Abstract
A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimalarials / chemistry*
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Antimalarials / pharmacology
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology
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Artemisinins / chemistry*
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Artemisinins / pharmacology
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Cysteine Endopeptidases / drug effects*
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Dipeptides / chemistry
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Dipeptides / pharmacology
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Drug Design
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Parasitic Sensitivity Tests
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Plasmodium falciparum / drug effects
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Structure-Activity Relationship
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Sulfones / chemistry*
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Sulfones / pharmacology
Substances
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Antimalarials
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Antiprotozoal Agents
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Artemisinins
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Dipeptides
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Sulfones
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divinyl sulfone
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Cysteine Endopeptidases
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falcipain 2