Design, synthesis and evaluation of dual pharmacology β 2-adrenoceptor agonists and PDE4 inhibitors

L Huang, W Shan, Q Zhou, J Xie, K Lai, X Li

Index: Huang, Ling; Shan, Wenjun; Zhou, Qi; Xie, Jiaxing; Lai, Kefang; Li, Xingshu Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 1 p. 249 - 253

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Citation Number: 9

Abstract

Abstract A novel series of formoterol–phthalazinone hybrids were synthesised and evaluated as dual pharmacology β 2-adrenoceptor agonists and PDE4 inhibitors. Most of the hybrids displayed high β 2-adrenoceptor agonist and moderate PDE4 inhibitory activities. The most potent compound,(R, R)-11c, exhibited agonist (EC 50= 1.05 nM, pEC 50= 9.0) and potent PDE4B2 inhibitory activities (IC 50= 0.092 μM).