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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, 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.
Stéphane, Bronner +6 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,
Andréa, Hemmerlin +4 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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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 +2 more
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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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Novel reverse thia-analogs of fosmidomycin: Synthesis and antiplasmodial activity
European Journal of Medicinal Chemistry, 2019Thia analogs of fosmidomycin are potent inhibitors of the non-mevalonate isoprenoid biosynthesis enzyme 1-deoxy-d-xylulose 5-phosphate reductoisomerase (IspC, Dxr) of Plasmodium falciparum. Several new thioethers displayed antiplasmodial in vitro activity in the low nanomolar range, without apparent cytotoxic effects in HeLa cells.
Claudia, Lienau +17 more
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Pharmacokinetics and metabolism of fosmidomycin, a new phosphonic acid, in rats and dogs
European Journal of Drug Metabolism and Pharmacokinetics, 1982The absorption, distribution, metabolism, and excretion of 3-(N-formylhydroxylamino) propylphosphonic acid monosodium salt (fosmidomycin), a new antibiotic, were investigated in rats and dogs after i.v. and oral dosing. After i.v. administration of 10 mg/kg of body weight, [14C]-fosmidomycin was excreted mainly in the urine (about 90% of dose within 72
T, Tsuchiya +5 more
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Non-Antifolate Antibiotics: Clindamycin, Doxycycline, Azithromycin and Fosmidomycin
2011A range of antibiotics, in addition to those that target folate metabolism, have demonstrated antimalarial activity. They include those belonging to the lincosamides, tetracyclines and macrolides classes and fosmidomycin, a derivative of phosphonic acid.
Sanjeev Krishna, Henry M. Staines
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Assessment of in vitro antimalarial interactions between dihydroartemisinin and fosmidomycin.
The Southeast Asian journal of tropical medicine and public health, 2008Malaria remains one of the leading causes of morbidity and mortality in the tropics with an annual estimate of 500 million clinical cases and 2 million deaths. The treatment and control of malaria is becoming increasingly difficult due to Plasmodium falciparum resistance to commonly used antimalarials.
Wanna, Chaijaroenkul +3 more
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