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

• Published in: Journal of medicinal chemistry Vol. 26; no. 2; pp. 294 - 298
• Main Authors: Tidwell, R. R, Geratz, J. D, Dubovi, E. J
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 01-02-1983
• Subjects: amidines; Amidines - chemical synthesis; Amidines - pharmacology; Animals; cell fusion; Cell Fusion - drug effects; Fibrinolysin - antagonists & inhibitors; Liver Neoplasms, Experimental - physiopathology; Protease Inhibitors; proteinase; Rats; respiratory syncytial virus; Respiratory Syncytial Viruses - drug effects; Respiratory Syncytial Viruses - physiology; Structure-Activity Relationship; Thrombin - antagonists & inhibitors; Trypsin Inhibitors - pharmacology; Urokinase-Type Plasminogen Activator - antagonists & inhibitors
• ISSN: 0022-2623; 1520-4804
• 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.