Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis

Detalhes bibliográficos
Autor(a) principal: Luciana Maria Ribeiro Antinarelli
Data de Publicação: 2020
Outros Autores: Marcus Vinícius Nora de Souza, Eduardo Antônio Ferraz Coelho, Wallace Pacienza Lima, Elaine Soares Coimbra
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UFMG
Texto Completo: https://doi.org/10.1590/0037-8682-0091-2020
http://hdl.handle.net/1843/51832
https://orcid.org/0000-0003-1566-8110
https://orcid.org/0000-0003-1005-278X
Resumo: Introduction: The drugs currently available for leishmaniasis treatment have major limitations. Methods: In vitro and in vivo studies were performed to evaluate the effect of a quinoline derivative, Hydraqui (7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline, against Leishmania amazonensis. In silico analyses of absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters were performed. Results: Hydraqui showed significant in vitro anti-amastigote activity. Also, Hydraqui-treated mice exhibited high efficacy in lesion size (48.3%) and parasitic load (93.8%) reduction, did not cause hepatic and renal toxicity, and showed appropriate ADMET properties. Conclusions: Hydraqui presents a set of satisfactory criteria for its application as an antileishmanial agent.
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spelling 2023-04-11T21:12:15Z2023-04-11T21:12:15Z202053https://doi.org/10.1590/0037-8682-0091-20201678-9849http://hdl.handle.net/1843/51832https://orcid.org/0000-0003-1566-8110https://orcid.org/0000-0003-1005-278XIntroduction: The drugs currently available for leishmaniasis treatment have major limitations. Methods: In vitro and in vivo studies were performed to evaluate the effect of a quinoline derivative, Hydraqui (7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline, against Leishmania amazonensis. In silico analyses of absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters were performed. Results: Hydraqui showed significant in vitro anti-amastigote activity. Also, Hydraqui-treated mice exhibited high efficacy in lesion size (48.3%) and parasitic load (93.8%) reduction, did not cause hepatic and renal toxicity, and showed appropriate ADMET properties. Conclusions: Hydraqui presents a set of satisfactory criteria for its application as an antileishmanial agent.Introdução: Os fármacos atualmente disponíveis para o tratamento da leishmaniose apresentam grandes limitações. Métodos: Estudos in vitro e in vivo foram realizados para avaliar o efeito de um derivado de quinolina, Hydraqui (7-cloro-4-(3-hidroxi-benzilidenohidrazo)quinolina, contra Leishmania amazonensis. Análises in silico dos parâmetros de absorção, distribuição, metabolismo, excreção e toxicidade (ADMET) foram realizado. Resultados: Hydraqui apresentou atividade antiamastigota significativa in vitro. Além disso, camundongos tratados com Hydraqui exibiram alta eficácia na redução do tamanho da lesão (48,3%) e da carga parasitária (93,8%), não causou toxicidade hepática e renal e apresentou ADMET adequado propriedades. Conclusões: Hydraqui apresenta um conjunto de critérios satisfatórios para sua aplicação como antileishmania.CNPq - Conselho Nacional de Desenvolvimento Científico e TecnológicoFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas GeraisOutra AgênciaengUniversidade Federal de Minas GeraisUFMGBrasilCOLTEC - COLEGIO TECNICOMEDICINA - FACULDADE DE MEDICINARevista da Sociedade Brasileira de Medicina TropicalLeishmania mexicanaLeishmaniose cutâneaTratamento farmacológicoQuinolinasToxicidadeLeishmania amazonensisQuinolineChemotherapyCutaneous leishmaniasisToxicityEfficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensisEficácia do 7-cloro-4-(3-hidroxi-benzilidenohidrazo) derivado de quinolina contra infecções causada por Leishmania amazonensisinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttps://www.scielo.br/j/rsbmt/a/cGYMQ3Qpkbfj7tQrJWh6dKK/?lang=enLuciana Maria Ribeiro AntinarelliMarcus Vinícius Nora de SouzaEduardo Antônio Ferraz CoelhoWallace Pacienza LimaElaine Soares Coimbraapplication/pdfinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFMGinstname:Universidade Federal de Minas Gerais (UFMG)instacron:UFMGLICENSELicense.txtLicense.txttext/plain; charset=utf-82042https://repositorio.ufmg.br/bitstream/1843/51832/1/License.txtfa505098d172de0bc8864fc1287ffe22MD51ORIGINALEfficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline derivative against infection caused by Leishmania amazonensis.pdfEfficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline derivative against infection caused by Leishmania amazonensis.pdfapplication/pdf1291213https://repositorio.ufmg.br/bitstream/1843/51832/2/Efficacy%20of%20the%207-chloro-4-%283-hydroxy-benzilidenehydrazo%29quinoline%20derivative%20against%20infection%20caused%20by%20Leishmania%20amazonensis.pdf17f73c5c854f37d626e986cde3ece693MD521843/518322023-04-11 18:12:15.275oai:repositorio.ufmg.br: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Repositório de PublicaçõesPUBhttps://repositorio.ufmg.br/oaiopendoar:2023-04-11T21:12:15Repositório Institucional da UFMG - Universidade Federal de Minas Gerais (UFMG)false
