Journal of medicinal chemistry

Substituted isatoic anhydrides: selective inactivators of trypsin-like serine proteases

MH Gelb, RH Abeles

Index: Gelb, Michael H.; Abeles, Robert H. Journal of Medicinal Chemistry, 1986 , vol. 29, # 4 p. 585 - 589

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Citation Number: 29

Abstract

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)-l-benzylisatoic anhydride was prepared and was a selective ...