A novel class of dual pharmacology bronchodilators targeting both β(2)-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better β(2)-adrenoceptor agonist activities (pEC(50)=8.47-9.20) than the reference compound salmeterol (pEC(50)=8.3) and good inhibitory activity on PDE4B2 (IC(50)=0.235-1.093 μM).