Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-β₂-agonist for the treatment of chronic obstructive pulmonary disease

Following interrogation of a wide-ligand profile database, a nonselective norepinephrin reuptake inhibitor was converted into a novel muscarinic antagonist using two medicinal chemistry transformations (M3/NRI selectivity of >1000). Conjugation to a β(2) agonist motif furnished a molecule with ba...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 54; H. 19; S. 6998
Hauptverfasser:	Osborne, Rachel, Clarke, Nick, Glossop, Paul, Kenyon, Amy, Liu, Hao, Patel, Sheena, Summerhill, Susan, Jones, Lyn H
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 13.10.2011
Schlagworte:	Adrenergic beta-2 Receptor Agonists - chemical synthesis Adrenergic beta-2 Receptor Agonists - chemistry Adrenergic beta-2 Receptor Agonists - pharmacology Adrenergic Uptake Inhibitors - chemical synthesis Adrenergic Uptake Inhibitors - chemistry Adrenergic Uptake Inhibitors - pharmacology Animals Bronchoconstriction - drug effects Bronchodilator Agents - chemical synthesis Bronchodilator Agents - chemistry Bronchodilator Agents - pharmacology Caco-2 Cells Cell Membrane Permeability Guinea Pigs Humans In Vitro Techniques Microsomes, Liver - metabolism Models, Molecular Muscarinic Antagonists - chemical synthesis Muscarinic Antagonists - chemistry Muscarinic Antagonists - pharmacology Pulmonary Disease, Chronic Obstructive - drug therapy Receptor, Muscarinic M3 - physiology Structure-Activity Relationship Trachea - drug effects Trachea - physiopathology
ISSN:	1520-4804, 1520-4804
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