Article ID Journal Published Year Pages File Type
10588050 Bioorganic & Medicinal Chemistry Letters 2013 5 Pages PDF
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).
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
, , , , , , , , ,