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Updated: Jul 30, 2026

Monitoring Neutrophil Elastase and Cathepsin G Activity in Human Sputum Samples
Published on: May 21, 2021
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams
S J Macdonald1, M D Dowle, L A Harrison
1Medical Chemistry 2, Glaxo Wellcome Medicines Research Centre, Stevenage, UK. sjfm5947@glaxowellcome.co.uk
Abstract:
Described are the acylation binding of trans-lactam 1 to porcine pancreatic elastase, the selection of the SO2Me activating group for the lactam N which also confers metabolic stability in hamster liver microsomes, the introduction of aqueous solubility through the piperidine salt 9, the in vivo oral activity of 9 and its bioavailability, and the introduction of 9 as an intracellular neutrophil elastase inhibitor.
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