Inhibition of human leukocyte elastase by N-substituted peptides containing. alpha.,. alpha.-difluorostatone residues at P1

JW Skiles, C Miao, R Sorcek, S Jacober…

Index: Skiles; Fuchs; Miao; Sorcek; Grozinger; Mauldin; Vitous; Mui; Jacober; Chow; Matteo; Skoog; Weldon; Possanza; Keirns; Letts; Rosenthal Journal of Medicinal Chemistry, 1992 , vol. 35, # 4 p. 641 - 662

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Citation Number: 32

Abstract

A series of tripeptides which contain a, a-difluorostatone residues at Pl-Pl'and span the S3'sl'subsites have been shown to be potent inhibitors of human leukocyte elastase (HLE). The tripeptides described contain the nonproteinogenic achiral residue N-(2, 3-dihydro-lH- inden-2-yl) glycine at the P2-position. This residue has previously been shown in the case of HLE to be a good bioisosteric replacement for L-proline. Of the peptides prepared, those ...