Assessment of the Activity of Nitroisoxazole Derivatives against Trypanosoma cruzi.

ABSTRACT: The development of new compounds to treat Chagas disease is imperative due to the adverse effects of current drugs and their low efficacy in the chronic phase. This study aims to investigate nitroisoxazole derivatives that produce oxidative stress while modifying the compounds' lipophilicity, affecting their ability to fight trypanosomes. The results indicate that these compounds are more effective against the epimastigote form of T. cruzi, with a 52 ± 4% trypanocidal effect for compound 9. However, they are less effective against the trypomastigote form, with a 15 ± 3% trypanocidal effect. Additionally, compound 11 interacts with a higher number of amino acid residues within the active site of the enzyme cruzipain. Furthermore, it was also found that the presence of a

SUBMITTER: Moncada-Basualto M 

PROVIDER: S-EPMC11207111 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature