| Literature DB >> 22932315 |
David Beattie1, David Beer, Michelle E Bradley, Ian Bruce, Steven J Charlton, Bernard M Cuenoud, Robin A Fairhurst, David Farr, John R Fozard, Diana Janus, Elizabeth M Rosethorne, David A Sandham, David A Sykes, Alexandre Trifilieff, Katharine L Turner, Elke Wissler.
Abstract
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 β(2)-adrenoceptor identified the 3,4-dihydroquinolinone and 5-n-butylindanyl analogues to demonstrate the most similar profiles to indacaterol. An α-methyl aminoindane analogue was discovered to be 25-fold more potent than indacaterol, and functional studies revealed an atypical β(2)-adrenoceptor activation profile for this compound consistent with that of a slowly dissociating 'super agonist'.Entities:
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Year: 2012 PMID： 22932315 DOI： 10.1016/j.bmcl.2012.07.096
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823