The identification of indacaterol as an ultralong-acting inhaled β2-adrenoceptor agonist

…, I Bruce, SJ Charlton, B Cuenoud, R Ernst…

Index: Baur, Francois; Beattie, David; Beer, David; Bentley, David; Bradley, Michelle; Bruce, Ian; Charlton, Steven J.; Cuenoud, Bernard; Ernst, Roland; Fairhurst, Robin A.; Faller, Bernard; Farr, David; Keller, Thomas; Fozard, John R.; Fullerton, Joe; Garman, Sheila; Hatto, Julia; Hayden, Claire; He, Handan; Howes, Colin; Janus, Diana; Jiang, Zhengjin; Lewis, Christine; Loeuillet-Ritzler, Frederique; Moser, Heinz; Reilly, John; Steward, Alan; Sykes, David; Tedaldi, Lauren; Trifilieff, Alexandre; Tweed, Morris; Watson, Simon; Wissler, Elke; Wyss, Daniel Journal of Medicinal Chemistry, 2010 , vol. 53, # 9 p. 3675 - 3684

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Citation Number: 65

Abstract

Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of β2-adrenoceptor agonists have been prepared and evaluated for their potential as inhaled ultralong-acting bronchodilators. Determination of their activities at the human β2- adrenoceptor receptor showed symmetrical substitution of the 2-aminoindan moiety at the 5- and 6-positions delivered the targeted intermediate potency and intrinsic-efficacy profiles ...