Synthesis of Compounds to Treat Human African Trypanosomiasis

Advisor Information

James Hagen

Location

Dr. C.C. and Mabel L. Criss Library

Presentation Type

Poster

Start Date

4-3-2016 9:00 AM

End Date

4-3-2016 10:30 AM

Abstract

Human African trypanosomiasis (HAT), also known as “sleeping sickness”, is caused by eukaryotic protozoan parasites. These protists circulate in the bloodstreams of their hosts after being transmitted by the bite of a tsetse fly. In the first stage of the HAT infection, the trypanosomes multiply in the blood and lymph causing headaches, fever, itching, joint pains, and swelling of the lymph nodes. In the second stage, the parasites invade the central nervous system. The result is confusion, behavioral changes, sensory disturbances, troubles with the sleep cycle, and eventually death. HAT poses a grave health concern in sub-Saharan Africa. Sixty million individuals are at risk of infection; with a morbidity rate estimated to exceed 50,000 cases per year. There are currently five drugs that are used to treat HAT. All current drugs have impractical administration protocols, are becoming ineffective due to drug-resistance, or are highly toxic. For example, melarsoprol causes fatal encephalopathy in ten percent of patients. Inexpensive, nontoxic, easily administered, and effective therapies are in high demand. Dr. James Hagen’s lab has synthesized a lead compound that possesses biological activity shown to be beneficial in the treatment of HAT, as well as low toxicity. The aim of this research was to synthesize analogues of the lead compound. The analogues were sent to the Swiss Tropical and Public Health Institute for biological and cytotoxicity testing against a protozoan panel. The poster will present information on both the schemes used to synthesize these compounds as well as their biological activity.

Additional Information (Optional)

Winner of Best Undergraduate Poster Presentation

This document is currently not available here.

COinS
 
Mar 4th, 9:00 AM Mar 4th, 10:30 AM

Synthesis of Compounds to Treat Human African Trypanosomiasis

Dr. C.C. and Mabel L. Criss Library

Human African trypanosomiasis (HAT), also known as “sleeping sickness”, is caused by eukaryotic protozoan parasites. These protists circulate in the bloodstreams of their hosts after being transmitted by the bite of a tsetse fly. In the first stage of the HAT infection, the trypanosomes multiply in the blood and lymph causing headaches, fever, itching, joint pains, and swelling of the lymph nodes. In the second stage, the parasites invade the central nervous system. The result is confusion, behavioral changes, sensory disturbances, troubles with the sleep cycle, and eventually death. HAT poses a grave health concern in sub-Saharan Africa. Sixty million individuals are at risk of infection; with a morbidity rate estimated to exceed 50,000 cases per year. There are currently five drugs that are used to treat HAT. All current drugs have impractical administration protocols, are becoming ineffective due to drug-resistance, or are highly toxic. For example, melarsoprol causes fatal encephalopathy in ten percent of patients. Inexpensive, nontoxic, easily administered, and effective therapies are in high demand. Dr. James Hagen’s lab has synthesized a lead compound that possesses biological activity shown to be beneficial in the treatment of HAT, as well as low toxicity. The aim of this research was to synthesize analogues of the lead compound. The analogues were sent to the Swiss Tropical and Public Health Institute for biological and cytotoxicity testing against a protozoan panel. The poster will present information on both the schemes used to synthesize these compounds as well as their biological activity.