| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372130 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics.
Graphical abstractA series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Renato Skerlj, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Ernest McEachern, Jonathan Langille, Curtis Harwig, Duane Veale, Wen Yang, Tongshong Li, Yongbao Zhu, Michael Bey, Ian Baird, Michael Sartori, Markus Metz, Renee Mosi, Kim Nelson, Veronique Bodart,