Neglected tropical diseases (NTDs) affect the world’s poorest population; mainly in Africa, Asia, and Latin America. According to the WHO, more than one billion people are affected by NTDs. The connection between these areas is the lack of proper sanition, and the persistence of the diseases, trap the affected countries in the poverty and disease cycle.<br/>African sleeping sickness, a prevalent NTD, is a parasitic infection caused by two parasites from the Trypanosoma brucei species and is transmitted by the tsetse fly or congenitally. The disease is manifested by fever, severe headaches, irritability, extreme fatigue, swollen lymph nodes, and aching muscles and joints. When it reaches the central nervous system it can cause progressive confusion, personality changes, and other neurologic problems. The high-cost and limited number of the drugs contribute to the increase of the cases resulting in a great impact on global health.<br/>The goal of our research is to develop inexpensive and effective drugs using low-cost organic starting materials that target the T. brucei parasite. Our target compounds are Mannich bases containing an aromatic moiety. Previous, but limited, studies have shown that this class of compounds demonstrates promising results against T. brucei. Our one step synthesis involves the use of nitro-substituted acetophenones, formaldehyde, and a variety of amines to make Mannich bases under conventional heating and microwave conditions. By changing the nitro-acetophenones and the amines used in the reaction, we hope to develop a robust drug library we can use to screen against T. brucei.

Mannich bases: A facile drug synthesis toward the treatment of human African trypanosomiasis

ACS Spring Meeting 2021

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