Screening and Identification of Inhibitors of Trypanosoma brucei Cathepsin L with Antitrypanosomal Activity

Current treatment options for human African trypanosomiasis ( HAT ) are ineffective, and they have several well‐known clinical limitations. In our continued efforts to identify chemotypes that can be developed into clinically useful drugs, we screened a targeted compound library against the major cathepsin L (rhodesain) in T. brucei . We report the antirhodesain activity and antitrypanosomal activity of the compounds in this letter. The identified compounds can serve as starting points for structure‐ and/or phenotype‐based lead optimization strategy against Trypanosoma brucei .