Abstract
A preliminary account on the structure-based design, synthesis and evaluation of peptidomimetic inhibitors of HIV-1 protease containing beta-D-mannopyranoside scaffolds is given. The compounds prepared had IC(50) values in the micromolar range. The results provide a platform for the development of more potent carbohydrate-based inhibitors of HIV-1 and other aspartic proteases.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aspartic Acid Endopeptidases / chemistry
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Binding Sites
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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 / pharmacology
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HIV-1 / drug effects*
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HIV-1 / enzymology
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Inhibitory Concentration 50
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Mannose / analogs & derivatives*
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Mannose / chemical synthesis
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Mannose / pharmacology
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Molecular Conformation
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Structure-Activity Relationship
Substances
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HIV Protease Inhibitors
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Aspartic Acid Endopeptidases
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Mannose