Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591014 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
The optimisation of two series of 4-hydroxybenzothiazolone derived β2-adrenoceptor agonists, bearing α-substituted cyclopentyl and β-phenethyl amino-substituents, as inhaled long-acting bronchodilators is described. Analogues were selected for synthesis using a lipophilicity based hypothesis to achieve the targeted rapid onset of action in combination with a long duration of action. The profiling of the two series led to identification of the α-substituted cyclopentyl analogue 2 as the optimal compound with a comparable profile to the inhaled once-daily long-acting β2-adrenoceptor agonist indacaterol. On the basis of these data 2 was promoted as the backup development candidate to indacaterol from the Novartis LABA project.
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Authors
Nicola Arnold, David Beattie, Michelle Bradley, Andrew Brearley, Lyndon Brown, Steven J. Charlton, Robin A. Fairhurst, David Farr, John Fozard, Joe Fullerton, Martin Gosling, Julia Hatto, Diana Janus, Darryl Jones, Lynne Jordan, Christine Lewis,