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Identification of novel epoxide inhibitors of hepatitis C virus replication using a high-throughput screen.


ABSTRACT: Using our high-throughput hepatitis C replicon assay to screen a library of over 8,000 novel diversity-oriented synthesis (DOS) compounds, we identified several novel compounds that regulate hepatitis C virus (HCV) replication, including two libraries of epoxides that inhibit HCV replication (best 50% effective concentration, < 0.5 microM). We then synthesized an analog of these compounds with optimized activity.

SUBMITTER: Peng LF 

PROVIDER: S-EPMC2043288 | biostudies-literature | 2007 Oct

REPOSITORIES: biostudies-literature

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Identification of novel epoxide inhibitors of hepatitis C virus replication using a high-throughput screen.

Peng Lee F LF   Kim Sun Suk SS   Matchacheep Sirinya S   Lei Xiaoguang X   Su Shun S   Lin Wenyu W   Runguphan Weerawat W   Choe Won-Hyeok WH   Sakamoto Naoya N   Ikeda Masanori M   Kato Nobuyuki N   Beeler Aaron B AB   Porco John A JA   Schreiber Stuart L SL   Chung Raymond T RT  

Antimicrobial agents and chemotherapy 20070806 10


Using our high-throughput hepatitis C replicon assay to screen a library of over 8,000 novel diversity-oriented synthesis (DOS) compounds, we identified several novel compounds that regulate hepatitis C virus (HCV) replication, including two libraries of epoxides that inhibit HCV replication (best 50% effective concentration, < 0.5 microM). We then synthesized an analog of these compounds with optimized activity. ...[more]

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