含联苯胺核心的强效丙型肝炎病毒NS5A抑制剂。
Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.
作者信息
Bae Il Hak, Choi Jin Kyu, Chough Chieyeon, Keum Sun Ju, Kim Heesun, Jang Sung Key, Kim B Moon
机构信息
Department of Chemistry, College of Natural Sciences, Seoul National University , Seoul 151-747, South Korea.
Department of Life Sciences, Pohang University of Science and Technology , Pohang 790-784, South Korea.
出版信息
ACS Med Chem Lett. 2013 Dec 4;5(3):255-8. doi: 10.1021/ml4003293. eCollection 2014 Mar 13.
Abstract
Here we report the discovery of a series of potent hepatitis C virus (HCV) NS5A inhibitors based on the benzidine prolinamide backbone. Taking a simple synthetic route, we developed a novel inhibitor structure, which allows easy modification, and through optimization of the capping group, we identified compound 6 with highly potent anti-HCV activity. Compound 6 is nontoxic and is anticipated to be an effective HCV drug candidate.
摘要
在此，我们报告基于联苯胺脯氨酰胺骨架发现了一系列强效丙型肝炎病毒（HCV）NS5A抑制剂。通过简单的合成路线，我们开发了一种易于修饰的新型抑制剂结构，并通过对封端基团的优化，鉴定出具有高效抗HCV活性的化合物6。化合物6无毒，有望成为一种有效的抗HCV药物候选物。
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