Design, synthesis and evaluation of dual pharmacology ß2-adrenoceptor agonists and PDE4 inhibitors.

A novel series of formoterol-phthalazinone hybrids were synthesised and evaluated as dual pharmacology ß2-adrenoceptor agonists and PDE4 inhibitors. Most of the hybrids displayed high ß2-adrenoceptor agonist and moderate PDE4 inhibitory activities. The most potent compound, (R,R)-11c, exhibited agonist (EC50=1.05nM, pEC50=9.0) and potent PDE4B2 inhibitory activities (IC50=0.092µM).