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Bioorg Med Chem Lett. 2011 Jul 1;21(13):4027-31. doi: 10.1016/j.bmcl.2011.04.135. Epub 2011 May 20.

Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.

Author information

1
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK. mike.stocks@astrazeneca.com

Abstract

The design and synthesis of a new series of high efficacy β(2)-agonists devoid of the key benzylic alcohol present in previously described highly efficacious β(2)-agonists is reported. A hypothesis for the unprecedented level of efficacy is proposed based on considerations of β(2)-adrenoceptor crystal structure, other biophysical data and modeling studies.

PMID:
21652207
DOI:
10.1016/j.bmcl.2011.04.135
[Indexed for MEDLINE]

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