Human African trypanosomiasis (HAT) is a parasitic disease that is endemic in 36 sub-Saharan African countries. It is 100% fatal if not treated. The early stage of the disease is characterized by flu-like symptoms. The latter stage of the disease is characterized by behavioral changes, confusion, and changes to the normal sleep cycle. This last symptom obviously led to the common name of the disease, African sleeping sickness. HAT is currently treated with several old compounds including the bis-amidine, pentamidine. However, none of these compounds has an ideal profile and most are characterized by serious side effects and poor pharmacokinetics. As part of our efforts to develop new compounds aimed at the treatment of parasitic infections, we are synthesizing heterocyclic and bicyclic analogs of pentamidine with the goal of improving activity and physicochemical properties. This poster will discuss progress towards the synthesis of those analogs and plans for future analogs.

Preparation of pentamidine analogs for the treatment of human African trypanosomiasis (HAT)

245th National Meeting (2013)

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