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Human neutrophil elastase phosphonic inhibitors with improved potency of action

Ł Winiarski, J Oleksyszyn…

文献索引:Winiarski, Lukasz; Oleksyszyn, Jozef; Sienczyk, Marcin Journal of Medicinal Chemistry, 2012 ,  vol. 55,  # 14  p. 6541 - 6553

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被引用次数: 18

摘要

Herein, we present the synthesis and the measurement of the inhibitory activity of novel peptidyl derivatives of α-aminoalkylphosphonate diaryl esters as human neutrophil elastase inhibitors. Their selectivity against other serine proteases, including porcine pancreatic elastase, chymotrypsin, and trypsin, was also demonstrated. We also describe the preparation of single peptide diastereomers. The most active and selective compound ...