Discovery of a novel series of cyclic urea as potent CCR5 antagonists |
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| Authors: | Duan Maosheng Kazmierski Wieslaw M Tallant Matt Jun Jung Ho Edelstein Mark Ferris Rob Todd Dan Wheelan Pat Xiong Zhiping |
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| Affiliation: | Infectious Disease Medicine Discovery and Development, GlaxoSmithKline Five Moore Drive, Research Triangle Park, NC 27706, USA. |
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| 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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| Keywords: | Cyclic urea CCR5 Antagonist Pharmacokinetics HIV-1 Chemokine |
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