title: Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β₂-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.
abstract: 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).
authors: Institute of Drug Synthesis and Pharmaceutical Process, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
authors: Anqiu
authors: A
authors: Liu
authors: Ling
authors: L
authors: Huang
authors: Zhiren
authors: Z
authors: Wang
authors: Zonghua
authors: Z
authors: Luo
authors: Fei
authors: F
authors: Mao
authors: Wenjun
authors: W
authors: Shan
authors: Jiaxing
authors: J
authors: Xie
authors: Kefang
authors: K
authors: Lai
authors: Xingshu
authors: X
authors: Li
mesh_terms: D058666:Adrenergic beta-2 Receptor Agonists / Q000737:chemistry / Q000494:pharmacology*; D000420:Albuterol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D000631:Aminopyridines / Q000737:chemistry* / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology*; D001993:Bronchodilator Agents / Q000494:pharmacology; D003521:Cyclopropanes / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D058988:Phosphodiesterase 4 Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy*; D000068299:Salmeterol Xinafoate
chemical_list: D058666:Adrenergic beta-2 Receptor Agonists; D000631:Aminopyridines; D001549:Benzamides; D001993:Bronchodilator Agents; D003521:Cyclopropanes; D058988:Phosphodiesterase 4 Inhibitors; C424423:Roflumilast; D000068299:Salmeterol Xinafoate; D000420:Albuterol