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

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??M) against hNE. Compound 4f was also superimposed onto the active center of hNE to understand the binding mode.

SUBMITTER: Xu Y 

PROVIDER: S-EPMC7801566 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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

Xu Yanzhao Y   Qi Na N   Wen Hui H   Zhang Gang G   Wang Yuchen Y   Cui Huaqing H  

Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents 20210112 2

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 <b>4f</b> shows moderate inhibitory activity (IC<sub>50</sub> = 35.2 μM) against hNE. Compound <b>4f</b> was also superimposed onto the active center of hNE to understand  ...[more]

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