- Synthesis, activity, and pharmacokinetic properties of a series of conformationally-restricted thiourea analogs as novel hepatitis C virus inhibitors
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A series of novel conformationally-restricted thiourea analogs were designed, synthesized, and evaluated for their anti-HCV activity. Herein we report the synthesis, structure-activity relationships (SARs), and pharmacokinetic properties of this new class of thiourea compounds that showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon assay. Among compounds tested, the fluorene compound 4b was found to possess the most potent activity (EC50 = 0.3 μM), lower cytotoxicity (CC50 > 50 μM), and significantly better pharmacokinetic properties compared to its corresponding fluorenone compound 4c.
- Kang, Iou-Jiun,Wang, Li-Wen,Yeh, Teng-Kuang,Lee, Chung-Chi,Lee, Yen-Chun,Hsu, Sheng-Ju,Wu, Yen-Shian,Wang, Jing-Chyi,Chao, Yu-Sheng,Yueh, Andrew,Chern, Jyh-Haur
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experimental part
p. 6414 - 6421
(2010/10/04)
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