Abstract
A series of novel artemisinin derivatives were synthesized from artemisinin and different anilines. All compounds were obtained as β-isomers. The target compounds were evaluated for inhibition activity against Plasmodium falciparum falcipain-2 in vitro, and most of them exhibited potent inhibition in the low micromolar range and proved to be new types of falcipain-2 inhibitors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aniline Compounds / chemistry
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Antimalarials / chemistry*
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Antimalarials / metabolism
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Antimalarials / pharmacology*
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Artemisinins / chemistry*
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Artemisinins / metabolism
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Artemisinins / pharmacology*
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Catalytic Domain / drug effects
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Cysteine Endopeptidases / chemistry
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Cysteine Endopeptidases / genetics
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Cysteine Endopeptidases / metabolism
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Cysteine Proteinase Inhibitors / chemistry*
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Cysteine Proteinase Inhibitors / metabolism
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Cysteine Proteinase Inhibitors / pharmacology*
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Drug Design
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Magnetic Resonance Spectroscopy
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Molecular Docking Simulation
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Osmolar Concentration
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Plasmodium falciparum / enzymology
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Protein Binding
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Protein Structure, Secondary / drug effects
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Protozoan Proteins / antagonists & inhibitors*
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Protozoan Proteins / chemistry
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Protozoan Proteins / genetics
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Protozoan Proteins / metabolism
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / chemistry
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Recombinant Proteins / metabolism
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Stereoisomerism
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Structure-Activity Relationship
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Thiosemicarbazones / chemistry
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Thiosemicarbazones / metabolism
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Thiosemicarbazones / pharmacology
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Transition Temperature
Substances
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Aniline Compounds
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Antimalarials
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Artemisinins
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Cysteine Proteinase Inhibitors
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Protozoan Proteins
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Recombinant Proteins
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Thiosemicarbazones
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artemisinin
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Cysteine Endopeptidases
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falcipain 2