8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study

8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study

β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay...

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Veröffentlicht in:European journal of medicinal chemistry 2021-11, Vol.224, p.113697-113697, Article 113697
Hauptverfasser: Xing, Gang, Zhi, Zhengxing, Yi, Ce, Zou, Jitian, Jing, Xuefeng, Yiu-Ho Woo, Anthony, Lin, Bin, Pan, Li, Zhang, Yuyang, Cheng, Maosheng
Format: Artikel
Sprache:eng
Schlagworte:
Asthma
COPD
Formoterol
Indacaterol
Olodaterol
β2-adrenoceptor agonist
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Zusammenfassung:β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2021.113697