Human African trypanosomiasis (HAT), commonly called African sleeping sickness, is a parasitic disease caused by the Trypanosmia brucei protozoa. Several drugs have been developed to treat HAT, but they are costly, difficult to transport, cannot kill parasites that have already moved into the brain, require extensive hospitalization, and are accompanied by a plethora of negative side effects. A safe, orally active drug that effectively kills parasites in the blood and brain is desperately needed. In 2014, GlaxoSmithKline published the results of a high-throughput screen of &gt;42,000 kinase inhibitors against T. brucei which identified 797 potent and selective hits. Of these hits, we selected NEU-0001101 for optimization.New compounds in this series of derivatives will be described.

Design, synthesis, and evaluation of 1,2-dihydroquinazolin-2-ones against Trypanosoma brucei

255th National Meeting (2018)

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