Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture

被引:66
作者
Burton, G
Ku, TW
Carr, TJ
Kiesow, T
Sarisky, RT
Lin-Goerke, J
Baker, A
Earnshaw, DL
Hofmann, GA
Keenan, RM
Dhanak, D
机构
[1] GlaxoSmithKline, Collegeville, PA 19426 USA
[2] GlaxoSmithKline, King Of Prussia, PA 19406 USA
[3] GlaxoSmithKline, Harlow CM19 5AW, Essex, England
关键词
hepatitis C virus; RNA polymerase; pyrrolidine; combinatorial mixture;
D O I
10.1016/j.bmcl.2005.01.076
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
HTS of the compound collection for inhibition of the HCV RNA dependent RNA polymerase identified two 168 member N-acyl pyrrolidine combinatorial mixture hits. Deconvolution and expansion of these mixtures by solid phase synthesis to establish initial SAR and identify a potent inhibitor is reported. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1553 / 1556
页数:4
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