Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin

J Med Chem. 1983 Feb;26(2):294-8. doi: 10.1021/jm00356a036.


Two series of amidine derivatives consisting of a total of 24 compounds were examined for a correlation between their blocking effect on respiratory syncytial virus induced cell fusion and their inhibitory activity against selected trypsin-like protease. Although no correlation was evident between the two activities, several potentially important discoveries were made. A highly selective inhibitor of plasmin over thrombin (compound 10) was obtained, and a potent new blocker of virus-induced cell fusion (compound 22) was identified.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amidines / chemical synthesis*
  • Amidines / pharmacology
  • Animals
  • Cell Fusion / drug effects
  • Fibrinolysin / antagonists & inhibitors*
  • Liver Neoplasms, Experimental / physiopathology
  • Protease Inhibitors*
  • Rats
  • Respiratory Syncytial Viruses / drug effects
  • Respiratory Syncytial Viruses / physiology*
  • Structure-Activity Relationship
  • Thrombin / antagonists & inhibitors*
  • Trypsin Inhibitors / pharmacology*
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors*


  • Amidines
  • Protease Inhibitors
  • Trypsin Inhibitors
  • Thrombin
  • Fibrinolysin
  • Urokinase-Type Plasminogen Activator