Abstract
New dicarboxylic acid bis(L-prolyl-pyrrolidine) amides were synthesized, and their inhibitory activity against prolyl oligopeptidase from pig brain was tested in vitro. As compared with earlier described prolyl oligopeptidase inhibitors, these new compounds have in common an L-prolyl-pyrrolidine moiety, but the typical lipophilic acyl end group is replaced by another L-prolyl-pyrrolidine moiety connected symmetrically with a short dicarboxylic acid linker. These compounds are a new type of peptidomimetic prolyl oligopeptidase inhibitor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Animals
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Brain / enzymology
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Proline / analogs & derivatives*
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Proline / chemical synthesis*
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Proline / chemistry
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Prolyl Oligopeptidases
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / chemistry
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Serine Endopeptidases / chemistry*
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Serine Proteinase Inhibitors / chemical synthesis*
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology
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Structure-Activity Relationship
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Swine
Substances
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Amides
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Pyrrolidines
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Serine Proteinase Inhibitors
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Proline
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Serine Endopeptidases
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Prolyl Oligopeptidases