Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369378 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
In a recent disclosure,1 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 EC50 in a genotype 1b replicon assay.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Omar D. Lopez, Van N. Nguyen, Denis R. St. Laurent, Makonen Belema, Michael H. Serrano-Wu, Jason T. Goodrich, Fukang Yang, Yuping Qiu, Amy S. Ripka, Peter T. Nower, Lourdes Valera, Mengping Liu, Donald R. O’Boyle II, Jin-Hua Sun, Robert A. Fridell,