Presentation Type
Panel Discussion
Start Date
20-3-2021 11:30 AM
Abstract
Chagas disease is caused by the parasite Trypanosoma Cruzi and plagues nearly 10 million people in the Americas. While this disease is not widely researched, it is an epidemic that is ravaging the desolate nations of Central and South America. Unfortunately for patients diagnosed with this disease, the two cures available are expensive, harmful to the patient, and are becoming alarmingly more ineffective due to drug resistances. Because of this, it is crucial that new chemical entities can be identified, created, and tested in search of a novel cure. In this research, viable drug targets from the squaramides class of compound are created from diethyl squarate in two high yielding and quick synthetic steps. Two classes of compounds have been synthesized: 1) those with two squarate cores and 2) those with one squarate core but using large amino side chains. These compounds are designed to interact with the parasite that causes Chagas disease, by puncturing holes within the membrane, killing the T. cruzi, thus ultimately curing the infected individual of this parasitic infection. This experimentation has found that the double squarate compounds are significantly lower in yield than those with different bulky side arms. The eighteen compounds with one squarate core and large amino side chains have an average percent yield of 68.8%, which is larger than the average percent yield of 40.7% for the eight compounds with two squarate cores. In future experimentation, the compounds created will be sent to the Drugs for Neglected Disease Initiative to test their efficiency against the parasite itself, giving insight into the most effective compounds in each class
Keywords
Chagas, Click Chemistry, Catalysis, Disquaramides, T. Cruzi, Neglected Tropical Disease
The fight against Chagas disease: creating an efficient and inexpensive cure
Chagas disease is caused by the parasite Trypanosoma Cruzi and plagues nearly 10 million people in the Americas. While this disease is not widely researched, it is an epidemic that is ravaging the desolate nations of Central and South America. Unfortunately for patients diagnosed with this disease, the two cures available are expensive, harmful to the patient, and are becoming alarmingly more ineffective due to drug resistances. Because of this, it is crucial that new chemical entities can be identified, created, and tested in search of a novel cure. In this research, viable drug targets from the squaramides class of compound are created from diethyl squarate in two high yielding and quick synthetic steps. Two classes of compounds have been synthesized: 1) those with two squarate cores and 2) those with one squarate core but using large amino side chains. These compounds are designed to interact with the parasite that causes Chagas disease, by puncturing holes within the membrane, killing the T. cruzi, thus ultimately curing the infected individual of this parasitic infection. This experimentation has found that the double squarate compounds are significantly lower in yield than those with different bulky side arms. The eighteen compounds with one squarate core and large amino side chains have an average percent yield of 68.8%, which is larger than the average percent yield of 40.7% for the eight compounds with two squarate cores. In future experimentation, the compounds created will be sent to the Drugs for Neglected Disease Initiative to test their efficiency against the parasite itself, giving insight into the most effective compounds in each class