| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370442 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
A novel series of pyridyl carboxamide-based CCR5 inhibitors was designed, synthesized, and demonstrated to be highly potent against HIV-1 infection in both HOS and PBL assays. Attempts to evaluate this series of compounds in a rat PK model revealed its instability in rat plasma. A hypothesis for this liability was proposed, and strategies to overcome this issue were pursued, leading to discovery of highly potent 40 and 41, which featured dramatically improved rat PK profiles.
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Related Topics
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Authors
Maosheng Duan, Wieslaw M. Kazmierski, Pek Y. Chong, Felix DeAnda, Mark Edelstein, Rob Ferris, Jennifer Peckham, Pat Wheelan, Zhiping Xiong, Huichang Zhang, Rena Nishizawa, Yoshikazu Takaoka,