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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Autores principales: Xu, Yanzhao, Qi, Na, Wen, Hui, Zhang, Gang, Wang, Yuchen, Cui, Huaqing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2021
Materias:
Original Research
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7801566/
https://www.ncbi.nlm.nih.gov/pubmed/33456292
http://dx.doi.org/10.1007/s00044-020-02684-4
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author Xu, Yanzhao
Qi, Na
Wen, Hui
Zhang, Gang
Wang, Yuchen
Cui, Huaqing
author_facet Xu, Yanzhao
Qi, Na
Wen, Hui
Zhang, Gang
Wang, Yuchen
Cui, Huaqing
author_sort Xu, Yanzhao
collection PubMed
description 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.
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spelling pubmed-78015662021-01-12 Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors Xu, Yanzhao Qi, Na Wen, Hui Zhang, Gang Wang, Yuchen Cui, Huaqing Med Chem Res Original Research 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. Springer US 2021-01-12 2021 /pmc/articles/PMC7801566/ /pubmed/33456292 http://dx.doi.org/10.1007/s00044-020-02684-4 Text en © The Author(s), under exclusive licence to Springer Science+Business Media, LLC part of Springer Nature 2021 This article is made available via the PMC Open Access Subset for unrestricted research re-use and secondary analysis in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic.
spellingShingle Original Research
Xu, Yanzhao
Qi, Na
Wen, Hui
Zhang, Gang
Wang, Yuchen
Cui, Huaqing
Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
title Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
title_full Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
title_fullStr Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
title_full_unstemmed Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
title_short Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors
title_sort synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hne) inhibitors
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7801566/
https://www.ncbi.nlm.nih.gov/pubmed/33456292
http://dx.doi.org/10.1007/s00044-020-02684-4
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