Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents

摘要

Author summary Human African trypanosomiasis (HAT) is a parasitic disease prevalent in sub-Saharan Africa. Current treatments cause severe toxicity, are difficult to administer, and are susceptible to resistance. In order to quickly discover new leads for HAT drug discovery, we screened human kinase inhibitors against Trypanosoma brucei, the parasite that causes HAT, and discovered several hundred compounds that demonstrated antiparasitic activity. In this paper, we present the results of medicinal chemistry follow-up work on a group of compounds known as isatins.