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

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

  • Org Lett. 2012 Dec 21;14(24):6322-5. doi: 10.1021/ol303092v.
Mark C Dobish 1,  Fernando Villalta,  Michael R Waterman,  Galina I Lepesheva,  Jeffrey N Johnston
Affiliations

Affiliation

  • 1 Department of Chemistry & Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37235, United States.
PMID: 23214987 DOI: 10.1021/ol303092v
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.

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