Abstract
A series of novel spirocyclic ethers were designed to function as nonpeptidal P2-ligands for HIV-1 protease inhibitors. Incorporation of designed ligands in the (R)-(hydroxyethylamino)sulfonamide isostere afforded potent HIV protease inhibitors.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Crystallography, X-Ray
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Drug Design
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Ethers, Cyclic / chemical synthesis*
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Ethers, Cyclic / chemistry*
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Ethers, Cyclic / pharmacology
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HIV Protease / metabolism*
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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 / enzymology
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Humans
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Kinetics
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Ligands
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Models, Molecular
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Molecular Conformation
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Ethers, Cyclic
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HIV Protease Inhibitors
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Ligands
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HIV Protease