Synthesis and evaluation of non-dimeric HCV NS5A inhibitors

被引：23

作者：

Amblard, Franck ^{[1
,2
]}

Zhang, Hongwang ^{[1
,2
]}

Zhou, Longhu ^{[1
,2
]}

Shi, Junxing ^{[3
]}

Bobeck, Drew R. ^{[3
]}

Nettles, James H. ^{[1
,2
]}

Chavre, Satish ^{[1
,2
]}

McBrayer, Tamara R. ^{[3
]}

Tharnish, Philip ^{[3
]}

Whitaker, Tony ^{[3
]}

Coats, Steven J. ^{[3
]}

Schinazi, Raymond F. ^{[1
,2
]}

机构：

[1] Emory Univ, Sch Med, Dept Pediat, Ctr AIDS Res,Lab Biochem Pharmacol, Decatur, GA 30033 USA

[2] Vet Affairs Med Ctr, Decatur, GA 30033 USA

[3] RFS Pharma LLC, Tucker, GA 30084 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 07期

关键词：

NS5A; Antiviral agent; HCV; HEPATITIS-C;

D O I：

10.1016/j.bmcl.2013.02.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000). (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：2031 / 2034

页数：4

共 24 条

[1] NS5A inhibitors: A new breakthrough for the treatment of chronic hepatitis C [J].

Asselah, Tarik .

JOURNAL OF HEPATOLOGY, 2011, 54 (05) :1069-1072

[2]

BACHAND C, 2008, Patent No. 2008144380

[3]

Bachand C., 2008, World Patent Application, Patent No. [WO-2008/021936, 2008021936]

[4]

BACHAND C, 2009, Patent No. 2009102318

[5]

Belema M., 2011, Preparation of Biphenyls End-Capped with Amino Acid or Peptide Derivatives as Hepatitis C Virus Inhibitors, Patent No. [WO 2011075439 A1, 2011075439]

[6]

Belema M., 2011, [No title captured], Patent No. [US 20110237636, 20110237636, US 20110237636 Al 20110929]

[7]

Belema M., 2011, U.S. Pat. Appl. Publ., Patent No. [US 20110286961 Al 20111124, 20110286961]

[8]

Belema M., 2010, U.S. Pat. AppL Publ, Patent No. [US 20100080772 A1 20100401, 20100080772]

[9]

Bender J.A., 2010, Preparation of Biphenylacetylenes, Biphenylethers, Terphenyls and Related Derivatives as End-Capped with Amino Acid or Peptide Derivatives as Hepatitis C Virus Inhibitors, Patent No. [WO 2010117635 A1, 2010117635]

[10]

BRISTOL MYERS SQUIBB, 2012, Patent No. 2012009394

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