Synthesis of peptidyl fluoromethyl ketones and peptidyl. alpha.-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human …

…, JP Burkhart, MR Angelastro, EL Giroux…

Index: Peet; Burkhart; Angelastro; Giroux; Mehdi; Bey; Kolb; Neises; Schirlin Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 394 - 407

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Citation Number: 147

Abstract

Comparison of MeO-Suc-Val-Pro-Phe-C02Me (29) and MeO-Suc-Ala-Ala-Pro-Phe-COzMe (25) with their corresponding trifluoromethyl ketones 9a and 9b, respectively, in rat and human neutrophil cathepsin G assays showed the a-keto esters to be more potent inhibitors. Likewise, Ac-Pro-Ala-Pro-Ala-C0, Me (21) was more potent than its correspondirg trifluoromethyl ketone (9c) in both porcine pancreatic elastase and human neutrophil ...