Fibrin-stabilizing factor inhibitors. 12. 5-Dibenzylaminopentylamine and related compounds, a new type of FSF [fibrin-stabilizing factor] inhibitors

A series of omegadibenzylaminoalkylamines and related compounds have been prepared and tested as inhibitors of fibrin cross-linking. This structural type was chosen in an attempt to develop noncompetitive inhibitors of fibrinoligase. By the combination of the dibenzylamino moiety at one end and the...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1975-03, Vol.18 (3), p.278-284
Main Authors: Hoffmann, Kurt Juergen, Stenberg, Pal, Ljunggren, Christine, Svensson, Uno, Nilsson, J. Lars G, Eriksson, Olle, Hartkoorn, Ann, Lunden, Ragnar
Format: Article
Language:English
Subjects:
Benzyl Compounds - chemical synthesis
Benzyl Compounds - pharmacology
Cadaverine - pharmacology
Dansyl Compounds
Diamines - chemical synthesis
Diamines - pharmacology
Factor XIII - antagonists & inhibitors
In Vitro Techniques
Structure-Activity Relationship
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Summary:A series of omegadibenzylaminoalkylamines and related compounds have been prepared and tested as inhibitors of fibrin cross-linking. This structural type was chosen in an attempt to develop noncompetitive inhibitors of fibrinoligase. By the combination of the dibenzylamino moiety at one end and the primary amino group at the other end of a polymethylene chain, the same compound could function both as a pseudo donor substrate and as a noncompetitive alkylating inhibitor. Some of the compounds, notably 74-79, are among the most active fibrinoligase inhibitors described. However, the data indicate that the compounds probably function only as pseudo donor inhibitors.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00237a014