dc.title.pt_BR.fl_str_mv Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
dc.title.alternative.pt_BR.fl_str_mv Eficácia do 7-cloro-4-(3-hidroxi-benzilidenohidrazo) derivado de quinolina contra infecções causada por Leishmania amazonensis
title Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
spellingShingle Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
Luciana Maria Ribeiro Antinarelli
Leishmania amazonensis
Quinoline
Chemotherapy
Cutaneous leishmaniasis
Toxicity
Leishmania mexicana
Leishmaniose cutânea
Tratamento farmacológico
Quinolinas
Toxicidade
title_short Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
title_full Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
title_fullStr Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
title_full_unstemmed Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
title_sort Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
author Luciana Maria Ribeiro Antinarelli
author_facet Luciana Maria Ribeiro Antinarelli
Marcus Vinícius Nora de Souza
Eduardo Antônio Ferraz Coelho
Wallace Pacienza Lima
Elaine Soares Coimbra
author_role author
author2 Marcus Vinícius Nora de Souza
Eduardo Antônio Ferraz Coelho
Wallace Pacienza Lima
Elaine Soares Coimbra
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Luciana Maria Ribeiro Antinarelli
Marcus Vinícius Nora de Souza
Eduardo Antônio Ferraz Coelho
Wallace Pacienza Lima
Elaine Soares Coimbra
dc.subject.por.fl_str_mv Leishmania amazonensis
Quinoline
Chemotherapy
Cutaneous leishmaniasis
Toxicity
topic Leishmania amazonensis
Quinoline
Chemotherapy
Cutaneous leishmaniasis
Toxicity
Leishmania mexicana
Leishmaniose cutânea
Tratamento farmacológico
Quinolinas
Toxicidade
dc.subject.other.pt_BR.fl_str_mv Leishmania mexicana
Leishmaniose cutânea
Tratamento farmacológico
Quinolinas
Toxicidade
description Introduction: The drugs currently available for leishmaniasis treatment have major limitations. Methods: In vitro and in vivo studies were performed to evaluate the effect of a quinoline derivative, Hydraqui (7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline, against Leishmania amazonensis. In silico analyses of absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters were performed. Results: Hydraqui showed significant in vitro anti-amastigote activity. Also, Hydraqui-treated mice exhibited high efficacy in lesion size (48.3%) and parasitic load (93.8%) reduction, did not cause hepatic and renal toxicity, and showed appropriate ADMET properties. Conclusions: Hydraqui presents a set of satisfactory criteria for its application as an antileishmanial agent.
publishDate 2020
dc.date.issued.fl_str_mv 2020
dc.date.accessioned.fl_str_mv 2023-04-11T21:12:15Z
dc.date.available.fl_str_mv 2023-04-11T21:12:15Z
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/1843/51832
dc.identifier.doi.pt_BR.fl_str_mv https://doi.org/10.1590/0037-8682-0091-2020
dc.identifier.issn.pt_BR.fl_str_mv 1678-9849
dc.identifier.orcid.pt_BR.fl_str_mv https://orcid.org/0000-0003-1566-8110
https://orcid.org/0000-0003-1005-278X
url https://doi.org/10.1590/0037-8682-0091-2020
http://hdl.handle.net/1843/51832
https://orcid.org/0000-0003-1566-8110
https://orcid.org/0000-0003-1005-278X
identifier_str_mv 1678-9849
dc.language.iso.fl_str_mv eng
language eng
dc.relation.ispartof.pt_BR.fl_str_mv Revista da Sociedade Brasileira de Medicina Tropical
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Minas Gerais
dc.publisher.initials.fl_str_mv UFMG
dc.publisher.country.fl_str_mv Brasil
dc.publisher.department.fl_str_mv COLTEC - COLEGIO TECNICO
MEDICINA - FACULDADE DE MEDICINA
publisher.none.fl_str_mv Universidade Federal de Minas Gerais
dc.source.none.fl_str_mv reponame:Repositório Institucional da UFMG
instname:Universidade Federal de Minas Gerais (UFMG)
instacron:UFMG
instname_str Universidade Federal de Minas Gerais (UFMG)
instacron_str UFMG
institution UFMG
reponame_str Repositório Institucional da UFMG
collection Repositório Institucional da UFMG
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