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Synthesis, antiviral activity, preliminary pharmacokinetics and structural parameters of thiazolide amine salts.
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- Additional Information
- Source:
Publisher: Future Science Country of Publication: England NLM ID: 101511162 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1756-8927 (Electronic) Linking ISSN: 17568919 NLM ISO Abbreviation: Future Med Chem Subsets: MEDLINE
- Publication Information:
Original Publication: London : Future Science, 2009-
- Subject Terms:
- Abstract:
Background: The thiazolides, typified by nitazoxanide, are an important class of anti-infective agents. A significant problem with nitazoxanide and its active circulating metabolite tizoxanide is their poor solubility. Results: We report the preparation and evaluation of a series of amine salts of tizoxanide and the corresponding 5-Cl thiazolide. These salts demonstrated improved aqueous solubility and absorption, as shown by physicochemical and in vivo measurements. They combine antiviral activity against influenza A virus with excellent cell safety indices. We also report the x-ray crystal structural data of the ethanolamine salt. Conclusion: The ethanol salt of thiazolide retains the activity of the parent together with an improved cell safety index, making it a good candidate for further evaluation.
- Contributed Indexing:
Keywords: amine salts; antiviral; pharmacokinetics; thiazolides; x-ray structure
- Accession Number:
0 (Amines)
0 (Antiviral Agents)
0 (Salts)
0 (Thiazoles)
- Publication Date:
Date Created: 20210817 Date Completed: 20220208 Latest Revision: 20220208
- Publication Date:
20221213
- Accession Number:
10.4155/fmc-2021-0055
- Accession Number:
34402654
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