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
Authors: Dobish MC, Villalta F, Waterman MR, Lepesheva GI, Johnston JN
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.
PMID: 23214987 [PubMed - indexed for MEDLINE]