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

苯磺酸衍生物作为人中性粒细胞弹性蛋白酶(hNE)抑制剂的合成及评价

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作者:Yanzhao Xu, Na Qi, Hui Wen, Gang Zhang, Yuchen Wang, Huaqing Cui

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

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