Abstract
The synthesis and structure-activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36, a potent gp120-CD4 inhibitor which exhibited antiviral potency across a spectrum of 25 clade B isolates.
MeSH terms
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Animals
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CD4 Antigens / metabolism*
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Cells, Cultured
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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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Half-Life
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Humans
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Isoquinolines / chemical synthesis
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Isoquinolines / chemistry*
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Isoquinolines / pharmacokinetics
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Nicotinic Acids / chemical synthesis
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Nicotinic Acids / chemistry*
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Nicotinic Acids / 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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Isoquinolines
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Nicotinic Acids