Journalartikel

Jahr der Veröffentlichung: 2003

Seiten: 2163-2166

Zeitschrift: Bioorganic & Medicinal Chemistry Letters

Bandnummer: 13

Heftnummer: 13

ISSN: 0960-894X

eISSN: 1464-3405

DOI Link: https://doi.org/10.1016/S0960-894X(03)00354-8

Verlag: Elsevier

Abstract: 
FR900098 represents an improved derivative of the new antimalarial drug fosmidomycin and acts through inhibition of the 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase, an essential enzyme of the mevalonate independent pathway of isoprenoid biosynthesis. Prodrugs with increased activity after oral administration were obtained by chemical modification of the phosphonate moiety to yield acyloxyalkyl esters. The most successful compound demonstrated 2-fold increased activity in mice infected with the rodent malaria parasite Plasmodium vinckei. (C) 2003 Elsevier Science Ltd. All rights reserved.

Harvard-Zitierstil: Ortmann, R., Wiesner, J., Reichenberg, A., Henschker, D., Beck, E., Jomaa, H., et al. (2003) Acyloxyalkyl ester Prodrugs of FR900098 with improved in vivo anti-malarial activity, Bioorganic & Medicinal Chemistry Letters, 13(13), pp. 2163-2166. https://doi.org/10.1016/S0960-894X(03)00354-8

APA-Zitierstil: Ortmann, R., Wiesner, J., Reichenberg, A., Henschker, D., Beck, E., Jomaa, H., & Schlitzer, M. (2003). Acyloxyalkyl ester Prodrugs of FR900098 with improved in vivo anti-malarial activity. Bioorganic & Medicinal Chemistry Letters. 13(13), 2163-2166. https://doi.org/10.1016/S0960-894X(03)00354-8