Abstract
The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential.
MeSH terms
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Amides / pharmacology*
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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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CCR5 Receptor Antagonists*
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Combinatorial Chemistry Techniques
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Drug Design
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Drug Discovery
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / drug effects
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HIV-1 / drug effects
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Humans
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Microsomes, Liver / drug effects
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Molecular Structure
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology*
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Structure-Activity Relationship
Substances
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Amides
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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Piperidines