Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
© The Author(s), under exclusive licence to Springer Science+Business Media, LLC part of Springer Nature 2021..
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:30 |
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| Enthalten in: |
Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents - 30(2021), 2 vom: 12., Seite 387-398 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Xu, Yanzhao [VerfasserIn] |
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| Links: |
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| Themen: |
ARDS |
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| Anmerkungen: |
Date Revised 18.02.2022 published: Print-Electronic Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1007/s00044-020-02684-4 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM320189139 |
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| 520 | |a © The Author(s), under exclusive licence to Springer Science+Business Media, LLC part of Springer Nature 2021. | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a ARDS | |
| 650 | 4 | |a Benzenesulfonic acid | |
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| 700 | 1 | |a Zhang, Gang |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Yuchen |e verfasserin |4 aut | |
| 700 | 1 | |a Cui, Huaqing |e verfasserin |4 aut | |
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