Abstract
VNI is a potent inhibitor of CYP51 and was recently shown to achieve a parasitological cure of mice infected with T. cruzi in both acute and chronic stages of infection. T. cruzi is the causative parasite of Chagas disease, a neglected tropical disease. The first enantioselective chemical synthesis of VNI (at a materials cost of less than $0.10/mg) is described. Furthermore, the key enantioselective step is performed at the 10 g scale.
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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Chagas Disease / drug therapy*
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Chagas Disease / parasitology
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Cytochrome P-450 Enzyme Inhibitors*
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Cytochrome P-450 Enzyme System
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / therapeutic use*
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Mice
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Molecular Structure
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Neglected Diseases
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Oxadiazoles / chemical synthesis*
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Oxadiazoles / chemistry
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Oxadiazoles / therapeutic use*
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Triazoles / chemistry
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Triazoles / therapeutic use
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Tropical Medicine
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Trypanosoma cruzi / drug effects*
Substances
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CYP51 protein, Trypanosoma cruzi
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Cytochrome P-450 Enzyme Inhibitors
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Imidazoles
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Oxadiazoles
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Triazoles
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VNI compound
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posaconazole
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Cytochrome P-450 Enzyme System