Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules

We sought to design dual pharmacology bronchodilators targeting both the M 3 muscarinic acetylcholine and beta-2 adrenergic (β 2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-03, Vol.21 (5), p.1354-1358
Hauptverfasser:	Hughes, Adam D., Chin, Kay H., Dunham, Sarah L., Jasper, Jeffrey R., King, Kristin E., Lee, Tae Weon, Mammen, Mathai, Martin, Jerri, Steinfeld, Tod
Format:	Artikel
Sprache:	eng
Schlagworte:	acetylcholine Adrenergic beta-2 Receptor Agonists - chemical synthesis Adrenergic beta-2 Receptor Agonists - chemistry Adrenergic beta-2 Receptor Agonists - pharmacology agonists antagonists Beta 2 adrenoceptor agonist Biological and medical sciences Bronchodilator Bronchodilator Agents - chemical synthesis Bronchodilator Agents - chemistry Bronchodilator Agents - pharmacology bronchodilators Catecholaminergic system chemistry Cholinergic system COPD Drug Design Dual pharmacology Humans Inhaled LABA LAMA MABA Medical sciences Molecular Structure Multivalent approach Muscarinic acetylcholine receptor antagonist Muscarinic Antagonists - chemical synthesis Muscarinic Antagonists - chemistry Muscarinic Antagonists - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors pharmacology Pharmacology. Drug treatments receptors Receptors, Adrenergic, beta-2 - chemistry Receptors, Muscarinic - chemistry Respiratory system Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	We sought to design dual pharmacology bronchodilators targeting both the M 3 muscarinic acetylcholine and beta-2 adrenergic (β 2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.01.043