Abstract
A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.
MeSH terms
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Animals
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Biological Availability
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CD4 Antigens / metabolism*
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Cell Line, Tumor
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Drug Design
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HIV Envelope Protein gp120 / antagonists & inhibitors*
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HIV Envelope Protein gp120 / metabolism
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HIV Fusion Inhibitors / chemical synthesis
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HIV Fusion Inhibitors / chemistry*
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HIV Fusion Inhibitors / pharmacokinetics
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HIV-1 / drug effects
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Humans
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Microsomes, Liver / metabolism
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Piperazines / chemical synthesis
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Piperazines / chemistry*
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Piperazines / pharmacokinetics
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Rats
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Structure-Activity Relationship
Substances
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CD4 Antigens
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HIV Envelope Protein gp120
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HIV Fusion Inhibitors
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Piperazines