Novel 4-Thiazolidinones as Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase
| Autor: | İlkay Küçükgüzel, Esra Tatar, Tanaji T. Talele, Javairia Zia, Dinesh Manvar, Bhargav A. Patel, Amartya Basu, Rupa Guhamazumder, Gizem Çakır, Neerja Kaushik-Basu |
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| Rok vydání: | 2014 |
| Předmět: |
Molecular model
Stereochemistry viruses Hepatitis C virus education virus diseases Pharmaceutical Science RNA-dependent RNA polymerase Hepatitis C Biology medicine.disease medicine.disease_cause digestive system diseases chemistry.chemical_compound chemistry Active compound Drug Discovery medicine IC50 NS5B Nucleoside |
| Zdroj: | Archiv der Pharmazie. 348:10-22 |
| ISSN: | 0365-6233 |
| DOI: | 10.1002/ardp.201400247 |
| Popis: | In continuation of our efforts to develop new derivatives as hepatitis C virus (HCV) NS5B inhibitors, we synthesized novel 5-arylidene-4-thiazolidinones. The novel compounds 29–42, together with their synthetic precursors 22–28, were tested for HCV NS5B inhibitory activity; 12 of these compounds displayed IC50 values between 25.3 and 54.1 µM. Compound 33, an arylidene derivative, was found to be the most active compound in this series with an IC50 value of 25.3 µM. Molecular docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds. |
| Databáze: | OpenAIRE |
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