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Article

Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: from lead to clinical compound.

Journal of medicinal chemistry - 13 Mar 2014

Kazmierski Wieslaw M, Maynard Andrew, Duan Maosheng, Baskaran Sam, Botyanszki Janos, Crosby Renae, Dickerson Scott, Tallant Matthew, Grimes Rick, Hamatake Robert, Leivers Martin, Roberts Christopher D, Walker Jill

Abstract excerpt

Rapid clinical progress of hepatitis C virus (HCV) replication inhibitors, including these selecting for resistance in the NS5A region (NS5A inhibitors), promises to revolutionize HCV treatment. Herein, we describe our explorations of diverse spiropyrrolidine motifs in novel NS5A inhibitors and a proposed interaction model. We discovered that the 1,4-dioxa-7-azaspiro[4.4]nonane motif in inhibitor 41H (GSK2236805)...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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PMID: 24568313
DOI: 10.1021/jm4013104

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