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MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-03-20 , DOI: 10.1016/j.bmcl.2018.03.049
Anilkumar G Nair 1 , Qingbei Zeng 1 , Oleg Selyutin 1 , Stuart B Rosenblum 1 , Yueheng Jiang 1 , De-Yi Yang 1 , Kerry Keertikar 1 , Guowei Zhou 1 , Michael Dwyer 1 , Seong Heon Kim 1 , Bandarpalle Shankar 1 , Wensheng Yu 1 , Ling Tong 1 , Lei Chen 1 , Robert Mazzola 1 , John Caldwell 1 , Haiqun Tang 1 , Sony Agrawal 1 , Rong Liu 1 , Rong Kong 1 , Paul Ingravallo 1 , Ellen Xia 1 , Ying Zhai 1 , Amin Nomeir 1 , Ernest Asante-Appiah 1 , Joseph A Kozlowski 1
Affiliation  

HCV NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays thus making them attractive components for inclusion in an all oral fixed dose combination regimen. Herein, we describe the discovery and characterization of silyl proline-containing HCV NS5A inhibitor MK-8325 with good pan-genotype activity and acceptable pharmacokinetic properties.



中文翻译:

MK-8325:一种含甲硅烷基脯氨酸的 NS5A 抑制剂,具有泛基因型活性,用于治疗 HCV

HCV NS5A 抑制剂在 HCV 复制子测定中显示出令人印象深刻的体外效力曲线,因此使其成为包含在全口服固定剂量组合方案中的有吸引力的成分。在此,我们描述了含有甲硅烷基脯氨酸的 HCV NS5A 抑制剂MK-8325的发现和表征,该抑制剂具有良好的泛基因型活性和可接受的药代动力学特性。

更新日期:2018-03-20
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