Abstract
A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 with affinity in the submicromolar range and that shows interesting antiparasitic properties against the different life cycle stages of T. cruzi.
Keywords:
Chagas disease; bromodomain inhibitor; chemically engineered extracts; diversification; oxime.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiparasitic Agents / chemistry*
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Antiparasitic Agents / isolation & purification
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Antiparasitic Agents / pharmacology
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Cell Survival / drug effects
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Chagas Disease / drug therapy*
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Chlorocebus aethiops
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Escherichia coli / genetics
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Oils, Volatile / chemistry*
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Oximes / chemistry
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Oximes / pharmacology
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Plant Extracts / chemistry*
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Plant Extracts / isolation & purification
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Plant Oils / chemistry*
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Plant Oils / isolation & purification
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Protein Binding
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Protein Conformation
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Trypanosoma cruzi / drug effects*
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Vero Cells
Substances
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Antiparasitic Agents
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Oils, Volatile
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Oximes
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Plant Extracts
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Plant Oils