ArticleAntimicrobial agents and chemotherapy2005
Efficacy of orally administered 2-substituted quinolines in experimental murine cutaneous and visceral leishmaniases.
Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 89 citations in OpenAlex.
- Efficacy of miltefosine for the treatment of American cutaneous leishmaniasis.The American journal of tropical medicine and hygiene · 2010Trial
- Quinolines: the role of substitution site in antileishmanial activity.Frontiers in chemistry · 2025Review
- The quinoline framework and related scaffolds in natural products with anti-Frontiers in chemistry · 2025Review
- Evolution of the Quinoline Scaffold for the Treatment of Leishmaniasis: A Structural Perspective.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Article
- Screening of the antileishmanial and antiplasmodial potential of synthetic 2-arylquinoline analogs.Scientific reports · 2023Article
- The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates.Molecules (Basel, Switzerland) · 2022Review
- Synthesis and evaluation of theHeliyon · 2021Article
- Nitroaromatic Antibiotics as Nitrogen Oxide Sources.Biomolecules · 2021Review
- Recent synthetic efforts in the preparation of 2-(3,4)-alkenyl (aryl) quinoline molecules towards anti-kinetoplastid agents.RSC advances · 2020Review
- Inhibition ofF1000Research · 2020Article
- GDP-Mannose Pyrophosphorylase: A Biologically Validated Target for Drug Development Against Leishmaniasis.Frontiers in cellular and infection microbiology · 2019Review
- Biochemical analysis of leishmanial and human GDP-Mannose Pyrophosphorylases and selection of inhibitors as new leads.Scientific reports · 2017Article
- VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.The Journal of infectious diseases · 2015Article
- Virtual screen for repurposing approved and experimental drugs for candidate inhibitors of EBOLA virus infection.F1000Research · 2015Article
- Investigational drugs for visceral leishmaniasis.Expert opinion on investigational drugs · 2015Article
- In vitro and in vivo activity of major constituents from Pluchea carolinensis against Leishmania amazonensis.Parasitology research · 2014Article
- Microwave-assisted synthesis of new substituted anilides of quinaldic acid.Molecules (Basel, Switzerland) · 2012Article
- Discovery of safe and orally effective 4-aminoquinaldine analogues as apoptotic inducers with activity against experimental visceral leishmaniasis.Antimicrobial agents and chemotherapy · 2012Article
- Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model.Parasite (Paris, France) · 2011Article
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We report in this study the in vivo efficacy of nine 2-substituted quinolines on the Leishmania amazonensis cutaneous infection murine model and on the Leishmania infantum and Leishmania donovani visceral infection murine models. In the case of the L. amazonensis model, quinolines were administered orally at 25 mg/kg twice daily for 15 days. Quinolines 1, 2, 3, and 7 reduced by 80 to 90% the parasite burdens in the lesion, whereas N-methylglucamine antimoniate (Glucantime), administered by subcutaneous injections at 100 mg [28 mg Sb(V)] per kg of body weight daily, reduced the parasite burdens by 98%. In visceral leishmaniasis due to L. infantum, mice treated orally at 25 mg/kg daily for 10 days with quinolines 1, 4, 5, and 6 showed a significant reduction of parasite burdens in the liver and spleen. These quinolines were significantly more effective than meglumine antimoniate to reduce the parasite burden in both the liver and spleen. Also, the oral in vivo activity of three quinolines (quinolines 4, 5, and 2-n-propylquinoline) were determined against L. donovani (LV 9) at 12.5 and 25 mg/kg for 10 days. Their activity was compared with that of miltefosine at 7.5 mg/kg. Miltefosine, 2-n-propylquinoline, and quinoline 5 at 12.5 mg/kg significantly reduced the parasite burdens in the liver by 72, 66, and 61%, respectively. From the present study, quinoline 5 is the most promising compound against both cutaneous and visceral leishmaniasis. The double antileishmanial and antiviral activities of these compounds suggest that this series could be a potential treatment for coinfection of Leishmania-human immunodeficiency virus.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.