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Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virus

Stachulski, Andrew V.; Santoro, M Gabriella; Piacentini, Sara; Belardo, Giuseppe; La Frazia, Simone; Pidathala, Chandrakala; Row, Eleanor C.; Berry, Neil G.; Iqbal, Mazhar; Allman, Sarah A.; Semple, J Edward; Eklov, Brian M.; O'Neill, Paul M. and Rossignol, Jean-Francois (2018). Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virus. Future Medicinal Chemistry, 10(8) pp. 851–862.

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DOI (Digital Object Identifier) Link: https://doi.org/10.4155/fmc-2017-0217
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Abstract

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 IC50s 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.

Item Type: Journal Item
Copyright Holders: 2018 Newlands Press
ISSN: 1756-8927
Keywords: antiviral drugs; computational chemistry; drug discovery; molecular modeling
Academic Unit/School: Faculty of Science, Technology, Engineering and Mathematics (STEM) > Life, Health and Chemical Sciences
Faculty of Science, Technology, Engineering and Mathematics (STEM)
Item ID: 54385
SWORD Depositor: Jisc Publications-Router
Depositing User: Jisc Publications-Router
Date Deposited: 16 Apr 2018 10:32
Last Modified: 27 Jan 2020 01:33
URI: http://oro.open.ac.uk/id/eprint/54385
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