A Non-Peptide-Based Fluorogenic Small-Molecule Probe for Elastase and Its Application

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Human neutrophil elastase (HNE) has been identified as a potential therapeutic target for the discovery of anti-inflammatory drugs for decades.However, the HNE-targeting drug discovery has achieved little progress due to the unavailability of synthetic substrates for measuring the activity of HNE.Herein, a small-molecule compound, 2,2,3,3,3-pentafluoro-N-(2-oxo-4-(trifluoromethyl)-2H-chromen-7-yl)-propanamide (compound 4), has been successfully designed as the first-ever non-peptide-based fluorogenic substrate for HNE.
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