Title: Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication
Authors: Skerlj, Renato ×
Bridger, Gary
Zhou, Yuanxi
Bourque, Elyse
McEachern, Ernest
Langille, Jonathan
Harwig, Curtis
Veale, Duane
Yang, Wen
Zhu, Yongbao
Bey, Michael
Baird, Ian
Sartori, Michael
Metz, Markus
Mosi, Renee
Nelson, Kim
Bodart, Veronique
Wong, Rebecca
Fricker, Simon
Mac Farland, Ron
Huskens, Dana
Schols, Dominique #
Issue Date: Dec-2011
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:21 issue:23 pages:6950-4
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.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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