- Substituted isatoic anhydrides: selective inactivators of trypsin-like serine proteases.
Substituted isatoic anhydrides: selective inactivators of trypsin-like serine proteases.
Journal of medicinal chemistry (1986-04-01)
M H Gelb, R H Abeles
PMID3514913
摘要
Derivatives of isatoic anhydride were prepared and tested as inhibitors of serine proteases. A number of isatoic anhydrides with positively charged substituents irreversibly inactivated several trypsin-like enzymes and preferentially inactivated trypsin over chymotrypsin. Further selectivity was obtained by introduction of an aromatic group on the N-1 position of isatoic anhydride. 7-(Aminomethyl)-1-benzylisatoic anhydride was prepared and was a selective inactivator of thrombin; thus it is possible to prepare derivatives of isatoic anhydride that are highly enzyme selective without attaching peptide recognition structures.
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