Abstract
A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / pharmacokinetics
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Animals
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CCR5 Receptor Antagonists*
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Cyclic N-Oxides / chemistry*
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Dogs
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Drug Design
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HIV-1 / drug effects*
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Humans
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Oximes
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Piperidines / chemistry*
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Pyridines / chemistry*
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Rats
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Receptors, CCR5 / metabolism
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Structure-Activity Relationship
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Virus Replication / drug effects
Substances
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Amides
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CCR5 Receptor Antagonists
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Cyclic N-Oxides
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Oximes
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Piperidines
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Pyridines
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Receptors, CCR5
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Ancriviroc