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

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 sili...

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Autores principales: Antinarelli, Luciana Maria Ribeiro, de Souza, Marcus Vinicius Nora, Coelho, Eduardo Antonio Ferraz, Lima, Wallace Pacienza, Coimbra, Elaine Soares
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Sociedade Brasileira de Medicina Tropical - SBMT 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7310358/
https://www.ncbi.nlm.nih.gov/pubmed/32578713
http://dx.doi.org/10.1590/0037-8682-0091-2020
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author Antinarelli, Luciana Maria Ribeiro
de Souza, Marcus Vinicius Nora
Coelho, Eduardo Antonio Ferraz
Lima, Wallace Pacienza
Coimbra, Elaine Soares
author_facet Antinarelli, Luciana Maria Ribeiro
de Souza, Marcus Vinicius Nora
Coelho, Eduardo Antonio Ferraz
Lima, Wallace Pacienza
Coimbra, Elaine Soares
author_sort Antinarelli, Luciana Maria Ribeiro
collection PubMed
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.
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spelling pubmed-73103582020-06-24 Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis Antinarelli, Luciana Maria Ribeiro de Souza, Marcus Vinicius Nora Coelho, Eduardo Antonio Ferraz Lima, Wallace Pacienza Coimbra, Elaine Soares Rev Soc Bras Med Trop Short Communication 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. Sociedade Brasileira de Medicina Tropical - SBMT 2020-06-22 /pmc/articles/PMC7310358/ /pubmed/32578713 http://dx.doi.org/10.1590/0037-8682-0091-2020 Text en https://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License
spellingShingle Short Communication
Antinarelli, Luciana Maria Ribeiro
de Souza, Marcus Vinicius Nora
Coelho, Eduardo Antonio Ferraz
Lima, Wallace Pacienza
Coimbra, Elaine Soares
Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo) quinoline derivative against infection caused by Leishmania amazonensis
title 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_short 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
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7310358/
https://www.ncbi.nlm.nih.gov/pubmed/32578713
http://dx.doi.org/10.1590/0037-8682-0091-2020
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