Journal of medicinal chemistry

Acid-sensitive latent inhibitors for proteolytic enzymes: synthesis and characterization

MS Silver, JH Haskell

Index: Silver, Marc S.; Haskell, John H. Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1253 - 1259

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Citation Number: 4

Abstract

The reaction between peptide aldehydes and acylhydrazones affords derivatives that represent potential prodrugs for selective inhibition of lysosomal enzymes. BzPheal= Ala, obtained from the reaction between N-benzoyl+ phenylalaninal and N-acetyl-calanine hydrazide, has been most carefully studied. When BzPheal= Ala is introduced into ongoing reactions catalyzed by a-chymotrypsin or papain, the rate of these reactions diminishes ...