An investigation into the structure–activity relationships associated with the systematic modification of the β 2-adrenoceptor agonist indacaterol

…, ME Bradley, I Bruce, SJ Charlton, BM Cuenoud…

Index: Beattie, David; Beer, David; Bradley, Michelle E.; Bruce, Ian; Charlton, Steven J.; Cuenoud, Bernard M.; Fairhurst, Robin A.; Farr, David; Fozard, John R.; Janus, Diana; Rosethorne, Elizabeth M.; Sandham, David A.; Sykes, David A.; Trifilieff, Alexandre; Turner, Katharine L.; Wissler, Elke Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6280 - 6285

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Citation Number: 11

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, ...