| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370423 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A novel series of cyclic urea-based CCR5 antagonists was designed aiming to resolve instability issue in the fasted simulated intestinal fluid (FSIF) associated with the acyclic urea moiety in 1. This class of CCR5 compounds demonstrated high antiviral activities against HIV-1 infection in both HOS and PBL assays. Further evaluation of these compounds indicated that 16-R not only substantially enhanced its stability, but also exhibited excellent pharmacokinetics properties.
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Related Topics
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Organic Chemistry
Authors
Maosheng Duan, Wieslaw M. Kazmierski, Matt Tallant, Jung Ho Jun, Mark Edelstein, Rob Ferris, Dan Todd, Pat Wheelan, Zhiping Xiong,