ArticleEuropean journal of medicinal chemistry2016
Nitroimidazole carboxamides as antiparasitic agents targeting Giardia lamblia, Entamoeba histolytica and Trichomonas vaginalis.
Article in European journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 70 citations in OpenAlex.
- A Lactone-Enabled Approach to Metronidazole-Based Scaffolds.The Journal of organic chemistry · 2026Article
- Importance and Involvement of Imidazole Structure in Current and Future Therapy.Molecules (Basel, Switzerland) · 2026Review
- Perspective on the use of scraping cytology for jawbone destructive lesions, entamoeba gingivalis, and actinomyces co-infection: a retrospective analysis.Head & face medicine · 2025Article
- Antigiardial and antiamebic activities of fexinidazole and its metabolites: new drug leads for giardiasis and amebiasis.Antimicrobial agents and chemotherapy · 2024Article
- A Bioluminescence-Based Drug Screen Identifies Activities of Fexinidazole and Its Metabolites againstAntibiotics (Basel, Switzerland) · 2022Article
- Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950-2021 Comprehensive Overview.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Inhibiting Pyridoxal Kinase ofFrontiers in cellular and infection microbiology · 2021Article
- Recent advances in the molecular biology of the protist parasiteFaculty reviews · 2021Review
- Antitubercular and Antiparasitic 2-Nitroimidazopyrazinones with Improved Potency and Solubility.Journal of medicinal chemistry · 2020Article
- 30 years of parasitology research analysed by text mining.Parasitology · 2020Article
- Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.Journal of medicinal chemistry · 2018Article
- High-Throughput Screening ofFrontiers in cellular and infection microbiology · 2018Article
- Detection and Investigation of Eagle Effect Resistance to Vancomycin inFrontiers in microbiology · 2018Article
- Click Chemistry-Facilitated Structural Diversification of Nitrothiazoles, Nitrofurans, and Nitropyrroles Enhances Antimicrobial Activity against Giardia lamblia.Antimicrobial agents and chemotherapy · 2017Article
- Design, Synthesis and Biological Evaluation of 2-(2-Amino-5(6)-nitro-1H-benzimidazol-1-yl)-N-arylacetamides as Antiprotozoal Agents.Molecules (Basel, Switzerland) · 2017Article
- Design, Synthesis and Preliminary Antimicrobial Evaluation ofMedChemComm · 2017Article
- Recent advances inF1000Research · 2016Review
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
Abstract
Diarrhoeal diseases caused by the intestinal parasites Giardia lamblia and Entamoeba histolytica constitute a major global health burden. Nitroimidazoles are first-line drugs for the treatment of giardiasis and amebiasis, with metronidazole 1 being the most commonly used drug worldwide. However, treatment failures in giardiasis occur in up to 20% of cases and development of resistance to metronidazole is of concern. We have re-examined 'old' nitroimidazoles as a foundation for the systematic development of next-generation derivatives. Using this approach, derivatisation of the nitroimidazole carboxamide scaffold provided improved antiparasitic agents. Thirty-three novel nitroimidazole carboxamides were synthesised and evaluated for activity against G. lamblia and E. histolytica. Several of the new compounds exhibited potent activity against G. lamblia strains, including metronidazole-resistant strains of G. lamblia (EC50 = 0.1-2.5 μM cf. metronidazole EC50 = 6.1-18 μM). Other compounds showed improved activity against E. histolytica (EC50 = 1.7-5.1 μM cf. metronidazole EC50 = 5.0 μM), potent activity against Trichomonas vaginalis (EC50 = 0.6-1.4 μM cf. metronidazole EC50 = 0.8 μM) and moderate activity against the intestinal bacterial pathogen Clostridium difficile (0.5-2 μg/mL, cf. metronidazole = 0.5 μg/mL). The new compounds had low toxicity against mammalian kidney and liver cells (CC50 > 100 μM), and selected antiparasitic hits were assessed for human plasma protein binding and metabolic stability in liver microsomes to demonstrate their therapeutic potential.
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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.