Cargando…
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...
Autores principales: | , , , , |
---|---|
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 |
_version_ | 1783549353416196096 |
---|---|
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. |
format | Online Article Text |
id | pubmed-7310358 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Sociedade Brasileira de Medicina Tropical - SBMT |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT antinarellilucianamariaribeiro efficacyofthe7chloro43hydroxybenzilidenehydrazoquinolinederivativeagainstinfectioncausedbyleishmaniaamazonensis AT desouzamarcusviniciusnora efficacyofthe7chloro43hydroxybenzilidenehydrazoquinolinederivativeagainstinfectioncausedbyleishmaniaamazonensis AT coelhoeduardoantonioferraz efficacyofthe7chloro43hydroxybenzilidenehydrazoquinolinederivativeagainstinfectioncausedbyleishmaniaamazonensis AT limawallacepacienza efficacyofthe7chloro43hydroxybenzilidenehydrazoquinolinederivativeagainstinfectioncausedbyleishmaniaamazonensis AT coimbraelainesoares efficacyofthe7chloro43hydroxybenzilidenehydrazoquinolinederivativeagainstinfectioncausedbyleishmaniaamazonensis |