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Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives

2023-05Artigo científico Acesso aberto
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dc.contributor.authorSantos, Natali de França Nibbering
dc.contributor.authorJunior, Natanael da Silva Bezerra
dc.contributor.authorde Oliveira, Jamerson Ferreira
dc.contributor.authorDuarte, Denise Maria Figueiredo Araújo
dc.contributor.authorDos Santos Soares, José Cleberson
dc.contributor.authorClara Marques, Diego Santa
dc.contributor.authorda Silva Santos, Aline Caroline
dc.contributor.authorNogueira, Fátima
dc.contributor.authorAlves Pereira, Valéria Rêgo
dc.contributor.authorAlves de Lima, Maria Carmo
dc.contributor.authorda Cruz Filho, Iranildo José
dc.contributor.institutionVector borne diseases and pathogens (VBD)
dc.contributor.institutionGlobal Health and Tropical Medicine (GHTM)
dc.contributor.institutionInstituto de Higiene e Medicina Tropical (IHMT)
dc.contributor.pblElsevier Science B.V., Amsterdam.
dc.date.accessioned2023-06-14T22:19:47Z
dc.date.available2023-06-14T22:19:47Z
dc.date.issued2023-05
dc.descriptionCopyright © 2023. Published by Elsevier Inc.
dc.description.abstractIn this work, 13 thiosemicarbazones (1a - m) and 16 thiazoles (2a - p) were obtained, which were properly characterized by spectroscopic and spectrometric techniques. The pharmacokinetic properties obtained in silico revealed that the derivatives are in accordance with the parameters established by lipinski and veber, showing that such compounds have good bioavailability or permeability when administered orally. In assays of antioxidant activity, thiosemicarbazones showed moderate to high antioxidant potential when compared to thiazoles. In addition, they were able to interact with albumin and DNA. Screening assays to assess the toxicity of compounds to mammalian cells revealed that thiosemicarbazones were less toxic when compared to thiazoles. In relation to in vitro antiparasitic activity, thiosemicarbazones and thiazoles showed cytotoxic potential against the parasites Leishmania amazonensis and Trypanosoma cruzi. Among the compounds, 1b, 1j and 2l stood out, showing inhibition potential for the amastigote forms of the two parasites. As for the in vitro antimalarial activity, thiosemicarbazones did not inhibit Plasmodium falciparum growth. In contrast, thiazoles promoted growth inhibition. This study shows in a preliminary way that the synthesized compounds have antiparasitic potential in vitro.en
dc.description.versionpublishersversion
dc.description.versionpublished
dc.format.extent14
dc.format.extent1381217
dc.identifier.doi10.1016/j.exppara.2023.108498
dc.identifier.issn0014-4894
dc.identifier.otherPURE: 61134152
dc.identifier.otherPURE UUID: 3efafc45-ca3a-4f27-9fbf-f0462c5c3a25
dc.identifier.otherPubMed: 36907541
dc.identifier.otherWOS: 000955647800001
dc.identifier.otherScopus: 85149838193
dc.identifier.otherORCID: /0000-0003-0313-0778/work/151409105
dc.identifier.urihttp://hdl.handle.net/10362/153926
dc.language.isoeng
dc.peerreviewedyes
dc.subjectcitotoxity in animal cells
dc.subjectLeishmania
dc.subjectPlasmodium falciparum
dc.subjectThiazoles/pharmacology
dc.subjectThiosemicarbazones/pharmacology
dc.subjectTrypanosoma cruzi
dc.subjectRM Therapeutics. Pharmacology
dc.subjectQR Microbiology
dc.subjectRA0421 Public health. Hygiene. Preventive Medicine
dc.subjectParasitology
dc.subjectPharmacology, Toxicology and Pharmaceutics(all)
dc.subjectSDG 3 - Good Health and Well-being
dc.subjectSDG 9 - Industry, Innovation, and Infrastructure
dc.titleSynthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivativesen
dc.typejournal article
degois.publication.firstPage
degois.publication.lastPage
degois.publication.titleExperimental Parasitology
degois.publication.volume248
dspace.entity.typePublication
rcaap.rightsopenAccess

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