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Bioorg Med Chem Lett. 2013 Feb 1;23(3):779-84. doi: 10.1016/j.bmcl.2012.11.086. Epub 2012 Dec 3.

HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies.

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  • 1Department of Medicinal Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. omar.lopez@bms.com


In a recent disclosure, we described the discovery of dimeric, prolinamide-based NS5A replication complex inhibitors exhibiting excellent potency towards an HCV genotype 1b replicon. That disclosure dealt with the SAR exploration of the peripheral region of our lead chemotype, and herein is described the SAR uncovered from a complementary effort that focused on the central core region. From this effort, the contribution of the core region to the overall topology of the pharmacophore, primarily vector orientation and planarity, was determined, with a set of analogs exhibiting <10 nM EC(50) in a genotype 1b replicon assay.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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