Abstract
Malaria is a very serious infectious disease against which the currently available drugs are loosing effectiveness. The main problem is the emergence and the spreading of resistant parasite strains. New treatments are needed in order to regain control over the disease. Drug discovery efforts towards this goal are likely to be more successful, if they focus towards novel mechanisms of action. Such efforts will result in drugs that are functionally and structurally different from the existing drugs and therefore will overcome existing resistances. Here we focus on the aspartic protease plasmepsin II, which is a promising new drug target. We review the drug discovery efforts that were published in the literature on this enzyme, and we present the compounds synthesized at Actelion Pharmaceuticals Ltd.
Keywords: plasmodium falciparum, parasite aspartic protease, plasmepsin II, antimalarial agents, malaria
Current Medicinal Chemistry
Title: Inhibitors of the Plasmodium Falciparum Parasite Aspartic Protease Plasmepsin II As Potential Antimalarial Agents
Volume: 10 Issue: 11
Author(s): C. Boss, S. Richard-Bildstein, T. Weller, W. Fischli, S. Meyer and C. Binkert
Affiliation:
Keywords: plasmodium falciparum, parasite aspartic protease, plasmepsin II, antimalarial agents, malaria
Abstract: Malaria is a very serious infectious disease against which the currently available drugs are loosing effectiveness. The main problem is the emergence and the spreading of resistant parasite strains. New treatments are needed in order to regain control over the disease. Drug discovery efforts towards this goal are likely to be more successful, if they focus towards novel mechanisms of action. Such efforts will result in drugs that are functionally and structurally different from the existing drugs and therefore will overcome existing resistances. Here we focus on the aspartic protease plasmepsin II, which is a promising new drug target. We review the drug discovery efforts that were published in the literature on this enzyme, and we present the compounds synthesized at Actelion Pharmaceuticals Ltd.
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Cite this article as:
Boss C., Richard-Bildstein S., Weller T., Fischli W., Meyer S. and Binkert C., Inhibitors of the Plasmodium Falciparum Parasite Aspartic Protease Plasmepsin II As Potential Antimalarial Agents, Current Medicinal Chemistry 2003; 10 (11) . https://dx.doi.org/10.2174/0929867033457674
DOI https://dx.doi.org/10.2174/0929867033457674 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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