Results 131 to 140 of about 1,209 (154)
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Comparison of the response ofEscherichia coli to fosfomycin and fosmidomycin
European Journal of Clinical Microbiology, 1987The 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
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Fosmidomycin as an antimalarial agent
2023This 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.
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Determination of fosmidomycin in human serum and urine by capillary electrophoresis
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences, 2004A capillary electrophoresis method with direct UV detection was developed for the determination of fosmidomycin, a promising new anti-malarial drug, in human serum and urine. Optimization of the separation parameters resulted in a buffer system adjusted to pH 10.8 containing a cationic reagent and an organic modifier.
Jochen Wiesner +2 more
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Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098
Archiv der Pharmazie, 2007AbstractThe 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
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Fosmidomycin as an Antimalarial Agent
2012The isoprenoid biosynthesis of Plasmodium falciparum, the causative agent of malignant tertiana malaria, solely depends on the mevalonate-independent 2-C-methyl-d-erythritol 4-phosphate (MEP) pathway [also known as the 1-deoxy-d-xylulose 5-phosphate (DXP) pathway]. The enzymes of the MEP pathway of P.
Jochen Wiesner +10 more
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Profiling of defense responses in Escherichia coli treated with fosmidomycin
Biochimie, 2014The mevalonate-independent isoprenoid biosynthesis pathway has been recognized as a promising target for designing new antibiotics. But pathogens treated with compounds such as fosmidomycin, a slow binding inhibitor of 1-deoxy-D-xylulose 5-phosphate reducto-isomerase, the second enzyme in this pathway, develop rapid drug resistance. In Escherichia coli,
Hemmerlin, A. +4 more
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Double prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents
Bioorganic & Medicinal Chemistry Letters, 2019A series of eleven double prodrug derivatives of a fosmidomycin surrogate were synthesized and investigated for their ability to inhibit in vitro growth of P. falciparum and M. tuberculosis. A pivaloyloxymethyl (POM) phosphonate prodrug modification was combined with various prodrug derivatisations of the hydroxamate moiety.
Charlotte Courtens +6 more
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Activity of fosmidomycin in an in vitro model of the treatment of bacterial cystitis
Infection, 1987The response to fosmidomycin of four strains of Escherichia coli was studied in an in vitro model of the treatment of bacterial cystitis. Three susceptible strains of E. coli responded well to relatively low concentrations of fosmidomycin: doses achieving peak concentrations of 50 or 250 mg/l suppressed bacterial growth for 13 h or more; however, when ...
Y, Kanimoto, D, Greenwood
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Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues
Bioorganic & Medicinal Chemistry Letters, 2015The continuous development of drug resistance by Plasmodium falciparum, the agent responsible for the most severe forms of malaria, creates the need for the development of novel drugs to fight this disease. Fosmidomycin is an effective antimalarial and potent antibiotic, known to act by inhibiting the enzyme 1-deoxy-d-xylulose-5-phosphate ...
Ana Maria Faísca Phillips +3 more
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γ‐Substituted Bis(pivaloyloxymethyl)ester Analogues of Fosmidomycin and FR900098
Archiv Der Pharmazie, 2007AbstractThe synthesis and in‐vitro antimalarial activity of γ‐substituted bis(pivaloyloxymethyl)ester analogues of the drug candidate fosmidomycin have been investigated. In contrast to the high antimalarial activity of α‐aryl substituted fosmidomycin analogues like α‐phenylfosmidomycin, γ‐substituted derivatives display only weak to moderate activity ...
Miriam Pein-Hackelbusch
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