ArticleJournal of medicinal chemistry2011
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 78 citations in OpenAlex.
- Niclosamide as a Promising Therapeutic Player in Human Cancer and Other Diseases.International journal of molecular sciences · 2022Pooled it
- Strategic Preparedness of Broad-Spectrum Antivirals for Rapid Response Towards Next Pandemics.Small science · 2026Article
- Enhancing thiazolide efficacy: C-4 aryl modifications drive selective SARS-CoV-2 inhibition.Future medicinal chemistry · 2025Article
- Salicylamide derivatives as potent HBV inhibitors: insights into structure-activity relationships.RSC medicinal chemistry · 2025Article
- Convenient syntheses of 2-acylamino-4-halothiazoles and acylated derivatives using a versatile Boc-intermediate.RSC advances · 2024Article
- Thiazolide Prodrug Esters and Derived Peptides: Synthesis and Activity.ACS bio & med chem Au · 2023Article
- Therapeutic potential of salicylamide derivatives for combating viral infections.Medicinal research reviews · 2023Review
- Nitazoxanide induced myocardial injury in zebrafish embryos by activating oxidative stress response.Journal of cellular and molecular medicine · 2021Article
- Safe-in-Man Broad Spectrum Antiviral Agents.Advances in experimental medicine and biology · 2021Article
- Drug repurposing for the treatment of COVID-19: Pharmacological aspects and synthetic approaches.Bioorganic chemistry · 2021Review
- Therapeutic potential of Nitazoxanide against Newcastle disease virus: A possible modulation of host cytokines.Cytokine · 2020Article
- Article
- Tizoxanide Inhibits Inflammation in LPS-Activated RAW264.7 Macrophages via the Suppression of NF-κB and MAPK Activation.Inflammation · 2019Article
- Review
- Synthesis and pre-clinical studies of new amino-acid ester thiazolide prodrugs.European journal of medicinal chemistry · 2017Article
- Thiazolides Elicit Anti-Viral Innate Immunity and Reduce HIV Replication.Scientific reports · 2016Article
- Antiprotozoal Nitazoxanide Derivatives: Synthesis, Bioassays and QSAR Study Combined with Docking for Mechanistic Insight.Current computer-aided drug design · 2015Article
- Nitazoxanide: a first-in-class broad-spectrum antiviral agent.Antiviral research · 2014Review
- Retinazone inhibits certain blood-borne human viruses including Ebola virus Zaire.Antiviral chemistry & chemotherapy · 2014Article
- Efficacy of nitazoxanide against clinical isolates of Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 2013Article
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
Abstract
We report the syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with QSAR analysis of our results. The prototypical thiazolide, nitazoxanide [2-hydroxybenzoyl-N-(5-nitrothiazol-2-yl)amide, NTZ] 1 is a broad spectrum antiinfective agent effective against anaerobic bacteria, viruses, and parasites. By contrast, 2-hydroxybenzoyl-N-(5-chlorothiazol-2-yl)amide 3 is a novel, potent, and selective inhibitor of hepatitis B replication (EC(50) = 0.33 μm) but is inactive against anaerobes. Several 4'- and 5'-substituted thiazolides show good activity against HBV; by contrast, some related salicyloylanilides show a narrower spectrum of activity. The ADME properties of 3 are similar to 1; viz., the O-acetate is an effective prodrug, and the O-aryl glucuronide is a major metabolite. The QSAR study shows a good correlation of observed EC(90) for intracellular virions with thiazolide structural parameters. Finally we discuss the mechanism of action of thiazolides in relation to the present results.
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Registered trials
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.