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Bioorg Med Chem Lett. 2012 Jan 1;22(1):300-4. doi: 10.1016/j.bmcl.2011.11.013. Epub 2011 Nov 9.

3-heterocyclyl quinolone inhibitors of the HCV NS5B polymerase.

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1
Myrexis Inc., 305 Chipeta Way, Salt Lake City, UT 84108, USA.

Abstract

The discovery and optimization of a novel class of quinolone small-molecules that inhibit NS5B polymerase, a key enzyme of the HCV viral life-cycle, is described. Our research led to the replacement of a hydrolytically labile ester functionality with bio-isosteric heterocycles. An X-ray crystal structure of a key analog bound to NS5B facilitated the optimization of this series of compounds to afford increased activity against the target enzyme and in the cell-based replicon assay system.

PMID:
22119470
DOI:
10.1016/j.bmcl.2011.11.013
[Indexed for MEDLINE]
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