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. 2008 Jun 1;18(11):3321-7.
doi: 10.1016/j.bmcl.2008.04.026. Epub 2008 Apr 15.

Arylethynyltriazole acyclonucleosides inhibit hepatitis C virus replication

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Arylethynyltriazole acyclonucleosides inhibit hepatitis C virus replication

Ruizhi Zhu et al. Bioorg Med Chem Lett. .

Abstract

Novel acyclic triazole nucleosides with various ethynyl moieties appended on the triazole nucleobase were synthesized efficiently using a convenient one-step Sonogashira reaction in aqueous solution and under microwave irradiation. One of the compounds, 1f, inhibited HCV subgenomic replication with a 50% effective concentration (EC(50)) of 22 microg/ml and did not inhibit proliferation of the host cell at a concentration of 50 microg/ml. A preliminary SAR study suggests that the appended phenyl ring as well as the rigid triple bond linker contributes importantly to the anti-HCV activity.

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