ArticleInternational journal for parasitology. Drugs and drug resistance2018
In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series.
Article in International journal for parasitology. Drugs and drug resistance, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 50 citations in OpenAlex.
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- Validated LC-MS/MS Method for Quantifying the Antiparasitic Nitroimidazole DNDI-0690 in Preclinical Target Site PK/PD Studies.Biomedical chromatography : BMC · 2025Article
- Synthesis and in vitro antitrypanosomatid activity of novel 5-nitroindole-rhodanine conjugates.Future medicinal chemistry · 2025Article
- Improving reproducibility and translational potential of mouse models: lessons from studying leishmaniasis.Frontiers in immunology · 2025Review
- Article
- Practical Synthesis of 6-Amino-1-hydroxy-2,1-benzoxaborolane: A Key Intermediate of DNDI-6148.Organic process research & development · 2024Article
- A QSAR Study for Antileishmanial 2-Phenyl-2,3-dihydrobenzofuransMolecules (Basel, Switzerland) · 2023Article
- Further Investigations of Nitroheterocyclic Compounds as Potential Antikinetoplastid Drug Candidates.Biomolecules · 2023Review
- Discovery of pyrazolopyrrolidinones as potent, broad-spectrum inhibitors ofFrontiers in tropical diseases · 2023Article
- Current leishmaniasis drug discovery.RSC medicinal chemistry · 2022Review
- DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.Journal of medicinal chemistry · 2021Article
- Identification of Resistance Determinants for a Promising Antileishmanial Oxaborole Series.Microorganisms · 2021Article
- Novel Linker Variants of Antileishmanial/Antitubercular 7-Substituted 2-Nitroimidazooxazines Offer Enhanced Solubility.ACS medicinal chemistry letters · 2021Article
- Collaborative virtual screening to elaborate an imidazo[1,2-RSC medicinal chemistry · 2021Article
- Pharmacokinetics and pharmacodynamics in the treatment of cutaneous leishmaniasis - challenges and opportunities.RSC medicinal chemistry · 2021Review
- Quinolizidine-Derived Lucanthone and Amitriptyline Analogues Endowed with Potent Antileishmanial Activity.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Antileishmanial Aminopyrazoles: Studies into Mechanisms and Stability of Experimental Drug Resistance.Antimicrobial agents and chemotherapy · 2020Article
- Of Drugs and Trypanosomatids: New Tools and Knowledge to Reduce Bottlenecks in Drug Discovery.Genes · 2020Review
- A ZnRSC advances · 2020Article
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectivesThree new chemical series (bicyclic nitroimidazoles, aminopyrazoles and oxaboroles) were selected by Drugs for Neglected Diseases initiative as potential new drug leads for leishmaniasis. Pharmacodynamics studies included both in vitro and in vivo efficacy, cross-resistance profiling against the current antileishmanial reference drugs and evaluation of their cidal activity potential.
methodsEfficacy against the reference laboratory strains of Leishmania infantum (MHOM/MA(BE)/67/ITMAP263) and L. donovani (MHOM/ET/67/L82) was evaluated in vitro on intracellular amastigotes and in vivo in the early curative hamster model. Cidal activity was assessed over a period of 15 days in an in vitro 'time-to-kill' assay. Cross-resistance was assessed in vitro on a panel of L. infantum strains with different degrees of resistance to either antimony, miltefosine or paromomycin.
resultsAll lead compounds showed potent and selective in vitro activity against the Leishmania strains tested and no cross-resistance could be demonstrated against any of the current antileishmanial drugs. Cidal activity was obtained in vitro for all series within 15 days of exposure with some differences noted between L. donovani and L. infantum. When evaluated in vivo, all lead compounds showed high efficacy and no adverse effects were observed.
conclusionsThe new lead series were shown to have cidal pharmacodynamic activity. The absence of cross-resistance with any of the current antileishmanial drugs opens possibilities for combination treatment to reduce the likelihood of treatment failures and drug resistance.
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