Abstract
The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak activity at the hERG ion channel.
MeSH terms
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Acquired Immunodeficiency Syndrome / drug therapy
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology*
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Butanes / chemical synthesis*
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Butanes / chemistry
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Butanes / pharmacology*
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CCR5 Receptor Antagonists*
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Combinatorial Chemistry Techniques
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Ether-A-Go-Go Potassium Channels / drug effects
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HIV / drug effects
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HIV Infections / drug therapy
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Humans
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Molecular Structure
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Piperidines / pharmacology*
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Structure-Activity Relationship
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Tropanes / chemistry
Substances
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Anti-HIV Agents
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Butanes
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CCR5 Receptor Antagonists
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Ether-A-Go-Go Potassium Channels
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KCNH1 protein, human
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Piperidines
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Tropanes