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Design,synthesis, and anti-HCV activity of thiourea compounds
Authors:Iou-Jiun Kang  Li-Wen Wang  Chung-Chi Lee  Yen-Chun Lee  Yu-Sheng Chao  Tsu-An Hsu  Jyh-Haur Chern
Institution:Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, ROC
Abstract:A series of thiourea derivatives were synthesized and their antiviral activity was evaluated in a cell-based HCV subgenomic replicon assay. SAR studies revealed that the chain length and the position of the alkyl linker largely influenced the in vitro anti-HCV activity of this class of potent antiviral agents. Among this series of compounds synthesized, the thiourea derivative with a six-carbon alkyl linker at the meta-position of the central phenyl ring (10) was identified as the most potent anti-HCV inhibitor (EC50 = 0.047 μM) with a selectivity index of 596.
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