Journal
ORGANIC LETTERS
Volume 14, Issue 24, Pages 6322-6325Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol303092v
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Funding
- National Institutes of Health (NIH) [GM084333]
- Vanderbilt Institute of Chemical Biology (VICB)
- VICB
- [GM067871]
- [AI080580]
- [U54 MD007593]
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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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