ArticleAntimicrobial agents and chemotherapy2005
In vitro efficacies of nitazoxanide and other thiazolides against Neospora caninum tachyzoites reveal antiparasitic activity independent of the nitro group.
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 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 55 citations in OpenAlex.
- A review and meta-analysis of the impact of intestinal worms on child growth and nutrition.Maternal & child nutrition · 2008Pooled it
- Construction of luciferase-expressing Neospora caninum and drug screening.Parasites & vectors · 2024Article
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- Amixicile Reduces Severity of Cryptosporidiosis but Does Not HaveAntimicrobial agents and chemotherapy · 2018Article
- In Vitro Evaluation of Novel Nitazoxanide Derivatives againstACS omega · 2017Article
- Antiprotozoal Nitazoxanide Derivatives: Synthesis, Bioassays and QSAR Study Combined with Docking for Mechanistic Insight.Current computer-aided drug design · 2015Article
- Di-cationic arylimidamides act against Neospora caninum tachyzoites by interference in membrane structure and nucleolar integrity and are active against challenge infection in mice.International journal for parasitology. Drugs and drug resistance · 2012Article
- Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication.Journal of medicinal chemistry · 2011Article
- Challenges of antibacterial discovery.Clinical microbiology reviews · 2011Review
- Evaluation of new thiazolide/thiadiazolide derivatives reveals nitro group-independent efficacy against in vitro development of Cryptosporidium parvum.Antimicrobial agents and chemotherapy · 2010Article
- Toltrazuril treatment of congenitally acquired Neospora caninum infection in newborn mice.Parasitology research · 2009Article
- Host cells participate in the in vitro effects of novel diamidine analogues against tachyzoites of the intracellular apicomplexan parasites Neospora caninum and Toxoplasma gondii.Antimicrobial agents and chemotherapy · 2008Article
- A novel Giardia lamblia nitroreductase, GlNR1, interacts with nitazoxanide and other thiazolides.Antimicrobial agents and chemotherapy · 2007Article
- Review
- In vitro metacestodicidal activities of genistein and other isoflavones against Echinococcus multilocularis and Echinococcus granulosus.Antimicrobial agents and chemotherapy · 2006Article
- In vitro effects of thiazolides on Giardia lamblia WB clone C6 cultured axenically and in coculture with Caco2 cells.Antimicrobial agents and chemotherapy · 2006Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The thiazolide nitazoxanide [2-acetolyloxy-N-(5-nitro-2-thiazolyl)benzamide] (NTZ) exhibits a broad spectrum of activities against a wide variety of intestinal and tissue-dwelling helminths, protozoa, and enteric bacteria infecting animals and humans. The drug has been postulated to act via reduction of its nitro group by nitroreductases, including pyruvate ferredoxin oxidoreductase. In this study, we investigated the efficacies of nitazoxanide and a number of other thiazolides against Neospora caninum tachyzoites in vitro. We employed real-time-PCR-based monitoring of tachyzoite adhesion, invasion, and intracellular proliferation, as well as electron microscopic visualization of the effects imposed by nitazoxanide. In addition, we investigated several modified versions of this drug. These modifications included on one hand the replacement of the nitro group on the thiazole ring with a bromide, thus removing the most reactive group, and on the other hand the differential positioning of methyl groups on the salicylate ring. We show that the thiazole-associated nitro group is not necessarily required for the action of the drug and that methylation of the salicylate ring can result in complete abrogation of the antiparasitic activity, depending on the positioning of the methyl group. These findings indicate that other mechanisms besides the proposed mode of action involving the pyruvate ferredoxin oxidoreductase enzyme could be responsible for the wide spectrum of antiparasitic activity of NTZ and that modifications in the benzene ring could be important in these alternative mechanisms.
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