Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virusStachulski, A. V., Santoro, M. G., Piacentini, S., Belardo, G., La Frazia, S., Pidathala, C., Row, E. C., Berry, N. G., Iqbal, M., Allman, S. A., Semple, J.E., Eklov, B. M., O'Neill, P. M. and Rossignol, J.-F. (2018) Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virus. Future Medicinal Chemistry, 10 (8). pp. 851-862. ISSN 1756-8927
It is advisable to refer to the publisher's version if you intend to cite from this work. See Guidance on citing. To link to this item DOI: 10.4155/fmc-2017-0217 Abstract/SummaryAim: 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.
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