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

Rev Soc Bras Med Trop. 2020 Jun 22:53:e20200091. doi: 10.1590/0037-8682-0091-2020. eCollection 2020.

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.

MeSH terms

  • Animals
  • Antiprotozoal Agents / therapeutic use*
  • Disease Models, Animal
  • Female
  • Leishmania mexicana / drug effects*
  • Leishmaniasis, Cutaneous / drug therapy*
  • Leishmaniasis, Cutaneous / parasitology
  • Mice
  • Mice, Inbred BALB C
  • Parasite Load
  • Quinolines / chemistry
  • Quinolines / therapeutic use*

Substances

  • Antiprotozoal Agents
  • Quinolines
  • quinoline