Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593577 | Bioorganic & Medicinal Chemistry Letters | 2013 | 8 Pages |
Abstract
The isoquinolinamide series of HCV NS5A inhibitors exemplified by compounds 2b and 2c provided the first dual genotype-1a/1b (GT-1a/1b) inhibitor class that demonstrated a significant improvement in potency toward GT-1a replicons compared to that of the initial program lead, stilbene 2a. Structure-activity relationship (SAR) studies that uncovered an alternate phenylglycine-based cap series that exhibit further improvements in virology profile, along with some insights into the pharmacophoric elements associated with the GT-1a potency, are described.
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Authors
Makonen Belema, Van N. Nguyen, Denis R. St. Laurent, Omar D. Lopez, Yuping Qiu, Andrew C. Good, Peter T. Nower, Lourdes Valera, Donald R. II, Jin-Hua Sun, Mengping Liu, Robert A. Fridell, Julie A. Lemm, Min Gao, Jay O. Knipe, Nicholas A. Meanwell,