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Bioorg Med Chem Lett. 2014 Jan 1;24(1):249-53. doi: 10.1016/j.bmcl.2013.11.028. Epub 2013 Nov 21.

Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.

Author information

1
Institute of Drug Synthesis and Pharmaceutical Process, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
2
Jiangsu Hansoh Pharmaceutical Research Institute Co., Ltd, Lianyungang 222000, China.
3
State Key Laboratory of Respiratory Diseases, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou 510120, China.
4
Institute of Drug Synthesis and Pharmaceutical Process, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: lixs@mail.sysu.edu.cn.

Abstract

A novel series of formoterol-phthalazinone hybrids were synthesised and evaluated as dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors. Most of the hybrids displayed high β2-adrenoceptor agonist and moderate PDE4 inhibitory activities. The most potent compound, (R,R)-11c, exhibited agonist (EC50=1.05nM, pEC50=9.0) and potent PDE4B2 inhibitory activities (IC50=0.092μM).

KEYWORDS:

Bronchodilator; Chronic obstructive pulmonary disease (COPD); PDE4 inhibitor; β(2)-Adrenoceptor agonist

PMID:
24300734
DOI:
10.1016/j.bmcl.2013.11.028
[Indexed for MEDLINE]

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