Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives
Autor(a) principal: | |
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Data de Publicação: | 2023 |
Outros Autores: | , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10362/153926 |
Resumo: | Copyright © 2023. Published by Elsevier Inc. |
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oai:run.unl.pt:10362/153926 |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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7160 |
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Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivativescitotoxity in animal cellsLeishmaniaPlasmodium falciparumThiazoles/pharmacologyThiosemicarbazones/pharmacologyTrypanosoma cruziRM Therapeutics. PharmacologyQR MicrobiologyRA0421 Public health. Hygiene. Preventive MedicineParasitologyPharmacology, Toxicology and Pharmaceutics(all)SDG 3 - Good Health and Well-beingSDG 9 - Industry, Innovation, and InfrastructureCopyright © 2023. Published by Elsevier Inc.In 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.Global Health and Tropical Medicine (GHTM)Instituto de Higiene e Medicina Tropical (IHMT)Vector borne diseases and pathogens (VBD)RUNSantos, Natali de França NibberingJunior, Natanael da Silva Bezerrade Oliveira, Jamerson FerreiraDuarte, Denise Maria Figueiredo AraújoDos Santos Soares, José ClebersonClara Marques, Diego Santada Silva Santos, Aline CarolineNogueira, FátimaAlves Pereira, Valéria RêgoAlves de Lima, Maria Carmoda Cruz Filho, Iranildo José2023-06-14T22:19:47Z2023-052023-05-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article14application/pdfhttp://hdl.handle.net/10362/153926eng0014-4894PURE: 61134152https://doi.org/10.1016/j.exppara.2023.108498info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-05-22T18:12:03Zoai:run.unl.pt:10362/153926Portal AgregadorONGhttps://www.rcaap.pt/oai/openairemluisa.alvim@gmail.comopendoar:71602024-05-22T18:12:03Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
title |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
spellingShingle |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives Santos, Natali de França Nibbering citotoxity in animal cells Leishmania Plasmodium falciparum Thiazoles/pharmacology Thiosemicarbazones/pharmacology Trypanosoma cruzi RM Therapeutics. Pharmacology QR Microbiology RA0421 Public health. Hygiene. Preventive Medicine Parasitology Pharmacology, Toxicology and Pharmaceutics(all) SDG 3 - Good Health and Well-being SDG 9 - Industry, Innovation, and Infrastructure |
title_short |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
title_full |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
title_fullStr |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
title_full_unstemmed |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
title_sort |
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives |
author |
Santos, Natali de França Nibbering |
author_facet |
Santos, Natali de França Nibbering Junior, Natanael da Silva Bezerra de Oliveira, Jamerson Ferreira Duarte, Denise Maria Figueiredo Araújo Dos Santos Soares, José Cleberson Clara Marques, Diego Santa da Silva Santos, Aline Caroline Nogueira, Fátima Alves Pereira, Valéria Rêgo Alves de Lima, Maria Carmo da Cruz Filho, Iranildo José |
author_role |
author |
author2 |
Junior, Natanael da Silva Bezerra de Oliveira, Jamerson Ferreira Duarte, Denise Maria Figueiredo Araújo Dos Santos Soares, José Cleberson Clara Marques, Diego Santa da Silva Santos, Aline Caroline Nogueira, Fátima Alves Pereira, Valéria Rêgo Alves de Lima, Maria Carmo da Cruz Filho, Iranildo José |
author2_role |
author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Global Health and Tropical Medicine (GHTM) Instituto de Higiene e Medicina Tropical (IHMT) Vector borne diseases and pathogens (VBD) RUN |
dc.contributor.author.fl_str_mv |
Santos, Natali de França Nibbering Junior, Natanael da Silva Bezerra de Oliveira, Jamerson Ferreira Duarte, Denise Maria Figueiredo Araújo Dos Santos Soares, José Cleberson Clara Marques, Diego Santa da Silva Santos, Aline Caroline Nogueira, Fátima Alves Pereira, Valéria Rêgo Alves de Lima, Maria Carmo da Cruz Filho, Iranildo José |
dc.subject.por.fl_str_mv |
citotoxity in animal cells Leishmania Plasmodium falciparum Thiazoles/pharmacology Thiosemicarbazones/pharmacology Trypanosoma cruzi RM Therapeutics. Pharmacology QR Microbiology RA0421 Public health. Hygiene. Preventive Medicine Parasitology Pharmacology, Toxicology and Pharmaceutics(all) SDG 3 - Good Health and Well-being SDG 9 - Industry, Innovation, and Infrastructure |
topic |
citotoxity in animal cells Leishmania Plasmodium falciparum Thiazoles/pharmacology Thiosemicarbazones/pharmacology Trypanosoma cruzi RM Therapeutics. Pharmacology QR Microbiology RA0421 Public health. Hygiene. Preventive Medicine Parasitology Pharmacology, Toxicology and Pharmaceutics(all) SDG 3 - Good Health and Well-being SDG 9 - Industry, Innovation, and Infrastructure |
description |
Copyright © 2023. Published by Elsevier Inc. |
publishDate |
2023 |
dc.date.none.fl_str_mv |
2023-06-14T22:19:47Z 2023-05 2023-05-01T00:00:00Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10362/153926 |
url |
http://hdl.handle.net/10362/153926 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
0014-4894 PURE: 61134152 https://doi.org/10.1016/j.exppara.2023.108498 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
14 application/pdf |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
instname_str |
Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
repository.mail.fl_str_mv |
mluisa.alvim@gmail.com |
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1817545937713627136 |