Assessment of the Activity of Nitroisoxazole Derivatives against <i>Trypanosoma cruzi</i>

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dc.contributor.authorMoncada-Basualto, Mauricio
dc.contributor.authorSaavedra-Olavarria, Jorge
dc.contributor.authorRivero-Jerez, Paula S.
dc.contributor.authorRojas, Cristian
dc.contributor.authorMaya, Juan D.
dc.contributor.authorLiempi, Ana
dc.contributor.authorZuniga-Bustos, Matias
dc.contributor.authorOlea-Azar, Claudio
dc.contributor.authorLapier, Michel
dc.contributor.authorPerez, Edwin G.
dc.contributor.authorPozo-Martinez, Josue
dc.date.accessioned2025-01-20T16:14:40Z
dc.date.available2025-01-20T16:14:40Z
dc.date.issued2024
dc.description.abstractThe 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 nitro group allows for the generation of free radicals; likewise, the large size of the compound enables increased interaction with aminoacidic residues in the active site of cruzipain, contributing to trypanocidal activity. This activity depends on the size and lipophilicity of the compounds. The study recommends exploring new compounds based on the nitroisoxazole skeleton, with larger substituents and lipophilicity to enhance their trypanocidal activity.
dc.fuente.origenWOS
dc.identifier.doi10.3390/molecules29122762
dc.identifier.eissn1420-3049
dc.identifier.urihttps://doi.org/10.3390/molecules29122762
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/90453
dc.identifier.wosidWOS:001257009700001
dc.issue.numero12
dc.language.isoen
dc.revistaMolecules
dc.rightsacceso restringido
dc.subjectChagas disease
dc.subjectTrypanosoma cruzi
dc.subjectnitroisoxazoles
dc.subjectROS
dc.subjectcruzipain enzyme
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleAssessment of the Activity of Nitroisoxazole Derivatives against <i>Trypanosoma cruzi</i>
dc.typeartículo
dc.volumen29
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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