1424337-30-3Relevant academic research and scientific papers
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD
Liu, Anqiu,Huang, Ling,Wang, Zhiren,Luo, Zonghua,Mao, Fei,Shan, Wenjun,Xie, Jiaxing,Lai, Kefang,Li, Xingshu
, p. 1548 - 1552 (2013/03/28)
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 (IC 50 = 0.235-1.093 μM).
