期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 13, 期 2, 页码 397-416出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.10.013
关键词
CCR5 antagonist; chemokine; HIV-1; piperidine-4-carboxamide
Replacement of the 5-oxopyrrolidin-3-yl fragment in the previously reported lead structure with a 1-acetylpiperidin-4-yl group led to the discovery of a novel series of potent CCR5 antagonists. Introduction of small hydrophobic substituents on the central phenyl ring increased the binding affinity, providing low to sub-nanomolar CCR5 antagonists. The selected compound 11f showed excellent antiviral activity against CCR5-using HIV-1 replication in human peripheral blood mononuclear cells (EC50 = 0.59 nM) and an acceptable pharmacokinetic profile in dogs. (C) 2004 Elsevier Ltd. All rights reserved.
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