Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors

Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors

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 scre...

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Veröffentlicht in:Medicinal chemistry research 2021, Vol.30 (2), p.387-398
Hauptverfasser: Xu, Yanzhao, Qi, Na, Wen, Hui, Zhang, Gang, Wang, Yuchen, Cui, Huaqing
Format: Artikel
Sprache:eng
Schlagworte:
Benzenesulfonic acids
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Elastase
Inhibitors
Inorganic Chemistry
Leukocytes (neutrophilic)
Medicinal Chemistry
Neutrophils
Original Research
Pharmacology/Toxicology
Respiratory distress syndrome
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Zusammenfassung: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 (IC 50  = 35.2 μM) against hNE. Compound 4f was also superimposed onto the active center of hNE to understand the binding mode.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-020-02684-4