期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 19, 页码 6280-6285出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.07.096
关键词
beta(2)-Adrenoceptor agonists; COPD; Indacaterol; Binding kinetics; Bronchodilator
The synthesis of a series of indacaterol analogues in which each of the three structural regions of indacaterol are modified in a systematic manner is described. Evaluation of the affinity of these analogues for the beta(2)-adrenoceptor identified the 3,4-dihydroquinolinone and 5-n-butylindanyl analogues to demonstrate the most similar profiles to indacaterol. An alpha-methyl aminoindane analogue was discovered to be 25-fold more potent than indacaterol, and functional studies revealed an atypical beta(2)-adrenoceptor activation profile for this compound consistent with that of a slowly dissociating 'super agonist'. (C) 2012 Elsevier Ltd. All rights reserved.
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