Abstract
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
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amidines / chemical synthesis*
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Amidines / pharmacology
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Animals
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Cell Fusion / drug effects
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Fibrinolysin / antagonists & inhibitors*
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Liver Neoplasms, Experimental / physiopathology
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Protease Inhibitors*
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Rats
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Respiratory Syncytial Viruses / drug effects
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Respiratory Syncytial Viruses / physiology*
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Structure-Activity Relationship
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Thrombin / antagonists & inhibitors*
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Trypsin Inhibitors / pharmacology*
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Urokinase-Type Plasminogen Activator / antagonists & inhibitors*
Substances
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Amidines
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Protease Inhibitors
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Trypsin Inhibitors
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Thrombin
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Fibrinolysin
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Urokinase-Type Plasminogen Activator