Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375792 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
Described herein is a set of non-nucleoside, small molecule inhibitors of genotype 1 HCV polymerase based on a benzothiadiazine screening hit. After demonstrating that a methylsulfonylamino D-ring substituent increased the enzyme potency into the low nanomolar range, a minimum core required for activity was explored. We observed that small aromatic rings and alkenyl groups appended to the 5-position of the B-ring were optimal, resulting in inhibitors with low nanomolar potencies.
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Authors
Pamela L. Donner, Qinghua Xie, John K. Pratt, Clarence J. Maring, Warren Kati, Wen Jiang, Yaya Liu, Gennadiy Koev, Sherie Masse, Debra Montgomery, Akhter Molla, Dale J. Kempf,