M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines
Copyright policy )M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines
Exploration of multiple regions of a bi-aryl amine template led to the identification of highly potent M(3) muscarinic acetylcholine receptor antagonists such as 14 (pA(2)=11.0) possessing good sub-type selectivity for M(3) over M(2). The structure-activity relationships (SAR) and optimization of the bi-aryl amine series are described.
- GlaxoSmithKline (United States) United States
- Cellzome, GSK, Middlesex, UK.
Receptor, Muscarinic M3, Molecular Structure, Chemistry, Pharmaceutical, Electrons, Amides, Asthma, Inhibitory Concentration 50, Kinetics, Pulmonary Disease, Chronic Obstructive, Structure-Activity Relationship, Models, Chemical, Drug Design, Humans, Amines
Receptor, Muscarinic M3, Molecular Structure, Chemistry, Pharmaceutical, Electrons, Amides, Asthma, Inhibitory Concentration 50, Kinetics, Pulmonary Disease, Chronic Obstructive, Structure-Activity Relationship, Models, Chemical, Drug Design, Humans, Amines
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