期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 21, 页码 6470-6475出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.080
关键词
Pyridyl carboxamide; CCR5; Antagonist; Pharmacokinetics; HIV-1; Chemokine
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. (C) 2011 Elsevier Ltd. All rights reserved.
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