Synthesis and biological evaluation of novel anti-hepatitis C virus (HCV) agents: 2-hydroxylphenethyl sulfanyl-oxopyrimidines
| Autor: | Feng Yue, Xian Chen, Wu Daochun, Wang Yueping, Xia Xueshan, Yan-Ping He, Cong Li, Hua Wang, Yang Junfeng, Yufang Zhang, Christopher C. Lai |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Molecular model Chemistry Hepatitis C virus Organic Chemistry Thio medicine.disease_cause 01 natural sciences Virology In vitro Virus 0104 chemical sciences 010404 medicinal & biomolecular chemistry 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology Sulfanyl medicine Pyrimidone General Pharmacology Toxicology and Pharmaceutics EC50 |
| Zdroj: | Medicinal Chemistry Research. 26:1388-1396 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-017-1815-z |
| Popis: | A novel series of dihydro-hydroxyl-phene-thylsulfanyl-ω-cyclohexyl/phenyl-oxopyrimidine derivatives have been synthesized and their in vitro anti-hepatitis C virus activities have been evaluated using Huh 7.5.1 cells. Some of the compounds showed moderate anti-hepatitis C virus activities, with EC50 range from 7.53 to 0.13 μM. Among all the compounds, 6-(cyclohexylmethyl)-5-ethyl-2-((2-hydroxy-2-phenylethyl)thio)-pyrimidin-4 (3H)-one (3a) had the most promising potential in inhibiting hepatitis C virus with an EC50 value of 0.13 μM and SI value of 121. It was noticed that some of these compounds are both active on hepatitis C virus and human immunodeficiency virus. In addition to experimental evaluation, structure-activity relationships and the molecular modeling analysis of these new congeners are also discussed. |
| Databáze: | OpenAIRE |
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