Metronidazole Therapy for Visceral Leishmaniasis

Estal, P. Laguna del; Moya, M. S.; Martin, Tungotyo; Lucero, M. J.; Salgado, Rául Mederos

doi:10.1093/clinids/19.6.1161

Cited by 4 publications

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“…Some in vitro studies by Arora and others (1991) and in vivo studies by Iong (1973), Masramon (1981) and Laguna del Estal (1994) have demonstrated the efficacy of metronidazole against Leishmania species even in human immunodeficiency virus-positive patients (Arranz-Caso 1995) and in a small prospective study of human visceral leishmaniasis (Mishra and others 1985) the recovery rate was 60 per cent.…”

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confidence: 97%

Efficacy of the treatment of dogs with leishmaniosis with a combination of metronidazole and spiramycin

et al. 2005

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Twenty-seven dogs infected naturally with Leishmania infantum were used in a randomised controlled trial to compare the clinical and parasitological efficacy of an oral treatment with a combination of metronidazole and spiramycin (13 dogs) with the efficacy of conventional treatment with meglumine antimonate and allopurinol (14 dogs) as controls. In the test group one dog had to be withdrawn from the treatment because it developed pemphigus foliaceus; 10 of the dogs were clinically responsive but none was cured parasitologically. In the control group four dogs were withdrawn from the treatment because of side effects; eight of the dogs were clinically responsive but none was cured parasitologically. The control group showed signs of improvement after an average of 30 days, whereas the test group did not show signs of improvement until after an average of 45 days.

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confidence: 97%

Efficacy of the treatment of dogs with leishmaniosis with a combination of metronidazole and spiramycin

et al. 2005

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“…Hence, in search of new potential candidates, we took the initiative to bring together the pharmacores of quinoline and metranidazole within a single entity. This is because metronidazoles are broad spectrum antiprotozoan drugs, which are known to exert significant efficacy against experimental VL and have the potential to lower parasitic burden if used in combination with other compounds. − On other hand, quinolines and its derivatives have been reported for their activity against both in vitro and in vivo form of experimental visceral and cutaneous leishmaniasis (against strains like L. donovani, L.…”

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Synthesis, Biological Evaluation, Structure–Activity Relationship, and Mechanism of Action Studies of Quinoline–Metronidazole Derivatives Against Experimental Visceral Leishmaniasis

et al. 2019

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In our efforts to identify novel chemical scaffolds for the development of antileishmanial agents, a series of quinoline–metronidazole hybrid compounds was synthesized and tested against the murine model of visceral leishmaniasis. Among all synthesized derivatives, 15b and 15i showed significant antileishmanial efficacy against both extracellular promastigote (IC50 9.54 and 5.42 μM, respectively) and intracellular amastigote (IC50 9.81 and 3.75 μM, respectively) forms of Leishmania donovani with negligible cytotoxicity toward the host (J774 macrophages, Vero cells). However, compound 15i effectively inhibited the parasite burden in the liver and spleen (>80%) of infected BALB/c mice. Mechanistic studies revealed that 15i triggers oxidative stress which induces bioenergetic collapse and apoptosis of the parasite by decreasing ATP production and mitochondrial membrane potential. Structure–activity analyses and pharmacokinetic studies suggest 15i as a promising antileishmanial lead and emphasize the importance of quinoline–metronidazole series as a suitable platform for the future development of antileishmanial agents.

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Experimental Evaluation of Second-Line Oral Treatments of Visceral Leishmaniasis Caused by Leishmania infantum

Gangneux

Dullin

Sulahian

et al. 1999

Antimicrob Agents Chemother

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Metronidazole Therapy for Visceral Leishmaniasis

Cited by 4 publications

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Efficacy of the treatment of dogs with leishmaniosis with a combination of metronidazole and spiramycin

Efficacy of the treatment of dogs with leishmaniosis with a combination of metronidazole and spiramycin

Synthesis, Biological Evaluation, Structure–Activity Relationship, and Mechanism of Action Studies of Quinoline–Metronidazole Derivatives Against Experimental Visceral Leishmaniasis

Experimental Evaluation of Second-Line Oral Treatments of Visceral Leishmaniasis Caused by Leishmania infantum

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