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Rev. Soc. Bras. Med. Trop ; 53: e20200091, 2020. graf
Article Dans Anglais | SES-SP, ColecionaSUS, LILACS | ID: biblio-1136875

Résumé

Abstract 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.


Sujets)
Animaux , Femelle , Quinoléines/usage thérapeutique , Leishmania mexicana/effets des médicaments et des substances chimiques , Leishmaniose cutanée/traitement médicamenteux , Antiprotozoaires/usage thérapeutique , Quinoléines/composition chimique , Leishmaniose cutanée/parasitologie , Modèles animaux de maladie humaine , Charge parasitaire , Souris , Souris de lignée BALB C
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