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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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Detalles Bibliográficos
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
Descripción
Sumario: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.