Dicarboxylic Acid bis(l-Prolyl-pyrrolidine) Amides as Prolyl Oligopeptidase Inhibitors

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 moi...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2002-09, Vol.45 (20), p.4581-4584
Main Authors: Wallén, Erik A. A, Christiaans, Johannes A. M, Forsberg, Markus M, Venäläinen, Jarkko I, Männistö, Pekka T, Gynther, Jukka
Format: Article
Language:English
Subjects:
Amides - chemical synthesis
Amides - chemistry
Analytical, structural and metabolic biochemistry
Animals
Biological and medical sciences
Brain - enzymology
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
Hydrolases
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Proline - analogs & derivatives
Proline - chemical synthesis
Proline - chemistry
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Pyrrolidines - chemical synthesis
Pyrrolidines - chemistry
Serine Endopeptidases - chemistry
Serine Proteinase Inhibitors - chemical synthesis
Serine Proteinase Inhibitors - chemistry
Serine Proteinase Inhibitors - pharmacology
Structure-Activity Relationship
Swine
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm020966g