Results 131 to 140 of about 1,235 (162)

Fosmidomycin as an Antimalarial Agent

2012
The 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, Armin Reichenberg, Martin Hintz, Regina Ortmann, Martin Schlitzer, Serge Van Calenbergh, Steffen Borrmann, Bertrand Lell, Peter G. Kremsner, David Hutchinson, Hassan Jomaa   +10 more
openaire   +1 more source

Determination of fosmidomycin in human serum and urine by capillary electrophoresis

Journal of Chromatography B, 2004
A 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, Corinne, Renault, Martin, Hintz, Jochen, Wiesner, Hassan, Jomaa, Henri, Monteil, François, Jehl   +6 more
openaire   +2 more sources

Activity of fosmidomycin in an in vitro model of the treatment of bacterial cystitis

Infection, 1987
The 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
openaire   +2 more sources

Double prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents

Bioorganic & Medicinal Chemistry Letters, 2019
A 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, Martijn Risseeuw, Guy Caljon, Louis Maes, Paul Cos, Anandi Martin, Serge Van Calenbergh   +6 more
openaire   +3 more sources

Profiling of defense responses in Escherichia coli treated with fosmidomycin

Biochimie, 2014
The 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., Tritsch, D., Hammann, P., Rohmer, M., Bach, T.J.   +4 more
openaire   +3 more sources

Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues

Bioorganic & Medicinal Chemistry Letters, 2015
The 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, Fátima Nogueira, Fernanda Murtinheira, Maria Teresa Barros   +3 more
openaire   +2 more sources

γ-Substituted Bis(pivaloyloxymethyl)ester Analogues of Fosmidomycin and FR900098

Archiv Der Pharmazie, 2007
AbstractThe 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 K Pein, Rolf D Walter
exaly   +3 more sources

Novel reverse thia-analogs of fosmidomycin: Synthesis and antiplasmodial activity

European Journal of Medicinal Chemistry, 2019
Thia 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, Tobias, Gräwert, Leandro A, Alves Avelar, Boris, Illarionov, Jana, Held, Tanja C, Knaab, Beate, Lungerich, Lasse, van Geelen, Dieter, Meier, Stefanie, Geissler, Holger, Cynis, Ulrich, Riederer, Mirko, Buchholz, Rainer, Kalscheuer, Adelbert, Bacher, Benjamin, Mordmüller, Markus, Fischer, Thomas, Kurz   +17 more
openaire   +2 more sources

Pharmacokinetics and metabolism of fosmidomycin, a new phosphonic acid, in rats and dogs

European Journal of Drug Metabolism and Pharmacokinetics, 1982
The 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, K, Ishibashi, M, Terakawa, M, Nishiyama, N, Itoh, H, Noguchi   +5 more
exaly   +3 more sources

Assessment of in vitro antimalarial interactions between dihydroartemisinin and fosmidomycin.

The Southeast Asian journal of tropical medicine and public health, 2008
Malaria 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, Pattaya, Pruktal, Poonuch, Muhamad, Kesara, Na-Bangchang   +3 more
openaire   +1 more source