Abstract
A series of peptidomimetic human immunodeficiency virus (HIV) protease inhibitors containing substituted allophenylnorstatine (Apns: (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid) were designed and synthesized. From the structure-activity relationship of this series of compounds, SM-309515 was found to have potent antiviral activity against wild-type and resistant HIV-1s and to possess a desirable pharmacokinetic profile in dogs.
MeSH terms
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Animals
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Dogs
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Drug Design
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HIV Protease Inhibitors / chemical synthesis
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HIV Protease Inhibitors / chemistry*
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HIV Protease Inhibitors / metabolism
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HIV Protease Inhibitors / pharmacology*
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HIV-1 / drug effects
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HIV-1 / enzymology
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HIV-1 / genetics
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Hepatocytes / drug effects
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Hepatocytes / enzymology
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Humans
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Molecular Structure
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Mutation / genetics
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Phenylbutyrates / chemical synthesis
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Phenylbutyrates / chemistry*
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Phenylbutyrates / pharmacology*
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Sensitivity and Specificity
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Structure-Activity Relationship
Substances
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HIV Protease Inhibitors
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Phenylbutyrates
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3-amino-2-hydroxy-4-phenylbutanoic acid