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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Inhibitors of the Plasmodium Falciparum Parasite Aspartic Protease Plasmepsin II As Potential Antimalarial Agents

Author(s): C. Boss, S. Richard-Bildstein, T. Weller, W. Fischli, S. Meyer and C. Binkert

Volume 10 , Issue 11 , 2003

Page: [883 - 907] Pages: 25

DOI: 10.2174/0929867033457674

Price: $65


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

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