New benzimidazolequinones as trypanosomicidal agents

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dc.contributor.authorLopez-Lira, Claudia
dc.contributor.authorTapia, Ricardo A.
dc.contributor.authorHerrera, Alejandra
dc.contributor.authorLapier, Michel
dc.contributor.authorMaya, Juan D.
dc.contributor.authorSoto-Delgado, Jorge
dc.contributor.authorOliver, Allen G.
dc.contributor.authorLappin, A. Graham
dc.contributor.authorUriarte, Eugenio
dc.date.accessioned2025-01-20T22:20:18Z
dc.date.available2025-01-20T22:20:18Z
dc.date.issued2021
dc.description.abstractHerein, the design and synthesis of new 2-phenyl(pyridinyl)benzimidazolequinones and their 5-phenoxy derivatives as potential anti-Trypanosoma cruzi agents are described. The compounds were evaluated in vitro against the epimastigotes and trypomastigote forms of Trypanosoma cruzi. The replacing of a benzene moiety in the naphthoquinone system by an imidazole enhanced the trypanosomicidal activity against Trypanosoma cruzi. Three of the tested compounds (11a-c) showed potent trypanosomicidal activity and compound 11a, with IC50 of 0.65 mu M on the trypomastigote form of T. cruzi, proved to be 15 times more active than nifurtimox. Additionally, molecular docking studies indicate that the quinone derivatives 11a-c could have a multitarget profile interacting preferentially with trypanothione reductase and Old Yellow Enzyme.
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.bioorg.2021.104823
dc.identifier.eissn1090-2120
dc.identifier.issn0045-2068
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2021.104823
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/94620
dc.identifier.wosidWOS:000656969400006
dc.language.isoen
dc.revistaBioorganic chemistry
dc.rightsacceso restringido
dc.subjectAryloxyquinones
dc.subjectTrypanosoma cruzi
dc.subjectMolecular docking
dc.subjectTrypanothione reductase
dc.subjectOld Yellow Enzyme
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleNew benzimidazolequinones as trypanosomicidal agents
dc.typeartículo
dc.volumen111
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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