Issue 9, 2011
From the journal:

MedChemComm

Optimized glucuronidation of dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD†

Laura Hilton,a   Rachel Osborne,a   Amy S. Kenyon,a   Helen Baldock,a   Mark E. Bunnage,a   Jane Burrows,b   Nick Clarke,c   Michele Coghlan,c   David Entwistle,b   David Fairman,d   Neil Feeder,b   Kim James,a   Rhys M. Jones,d   Nadia Laouar,a   Graham Lunn,a   Stuart Marshall,c   Sandra D. Newman,a   Sheena Patel,c   Matthew D. Selby,a   Fiona Spence,e   Emilio F. Stuart,c   Susan Summerhill,c   Michael A. Trevethick,c   Karen N. Wright,c   Michael Yeadon,c   David A. Pricea  and  Lyn H. Jones*a  

* Corresponding authors

a Sandwich Chemistry, World Wide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich, UK

b Pharmaceutical Sciences, Pfizer, Ramsgate Road, Sandwich, UK

c Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich, UK

d Pharmacokinetics, Dynamics and Metabolism, Pfizer, Ramsgate Road, Sandwich, UK

e Drug Safety, Pfizer, Ramsgate Road, Sandwich, UK

Abstract

‘Inhalation by design’ concepts were developed to create novel dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder. A key feature of this work is the combination of balanced potency and pharmacological duration with optimised glucuronidation through the incorporation of metabolically vulnerable phenols.

Graphical abstract: Optimized glucuronidation of dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD

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Article information

DOI
https://doi.org/10.1039/C1MD00140J
Article type
Concise Article
Submitted
27 May 2011
Accepted
20 Jun 2011
First published
11 Jul 2011

Med. Chem. Commun., 2011,2, 870-876

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Optimized glucuronidation of dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD

L. Hilton, R. Osborne, A. S. Kenyon, H. Baldock, M. E. Bunnage, J. Burrows, N. Clarke, M. Coghlan, D. Entwistle, D. Fairman, N. Feeder, K. James, R. M. Jones, N. Laouar, G. Lunn, S. Marshall, S. D. Newman, S. Patel, M. D. Selby, F. Spence, E. F. Stuart, S. Summerhill, M. A. Trevethick, K. N. Wright, M. Yeadon, D. A. Price and L. H. Jones, Med. Chem. Commun., 2011, 2, 870 DOI: 10.1039/C1MD00140J

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