Chalcogen Derivatives for the Treatment of African Trypanosomiasis: Biological Evaluation of Thio- and Seleno-Semicarbazones and Their Azole Derivatives.

ABSTRACT: Human African trypanosomiasis (HAT) is caused by Trypanosoma brucei. Drug therapy remains challenging due to drug resistance and/or toxicity. New drugs are needed. Using thiosemicarbazones as a starting point, we employed a S to Se isosteric replacement strategy to design 44 analogs which were evaluated against T. brucei in vitro. Compounds were divided into 11 groups of four derivatives corresponding to thio-, selenosemicarbazones, and their cyclic counterparts, thio- and selenazoles. We selected three groups which contained a total of six derivatives that inhibited parasite growth by >70%. Then, we investigated the mechanism of action of these compounds, performing quantitative assays to measure their inhibition of the T. brucei cathepsin L-like protease (TbrC

SUBMITTER: Rubio-Hernandez M 

PROVIDER: S-EPMC12177781 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature