Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent β2-adrenoceptor agonists

Xing, Gang; Li, Pan; Yi, Ce; Li, Xiaoran; Ge, Xinyue; Zhao, Ying; Liu, Yichuang; Li, Jinyan; Woo, Anthony Yiu-Ho; Lin, Bin; Zhang, Yuyang; Cheng, Maosheng

doi:10.1016/j.bmc.2018.10.043

Cited by 11 publications

(9 citation statements)

References 25 publications

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“…The reduction in serum albumin is currently considered to be an independent predictor of progression to cirrhosis and mortality. 24 Previous research has indicated that PBC can be classified into three stages according to albumin and serum bilirubin concentrations. They were also considered to be the most consistent prognostic factors with survival.…”

Section: Discussionmentioning

confidence: 99%

A nomogram based on pretreatment clinical parameters for the prediction of inadequate biochemical response in primary biliary cholangitis

Tian

Liu

Sun

et al. 2020

Clinical Laboratory Analysis

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Section: Discussionmentioning

confidence: 99%

A nomogram based on pretreatment clinical parameters for the prediction of inadequate biochemical response in primary biliary cholangitis

Tian

Liu

Sun

et al. 2020

Clinical Laboratory Analysis

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“…Furthermore, a series of novel b 2 -AR agonists with a 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)one moiety have been developed (Xing et al, 2019). Compounds 9g and (R)-18c produced potent relaxant effects on ASM with a rapid onset and sustained duration of action in guinea pig trachea in vitro.…”

Section: Emerging Classes Of Bronchodilator Drugsmentioning

confidence: 99%

Pharmacology and Therapeutics of Bronchodilators Revisited

et al. 2019

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“…They utilized the indacaterol scaffold to create new β 2 agonists with a 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one moiety. 92 Two of these novel molecules, 9g and (R)-18c, are potent and selective β 2 agonists with a rapid onset of action similar to isoprenaline and a duration of action equivalent to salmeterol in cell and isolated guinea pig trachea assays and were selected for further development. They have also combined the head and tail groups of indacaterol with the core of trantinterol to produce a compound, 5a, and a series of analogs with modifications of the tail group.…”

Section: Drug Backbone Restructuringmentioning

confidence: 99%

<p>Ultra Long-Acting β-Agonists in Chronic Obstructive Pulmonary Disease</p>

Burkes¹,

Panos²

2020

JEP

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Introduction Inhaled β-agonists have been foundational medications for maintenance COPD management for decades. Through activation of cyclic adenosine monophosphate pathways, these agents relax airway smooth muscle and improve expiratory airflow by relieving bronchospasm and alleviating air trapping and dynamic hyperinflation improving breathlessness, exertional capabilities, and quality of life. β-agonist drug development has discovered drugs with increasing longer durations of action: short acting (SABA) (4–6 h), long acting (LABA) (6–12 h), and ultra-long acting (ULABA) (24 h). Three ULABAs, indacaterol, olodaterol, and vilanterol, are approved for clinical treatment of COPD. Purpose This article reviews both clinically approved ULABAs and ULABAs in development. Conclusion Indacaterol and olodaterol were originally approved for clinical use as monotherapies for COPD. Vilanterol is the first ULABA to be approved only in combination with other respiratory medications. Although there are many other ULABA’s in various stages of development, most clinical testing of these novel agents is suspended or proceeding slowly. The three approved ULABAs are being combined with antimuscarinic agents and corticosteroids as dual and triple agent treatments that are being tested for clinical use and efficacy. Increasingly, these clinical trials are using specific COPD clinical characteristics to define study populations and to begin to develop therapies that are trait-specific.

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Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent β2-adrenoceptor agonists

Cited by 11 publications

References 25 publications

A nomogram based on pretreatment clinical parameters for the prediction of inadequate biochemical response in primary biliary cholangitis

A nomogram based on pretreatment clinical parameters for the prediction of inadequate biochemical response in primary biliary cholangitis

Pharmacology and Therapeutics of Bronchodilators Revisited

<p>Ultra Long-Acting β-Agonists in Chronic Obstructive Pulmonary Disease</p>

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