosmidomycin as an antimalarial agent

2023
This chapter focuses on the antimalarial agent fosmidomycin, which was isolated from the bacterium Streptomyces lavendulae in the late 1970s. It describes the structure of fosmidomycin and shows that it consists of a 3-carbon linker between the hydroxamic acid and phosphonate group. These are crucial to its antimalarial activity.
openaire   +1 more source

Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098

Archiv der Pharmazie, 2007
AbstractThe synthesis and in‐vitro antimalarial activity of conformationally restrained bis(pivaloyloxymethyl) ester analogues of the natural product fosmidomycin is presented. In contrast to α‐aryl‐substituted analogues, conformationally restrained aromatic analogues exhibit only moderate in‐vitro antimalarial activity against the chloroquine ...
Thomas, Kurz   +5 more
openaire   +2 more sources

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