Abstract
A series of P1/P1' substituted cyclic urea analogues were prepared in an attempt to increase the intra-cellular antiviral potency of the nonsymmetrical 3-aminoindazoles DMP 850 and DMP 851. The effect of alkyl substitution of the P1/P1' residues on cellular antiviral potency, protein binding, resistance profile and pharmacokinetics are described.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Dogs
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Drug Resistance
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HIV / drug effects
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HIV Protease Inhibitors / chemical synthesis*
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HIV Protease Inhibitors / pharmacokinetics
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HIV Protease Inhibitors / pharmacology*
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Heterocyclic Compounds, 4 or More Rings / chemical synthesis
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Heterocyclic Compounds, 4 or More Rings / pharmacokinetics
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Heterocyclic Compounds, 4 or More Rings / pharmacology
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Hydrophobic and Hydrophilic Interactions
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Protein Binding
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Structure-Activity Relationship
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Urea / analogs & derivatives*
Substances
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DMP 850
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DMP 851
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HIV Protease Inhibitors
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Heterocyclic Compounds, 4 or More Rings
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Urea