| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594530 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
The installation of geminal substitution at the C5â² position of the carbosugar in our pyrimidine-derived hepatitis C inhibitor series is reported. SAR studies around the C5â² position led to the installation of the dimethyl group as the optimal functionality. An improved route was subsequently designed to access these substitutions. Expanded SAR at the C2 amino position led to the utilization of C2 ethers. These compounds exhibited good potency, high selectivity, and excellent plasma exposure and bioavailability in rodent as well as in higher species.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Vishal A. Verma, Randall Rossman, Frank Bennett, Lei Chen, Stephen Gavalas, Vinay Girijavallabhan, Yuhua Huang, Seong-Heon Kim, Aneta Kosinski, Patrick Pinto, Razia Rizvi, Bandarpalle Shankar, Ling Tong, Francisco Velazquez, Srikanth Venkatraman,