Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
- 12 January 2021
- journal article
- research article
- Published by Springer Science and Business Media LLC in Medicinal Chemistry Research
- Vol. 30 (2), 387-398
- https://doi.org/10.1007/s00044-020-02684-4
Abstract
Herein we report our investigation concerning the development of Human neutrophil elastase (hNE) inhibitors for the treatment of Acute Respiratory Distress Syndrome (ARDS). Various benzenesulfonic acid derived compounds were synthesized and evaluated as competitive inhibitors of hNE. Biological screening revealed that compound 4f shows moderate inhibitory activity (IC50 = 35.2 μM) against hNE. Compound 4f was also superimposed onto the active center of hNE to understand the binding mode.Keywords
Funding Information
- CAMS Innovation Fund for Medical Sciences (2017-I2M-1-010, 2017-I2M-1-010)
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