Neglected tropical diseases affect over 1 billion people per year, causing effects that range from fever to heart and bowel failure. Some of the more well-known illnesses of this class include Malaria, Rabies, Leprosy, and African Sleeping Sickness. While these maladies are fairly simple in their nature, they are considered neglected because of the lack of research or drugs available to treat them. The main focus of our research, Chagas disease, falls under this category. Chagas disease manifests itself in two forms, the acute phase which causes fever and swelling of the spleen and liver, and the chronic phase which is thought to be the leading cause of heart disease in Latin America, in countries such as Argentina, Brazil, and Bolivia.<br/>Our research focuses on creating multi-modal drugs for the treatment of Chagas disease using short synthetic pathways and inexpensive starting materials.<br/>In working to produce a multi-modal drug for Chagas disease we have started with a relatively inexpensive compound, commonly known as squaric acid. While this compound has shown some anti-Chagistic properities of its own, one of its main features is its ability to be further functionalized after being converted to a squaramide, a known class of anti-parasitics that target Chagas disease. Our current work is focused on converting squaric acid to a squaramide via an intermediary dimethyl ester by substituting two di-amino “arms” that are capable of further modification. In the future, we hope to perfect this first step in order to facilely create a novel library of compounds with different functional groups that may prove to be potent against Chagas disease.

Synthesis of multi-modal drugs toward treatment of Chagas disease

255th National Meeting (2018)

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