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Recent Developments in Therapies and Strategies Against COVID-19
Published in Hanadi Talal Ahmedah, Muhammad Riaz, Sagheer Ahmed, Marius Alexandru Moga, The Covid-19 Pandemic, 2023
Misbah Hameed, M. Zia-Ul-Haq, Marius Moga
Nitazoxanide is a broad-spectrum antiviral and antiparasitic agent. It is used for the treatment of different helminthic, protozoal, and viral infections. Nitazoxanide is the prototype agent of the thiazolides, which is a group having synthetic nitrothiazolyl-salicylamide derivatives with antiviral and antiparasitic activity. Tizoxanide, an active metabolite of nitazoxanide also antiparasitic drug of the thiazolide class. Clinical trials of nitazoxanide against influenza has been done and shown inhibitory effect on a broad range of influenza virus subtypes. The drug is also effective against influenza viruses which develop some resistance to neuraminidase inhibitors like oseltamivir Nitazoxanide is also being investigated as a potential treatment for chronic hepatitis B, chronic hepatitis C, norovirus gastroenteritis and rotavirus.
The Renewal of Interest in Nitroaromatic Drugs
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Nicolas Primas, Caroline Ducros, Patrice Vanelle, Pierre Verhaeghe
Also studied were other 5-membered heterocycles like the 5-nitrothiazoles. Nitazoxanide (35) (Figure 10), belonging to the thiazolide family (thiazole-amide), is a broad-spectrum antiparasitic molecule indicated for the treatment of infection by Cryptosporidium parvum and Giardia lamblia infections. In humans, the salicylate moiety of nitazoxanide (35) is rapidly metabolized to tizoxanide (36) (Figure 10), which is as effective as the parent drug (Broekhuysen et al. 2000). Chan-Bacab et al. assessed the activity of both nitazoxanide (35) and its de-acetyl metabolite tizoxanide (36), as well as one other related compound (37) (Figure 10) (Chan-Bacab et al. 2009). These derivatives were twice active as benznidazole (9) against T. cruzi epimastigotes. Structures of some antichagasic 5-nitrothiazoles.
Nitazoxanide
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Drug levels after administration of the nitazoxanide suspension are 70% of those achieved with tablets (Romark Laboratories, 2005). If nitazoxanide is taken with food, the bioavailability of the drug is greatly increased, with this effect being greater for the tablets than for the suspension (Romark Laboratories, 2005). Nitazoxanide is rapidly deacetylated (half-life of 6 minutes) into its main active metabolite, tizoxanide, of which over 99% is bound to plasma proteins (Broekhuysen et al., 2000). Tizoxanide is further glucuronidated to tizoxanide glucuronide, which can be found in human plasma, urine, and bile (Broekhuysen et al., 2000).
Current pharmacotherapy of cryptosporidiosis: an update of the state-of-the-art
Published in Expert Opinion on Pharmacotherapy, 2021
Anne Schneider, Sebastian Wendt, Christoph Lübbert, Henning Trawinski
The discovery of potential molecular targets (e.g. CDPK1, PI(4)K and isoprenoid synthesis) and high-throughput phenotypic screening have led to the development of several new chemical entities which have proven to be active in vitro and in mice studies [31]. To date, only a small number of these entities (BKI of CDPK1, PI(4)K inhibitor KDU731, piperazine-based compound MMV665917 and the benzoxaboroles derivative AN7973) have been tested among neonatal calves, whose infection are considered to most closely resemble human infection [31,32,41]. Unfortunately, many newly discovered compounds have already been abandoned due to relevant toxicity. Better news is that a new thiazolide compound, aminoxanide, a prodrug of tizoxanide, the active metabolite of nitazoxanide, has been synthetized. Parenterally administered aminoxanide is as effective as a 4-fold lower dose of oral nitazoxanide and could be a candidate for treatment of severe and/or extraintestinal cryptosporidiosis [52].
Searching for effective antiviral small molecules against influenza A virus: A patent review
Published in Expert Opinion on Therapeutic Patents, 2021
Tiziana Ginex, F. Javier Luque
Nitazoxanide is an FDA-approved thiazolide initially licensed for the treatment of parasitic infections with minimal adverse side effects but patented as anti-influenza agent [114] (Figure 6). The compound is a prodrug that is rapidly hydrolyzed to the active form, tizoxanide, and has been reported to inhibit a broad array of viruses in both tissue culture and animal models. This compound blocks the maturation of the viral glycoprotein HA, altering its intracellular trafficking and insertion into the host plasma membrane, but the net effect is reinforced by a broad amplification of the innate immune response [115].
Drug repurposing strategies and key challenges for COVID-19 management
Published in Journal of Drug Targeting, 2022
Shubham Mule, Ajit Singh, Khaled Greish, Amirhossein Sahebkar, Prashant Kesharwani, Rahul Shukla
Due to its antiviral potential, nitazoxanide an antiparasitic medication, and its deacylated metabolite tizoxanide have been repurposed for the management of COVID infected patients. Efficacy of nitazoxanide against SARS-COV2 occurs through amplification of melanoma differentiation-associated protein 5, retinoic acid-inducible gene 1, mitochondrial antiviral-signalling protein 5, afterward, interferon-stimulated genes are downregulated. In peripheral blood mononuclear cells, nitazoxanide effectively inhibits the cytokine surge caused by cellular infiltration [144].