Nitazoxanide, tizoxanide and other thiazolides are potent inhibitors of hepatitis B virus and hepatitis C virus replication

Korba, Brent E.; Montero, Abigail; Farrar, Kristine; Gaye, Karen; Mukerjee, Sampa; Ayers, Marc S.; Rossignol, Jean‐François

doi:10.1016/j.antiviral.2007.08.005

Cited by 208 publications

(201 citation statements)

References 35 publications

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“…Two Thiazolides derivatives (A and B) obtained from NIBGE Faisalabad (Voucher number 234) were dissolved in a solvent dimethyl sulfoxide (DMSO), following modified procedure described previously (11). Chemical structures of the thiazolides derivatives A (DD2) and B (DD10) used in this study are shown in Figure 1.…”

Section: Thiazolide Derivativesmentioning

confidence: 99%

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Antiviral Activity of Thiazolide Derivatives Against Dengue Virus in Huh-7 Cell Line

Yasmin

Yaqub

Khan

et al. 2017

Jundishapur J Microbiol

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Background: Dengue is one of the main health problems worldwide with dramatic increases in reported cases in the last few decades. Now, dengue is a major threat to half of the world's population and approximately 50 million infections occur every year. Objectives: The major aim of this study was to screen out different synthetic antiviral compounds against dengue virus. As treatments used for dengue virus infections are nonspecific and effectless, it is necessary to find specific antiviral compounds that may be helpful in the treatment of dengue fever. In cell culture models, thiazolides are active against anaerobic bacteria, protozoa, and a range of viruses. Methods: Samples from positive dengue fever patients were included in the study. For dengue serotype-2, serum samples were further confirmed by serotyping protocol. Results: After toxicological analysis, a sharp significant antiviral response was shown by compounds A and B decreasing the viral titer of serotype 2 as 46% and 53%, respectively. A greater antiviral activity was indicated by compound "B" against NS3 gene as compared to compound "A". Against NS3 gene, a comparable antiviral activity was observed for compounds "A" and "B". Conclusions: From our results, it can be concluded that compounds A and B (Thiazolides) as dengue antiviral drugs can reduce viral load in patients if their inhibitory effects are reproduced in vivo. To identify the specific active ingredients, further studies are required by using various techniques to determine the efficacy of these compounds in animal model.

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Section: Thiazolide Derivativesmentioning

confidence: 99%

“…Nonstructural proteins are responsible for the replication of viral genome and evasion from host immunity. Many antiviral compounds have been reported to inhibit DENV replication in vitro and in vivo (6,11,12). However, no approved antiviral drug is yet available for the treatment of DENV infectious disease.…”

Section: Introductionmentioning

confidence: 99%

Antiviral Activity of Thiazolide Derivatives Against Dengue Virus in Huh-7 Cell Line

Yasmin

Yaqub

Khan

et al. 2017

Jundishapur J Microbiol

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“…Nitazoxanide was originally licensed in the USA and in many countries of the world as an antiprotozoal agent and more importantly it is the only licensed drug for the treatment of the emerging apicomplexan protozoa, Cryptosporidium parvum [4]. Its antiviral activity was first reported against the hepatitis B and C viruses [5], later against the influenza A and B viruses [2] and finally against rotavirus [6]. It is being re-purposed in the USA as a broad-spectrum antiviral agent in the treatment of viral respiratory infections.…”

mentioning

confidence: 99%

Second-Generation Nitazoxanide Derivatives: Thiazolides are Effective Inhibitors of the Influenza a Virus

Stachulski

Piacentini

et al. 2018

Future Med. Chem.

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Aim:The only small molecule drugs currently available for treatment of influenza A virus (IAV) are M2 ion channel blockers and sialidase inhibitors. The prototype thiazolide, nitazoxanide, has successfully completed Phase III clinical trials against acute uncomplicated influenza.Results: We report the activity of seventeen thiazolide analogs against A/PuertoRico/8/1934(H1N1), a laboratory-adapted strain of the H1N1 subtype of IAV, in a cell culture-based assay. A total of eight analogs showed IC 50 s in the range of 0.14-5.0 μM. Additionally a quantitative structure-property relationship study showed high correlation between experimental and predicted activity based on a molecular descriptor set. Conclusion: A range of thiazolides show useful activity against an H1N1 strain of IAV. Further evaluation of these molecules as potential new small molecule therapies is justified. Graphical abstract:OR 2 A number of thiazolides (R 1 = a 3, 4 or 5-substituent; R 2 = H or CH 3 CO; R 3 = a 4´ -or 5´-substituent) are active with IC 50 = 0.14-5.0 µM against a prototypical H1N1 strain of influenza A virus in MDCK cells; a QSAR regression model was developed, showing good correlation between predicted and measured in vitro activity.Since the prototype nitazoxanide has successfully completed Phase III clinical trials against acute uncomplicated influenza, this molecule series has considerable potential for future development.

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“…6 NTZ has also recently shown antiviral activity against influenza, 7 rotavirus, 8,9 and hepatitis B virus (HBV) and hepatitis C virus (HCV) 10 in cell culture and in patients. 11,12 NTZ was shown to have activity against HCV and HBV infection through suppressing viral replication 10 by increasing the phosphorylation of eIF2a, which plays a role in the interferon (IFN)-induced antiviral response.…”

mentioning

confidence: 99%

“…11,12 NTZ was shown to have activity against HCV and HBV infection through suppressing viral replication 10 by increasing the phosphorylation of eIF2a, which plays a role in the interferon (IFN)-induced antiviral response. 13 Furthermore, in a cohort of patients infected with HCV Genotype 4, NTZ was added to standard of care (SOC) with Peg-IFN-a-2a and compared against SOC.…”

mentioning

confidence: 99%

Short Communication: Nitazoxanide Inhibits HIV Viral Replication in Monocyte-Derived Macrophages

Gekonge

Bardin

Montaner

2015

AIDS Research and Human Retroviruses

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We document the anti-HIV activity of nitazoxanide (NTZ), the first member of the thiazolide class of antiinfective drugs, originally effective against enteritis caused by Cryptosporidium parvum and Giardia lamblia. NTZ has been administered extensively worldwide, with no severe toxicities associated with its use. Here, we show for the first time that NTZ decreases HIV-1 replication in monocyte-derived macrophages (MDM) if present before or during HIV-1 infection. This NTZ effect is associated with downregulation of HIV-1 receptors CD4 and CCR5, and increasing gene expression of host cell anti-HIV resistance factors APOBEC3A/3G and tetherin. As NTZ is already in clinical use for other conditions, this newly described anti-HIV activity in MDM may facilitate innovative intensification strategies against HIV-1 when combined with current antiretroviral drug regimens.

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Nitazoxanide, tizoxanide and other thiazolides are potent inhibitors of hepatitis B virus and hepatitis C virus replication

Cited by 208 publications

References 35 publications

Antiviral Activity of Thiazolide Derivatives Against Dengue Virus in Huh-7 Cell Line

Antiviral Activity of Thiazolide Derivatives Against Dengue Virus in Huh-7 Cell Line

Second-Generation Nitazoxanide Derivatives: Thiazolides are Effective Inhibitors of the Influenza a Virus

Short Communication: Nitazoxanide Inhibits HIV Viral Replication in Monocyte-Derived Macrophages

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