Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.

Abstract

A series of peptide-based transition-state human neutrophil elastase (HNE) inhibitors with N-terminal acidic moieties were synthesized and their inhibitory activity against HNE was evaluated both in vitro and in vivo. Our results show that compounds containing cyclic amide bridged acidic moieties at the N-terminal have not only improved water solubility but… (More)
DOI: 10.1016/j.bmc.2009.09.020

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Cite this paper

@article{Inoue2009DevelopmentOA, title={Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.}, author={Yasunao Inoue and Tomoki Omodani and Ryotaro Shiratake and Hiroshi Okazaki and A. Kuromiya and Taeko Kubo and Fuminori Sato}, journal={Bioorganic & medicinal chemistry}, year={2009}, volume={17 21}, pages={7477-86} }