Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β 2-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD

A Liu, L Huang, Z Wang, Z Luo, F Mao, W Shan…

Index: Liu, Anqiu; Huang, Ling; Wang, Zhiren; Luo, Zonghua; Mao, Fei; Shan, Wenjun; Xie, Jiaxing; Lai, Kefang; Li, Xingshu Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1548 - 1552

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Citation Number: 14

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 activity on PDE4B2 (IC50= 0.235–1.093 μM).