Design, synthesis, and anti-HCV activity of thiourea compounds.
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 (EC(50) = 0.047 microM) with a selectivity index of 596.
Kang
Iou-Jiun
IJ
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, ROC.
Wang
Li-Wen
LW
Lee
Chung-Chi
CC
Lee
Yen-Chun
YC
Chao
Yu-Sheng
YS
Hsu
Tsu-An
TA
Chern
Jyh-Haur
JH
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D015195:Drug Design; D016174:Hepacivirus / Q000187:drug effects*; D006801:Humans; D012093:Replicon / Q000235:genetics; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000998:Antiviral Agents; D013890:Thiourea