Abstract
A general enantioselective synthesis of new syn-hydroxyethylamine isosteres has been developed. The approach, based on the controlled opening of functionalized optically active 2,3-epoxy amines, can be conveniently used for the preparation of new peptidomimetics with various residues. Finally the total synthesis of two diastereoisomer analogues of HIV-Protease inhibitor Saquinavir has been achieved and their biological activity evaluated.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Combinatorial Chemistry Techniques
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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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Inhibitory Concentration 50
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Molecular Mimicry
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Molecular Structure
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Peptides / chemical synthesis
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Peptides / chemistry*
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Peptides / pharmacology
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Saquinavir* / analogs & derivatives
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Saquinavir* / chemical synthesis
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Saquinavir* / chemistry
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Saquinavir* / pharmacology
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Stereoisomerism
Substances
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HIV Protease Inhibitors
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Peptides
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Saquinavir