Arylethynyltriazole acyclonucleosides inhibit hepatitis C virus replication.
Arylethynyltriazole acyclonucleosides inhibit hepatitis C virus replication.
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DOI:
10.1016/j.bmcl.2008.04.026
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发表时间:
2008-06
影响因子:
2.7
通讯作者:
Ruizhi Zhu;Menghua Wang;Yi Xia;Fanqi Qu;J. Neyts;Ling Peng
中科院分区:
文献类型:
--
作者:
Ruizhi Zhu;Menghua Wang;Yi Xia;Fanqi Qu;J. Neyts;Ling Peng
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 (EC50) of 22μg/ml and did not inhibit proliferation of the host cell at a concentration of 50μg/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.