Abstract
A rational approach was used to synthesize a new set of 15 1H-1,2,4-triazol-3-yl benzenesulfonamide derivatives with the aim of developing new antimalarial lead compounds. These derivatives were prepared in yields between 50% and 62%, and their structures were elucidated using IR, ¹H-, ¹³C-, ¹⁹F-NMR, MS and elemental analysis. A docking study based on sulfonamides previously used against malaria identified trifluoromethyl-substituted derivatives to be the best lead compounds for new antimalarial drug development.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Antimalarials / chemical synthesis*
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Antimalarials / chemistry
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Benzenesulfonamides
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Catalytic Domain
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Computer Simulation
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Conserved Sequence
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Cyclization
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Dihydropteroate Synthase / chemistry
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Drug Design
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Fluorine Compounds / chemical synthesis*
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Fluorine Compounds / chemistry
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Hydrogen Bonding
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Sequence Data
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Molecular Structure
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Plasmodium falciparum / enzymology
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Protein Binding
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Sulfadiazine / chemistry
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Sulfadoxine / chemistry
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Sulfalene / chemistry
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Thermodynamics
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Triazoles / chemical synthesis*
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Triazoles / chemistry
Substances
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Antimalarials
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Fluorine Compounds
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Sulfonamides
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Triazoles
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Sulfadiazine
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Sulfadoxine
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Dihydropteroate Synthase
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Sulfalene