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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Detalles Bibliográficos
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
Descripción
Sumario: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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