期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 4, 页码 1523-1526出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.013
关键词
Asthma and COPD; Bronchodilator; beta(2)-Adrenoceptor agonist; PDE4 inhibitor
资金
- Natural Science Foundation of China [20972198]
- State Key Laboratory of Respiratory Diseases [2007DA-80154F1110]
We designed and synthesized a novel class of dual pharmacology bronchodilators targeting both beta 2-adrenoceptor and PDE4 by applying a multivalent approach. The most potent dual pharmacology molecule, compound 29, possessed good inhibitory activity on PDE4B2 (IC50 = 0.278 mu M, which was more potent than phthalazinone, IC50 = 0.520 mu M) and possessed excellent relaxant effects on tracheal rings precontracted by histamine (pEC(50) = 9.3). (C) 2012 Elsevier Ltd. All rights reserved.
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