Inhalation by design: Dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD

This paper describes the successful design and development of dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder using the principles of ‘inhalation by design’. A key feature of this work is the combination of balanced potency and pharmacodynam...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 21; no. 9; pp. 2759 - 2763
Main Authors:	Jones, Lyn H., Baldock, Helen, Bunnage, Mark E., Burrows, Jane, Clarke, Nick, Coghlan, Michele, Entwistle, David, Fairman, David, Feeder, Neil, Fulton, Craig, Hilton, Laura, James, Kim, Jones, Rhys M., Kenyon, Amy S., Marshall, Stuart, Newman, Sandra D., Osborne, Rachel, Patel, Sheena, Selby, Matthew D., Stuart, Emilio F., Trevethick, Michael A., Wright, Karen N., Price, David A.
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 01.05.2011 Elsevier
Subjects:	Administration, Inhalation Adrenergic beta-2 Receptor Agonists - administration & dosage Animals antagonists Benzhydryl Compounds - administration & dosage Biological and medical sciences breathing Catecholaminergic system chemistry Cholinergic system COPD Cresols - administration & dosage Crystallinity Drug Design Drug Therapy, Combination Dual pharmacology Guinea Pigs Inhalation MABA Medical sciences Molecular Structure Muscarinic Antagonists - administration & dosage Neuropharmacology Neurotransmitters. Neurotransmission. Receptors pharmacokinetics Pharmacology. Drug treatments Phenylpropanolamine - administration & dosage Pulmonary Disease, Chronic Obstructive - drug therapy Respiratory system Tolterodine Tartrate MABA Dual pharmacology Crystallinity COPD Inhalation Agonist Nitrogen heterocycle Lactam β2-Adrenergic receptor Physicochemical properties activity relationship Aminophenols Cholinergic receptor Ex vivo Structure activity relation Bicyclic compound Chronic obstructive pulmonary disease Aromatic compound Antagonist M3 Muscarinic receptor Aminoalcohol Ether Bronchodilator Benzene derivatives In vitro Treatment Affinity Property structure relationship Lipophilicity Physicochemical properties Duration of action
ISSN:	0960-894X, 1464-3405, 1464-3405
Online Access:	Get full text
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Summary:	This paper describes the successful design and development of dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder using the principles of ‘inhalation by design’. A key feature of this work is the combination of balanced potency and pharmacodynamic duration with desirable pharmacokinetic and material properties, whilst keeping synthetic complexity to a minimum.
Bibliography:	http://dx.doi.org/10.1016/j.bmcl.2010.10.132 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 ObjectType-Article-2 ObjectType-Feature-1
ISSN:	0960-894X 1464-3405 1464-3405
DOI:	10.1016/j.bmcl.2010.10.132