ArticleAntimicrobial agents and chemotherapy2006
In vitro effects of thiazolides on Giardia lamblia WB clone C6 cultured axenically and in coculture with Caco2 cells.
Article in Antimicrobial agents and chemotherapy, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 73 citations in OpenAlex.
- Enhancing thiazolide efficacy: C-4 aryl modifications drive selective SARS-CoV-2 inhibition.Future medicinal chemistry · 2025Article
- Establishment of an in vitro co-infection model of Cryptosporidium parvum and Giardia duodenalis.Parasites & vectors · 2025Article
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- Nitazoxanide Inhibits the Bifunctional Enzyme GlG6PD::6PGL ofInternational journal of molecular sciences · 2023Article
- An Overview of Mucosa-Associated Protozoa: Challenges in Chemotherapy and Future Perspectives.Frontiers in cellular and infection microbiology · 2022Review
- Nitroreductase Activites inPathogens (Basel, Switzerland) · 2021Article
- Discovery and Preclinical Development of Antigiardiasis Fumagillol Derivatives.Antimicrobial agents and chemotherapy · 2020Article
- Transfection With Plasmid Causing Stable Expression of a Foreign Gene Affects General Proteome Pattern inFrontiers in cellular and infection microbiology · 2020Article
- Recent advances in functional research in Giardia intestinalis.Advances in parasitology · 2020Review
- Aminoguanidines: New leads for treatment of Giardia duodenalis infection.International journal for parasitology. Drugs and drug resistance · 2019Article
- Development of a Novel Ex-vivo 3D Model to Screen Amoebicidal Activity on Infected Tissue.Scientific reports · 2019Article
- Resistance formation to nitro drugs in Giardia lamblia: No common markers identified by comparative proteomics.International journal for parasitology. Drugs and drug resistance · 2019Article
- Physiological aspects of nitro drug resistance in Giardia lamblia.International journal for parasitology. Drugs and drug resistance · 2018Article
- Thiazolides promote apoptosis in colorectal tumor cells via MAP kinase-induced Bim and Puma activation.Cell death & disease · 2015Article
- Understanding drug resistance in human intestinal protozoa.Parasitology research · 2015Review
- Article
- Antigiardial activity of novel triazolyl-quinolone-based chalcone derivatives: when oxygen makes the difference.Frontiers in microbiology · 2015Article
- The effect of 3-(biphenyl-4-yl)-3-hydoxyquinuclidine (BPQ-OH) and metronidazole on Trichomonas vaginalis: a comparative study.Parasitology research · 2014Article
- O(2)-dependent efficacy of novel piperidine- and piperazine-based chalcones against the human parasite Giardia intestinalis.Antimicrobial agents and chemotherapy · 2014Article
- Nitroimidazole drugs vary in their mode of action in the human parasite Giardia lamblia.International journal for parasitology. Drugs and drug resistance · 2012Article
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The thiazolides represent a novel class of anti-infective drugs, with the nitrothiazole nitazoxanide [2-acetolyloxy-N-(5-nitro 2-thiazolyl) benzamide] (NTZ) as the parent compound. NTZ exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans. In vivo, NTZ is rapidly deacetylated to tizoxanide (TIZ), which exhibits similar activities. We have here comparatively investigated the in vitro effects of NTZ, TIZ, a number of other modified thiazolides, and metronidazole (MTZ) on Giardia lamblia trophozoites grown under axenic culture conditions and in coculture with the human cancer colon cell line Caco2. The modifications of the thiazolides included, on one hand, the replacement of the nitro group on the thiazole ring with a bromide, and, on the other hand, the differential positioning of methyl groups on the benzene ring. Of seven compounds with a bromo instead of a nitro group, only one, RM4820, showed moderate inhibition of Giardia proliferation in axenic culture, but not in coculture with Caco2 cells, with a 50% inhibitory concentration (IC50) of 18.8 microM; in comparison, NTZ and tizoxanide had IC50s of 2.4 microM, and MTZ had an IC50 of 7.8 microM. Moreover, the methylation or carboxylation of the benzene ring at position 3 resulted in a significant decrease of activity, and methylation at position 5 completely abrogated the antiparasitic effect of the nitrothiazole compound. Trophozoites treated with NTZ showed distinct lesions on the ventral disk as soon as 2 to 3 h after treatment, whereas treatment with metronidazole resulted in severe damage to the dorsal surface membrane at later time points.
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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.