Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596558 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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 β2-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 β2-adrenoceptor activation profile for this compound consistent with that of a slowly dissociating 'super agonist'.
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Authors
David Beattie, 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,