Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588050 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A novel class of dual pharmacology bronchodilators targeting both β2-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better β2-adrenoceptor agonist activities (pEC50 = 8.47-9.20) than the reference compound salmeterol (pEC50 = 8.3) and good inhibitory activities on PDE4B2 (IC50 = 0.235-1.093 μM).
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Authors
Anqiu Liu, Ling Huang, Zhiren Wang, Zonghua Luo, Fei Mao, Wenjun Shan, Jiaxing Xie, Kefang Lai, Xingshu Li,