Michael Waterman
Faculty Member
Last active: 2/12/2015

Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease.

Dobish MC, Villalta F, Waterman MR, Lepesheva GI, Johnston JN
Org Lett. 2012 14 (24): 6322-5

PMID: 23214987 · PMCID: PMC3528807 · DOI:10.1021/ol303092v

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.

MeSH Terms (12)

Animals Chagas Disease Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System Imidazoles Mice Molecular Structure Neglected Diseases Oxadiazoles Triazoles Tropical Medicine Trypanosoma cruzi

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