Results 21 to 30 of about 1,660 (188)

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   +5 more sources

Methyl-Jasmonate Functions as a Molecular Switch Promoting Cross-Talk between Pathways for the Biosynthesis of Isoprenoid Backbones Used to Modify Proteins in Plants [PDF]

Plants
In plants, the plastidial mevalonate (MVA)-independent pathway is required for the modification with geranylgeranyl groups of CaaL-motif proteins, which are substrates of protein geranylgeranyltransferase type-I (PGGT-I).
Quentin Chevalier, Alexandre Huchelmann, Pauline Debié, Pierre Mercier, Michael Hartmann, Catherine Vonthron-Sénécheau, Thomas J. Bach, Hubert Schaller, Andréa Hemmerlin   +8 more
doaj   +2 more sources

Beyond the MEP Pathway: A novel kinase required for prenol utilization by malaria parasites. [PDF]

PLoS Pathogens
A proposed treatment for malaria is a combination of fosmidomycin and clindamycin. Both compounds inhibit the methylerythritol 4-phosphate (MEP) pathway, the parasitic source of farnesyl and geranylgeranyl pyrophosphate (FPP and GGPP, respectively). Both
Marcell Crispim, Ignasi Bofill Verdaguer, Agustín Hernández, Thales Kronenberger, Àngel Fenollar, Lydia Fumiko Yamaguchi, María Pía Alberione, Miriam Ramirez, Sandra Souza de Oliveira, Alejandro Miguel Katzin, Luis Izquierdo   +10 more
doaj   +2 more sources

Synthesis and Antiplasmodial Activity of Novel Fosmidomycin Derivatives and Conjugates with Artemisinin and Aminochloroquinoline [PDF]

Molecules, 2020
Malaria, despite many efforts, remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by Plasmodium falciparum.
Despina Palla, Antonia I. Antoniou, Michel Baltas, Christophe Menendez, Philippe Grellier, Elisabeth Mouray, Constantinos M. Athanassopoulos   +6 more
doaj   +4 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, Gräwert, Tobias, Konzuch, Sarah, Held, Jana, Lienau, Claudia, Behrendt, Christoph, Illarionov, Boris, Maes, Louis, Bacher, Adelbert, Wittlin, Sergio, Mordmüller, Benjamin, Fischer, Markus, Kurz, Thomas   +12 more
openaire   +5 more sources

Effect of fosmidomycin on metabolic and transcript profiles of the methylerythritol phosphate pathway in Plasmodium falciparum

Memorias do Instituto Oswaldo Cruz, 2007
In Plasmodium falciparum, the formation of isopentenyl diphosphate and dimethylallyl diphosphate, central intermediates in the biosynthesis of isoprenoids, occurs via the methylerythritol phosphate (MEP) pathway.
María B Cassera, Emilio F Merino, Valnice J Peres, Emilia A Kimura, Gerhard Wunderlich, Alejandro M Katzin   +5 more
doaj   +3 more sources

Expanding the Chemical Space of Reverse Fosmidomycin Analogs. [PDF]

ACS Med Chem Lett
Multidrug-resistant pathogens pose a major threat to human health, necessitating the identification of new drug targets and lead compounds that are not susceptible to cross-resistance. This study demonstrates that novel reverse thia analogs of the phosphonohydroxamic acid antibiotic fosmidomycin inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase ...
Knak T, Takada S, Illarionov B, Krisilia V, Pessanha de Carvalho L, Lungerich B, Sakamoto Y, Höfmann S, Bacher A, Kalscheuer R, Held J, Fischer M, Tanaka N, Kurz T.   +13 more
europepmc   +3 more sources

A Chemical Probe for Increasing Leaf Tocopherol Levels by Coordinated Modulation of Biosynthesis, Competition and Storage. [PDF]

Plant Biotechnol J
ABSTRACT Plant biofortification with phytonutrients typically relies on metabolic engineering strategies known as ‘push’ (enhancing biosynthetic flux), ‘block’ (inhibiting competing pathways) and ‘pull’ (promoting metabolite storage). Here, we describe a novel synthetic compound, X57, that simultaneously targets biosynthesis, competition and storage to
Perez-Colao P, Glauser G, Cruces J, Lozano-Juste J, Rodriguez-Concepcion M.   +4 more
europepmc   +2 more sources

Preparation of gem-difluorinated retrohydroxamic-fosmidomycin [PDF]

ARKIVOC, 2015
From several decades, some organophosphorus compounds specifically designed to alter biological systems were introduced on market as agr ochemicals (ie glyphosate and glufosinate as herbicides). Nevertheless, it becomes necessary to find new compounds in order to counter plant resistances already observed with glyphosate. Fosmi domicyn and its N-acetyl
Jean-Noël Volle, Camille Midriera, Vincent Blanchard, Ralf Braun, Klaus Haaf, Lothar Willms, Jean-Luc Pirata, David Virieux   +7 more
doaj   +2 more sources

Fosmidomycin, a Novel Chemotherapeutic Agent for Malaria [PDF]

Antimicrobial Agents and Chemotherapy, 2003
ABSTRACT In previous studies, fosmidomycin has been shown to possess activity against Plasmodium falciparum in vitro and in the mouse model. It has a novel mode of action through inhibition of 1-deoxy- d -xylulose 5-phosphate reductoisomerase, an enzyme of the nonmevalonate pathway ...
Bertrand, Lell, Ronnatrai, Ruangweerayut, Jochen, Wiesner, Michel Anoumou, Missinou, Andreas, Schindler, Thomas, Baranek, Martin, Hintz, David, Hutchinson, Hassan, Jomaa, Peter Gottfried, Kremsner   +9 more
openaire   +2 more sources