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In recent decades, neglected tropical diseases and poverty-related diseases have become a serious health problem worldwide. Among these pathologies, human African trypanosomiasis, and malaria present therapeutic problems due to the onset of resistance, toxicity problems and the limited spectrum of action. In this drug discovery process, rhodesain and falcipain-2, of <i>Trypanosoma brucei rhodesiense</i> and <i>Plasmodium falciparum</i>, are currently considered the most promising targets for the development of novel antitrypanosomal and antiplasmodial agents, respectively. Therefore, in our study we identified a novel lead-like compound, i.e., inhibitor <b>2b</b>, which we proved to be active against both targets, with a <i>K</i>_i = 5.06 µM towards rhodesain and an IC₅₀ = 40.43 µM against falcipain-2.