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Bioorg Med Chem Lett. 2012 Jan 1;22(1):689-95. doi: 10.1016/j.bmcl.2011.10.049. Epub 2011 Oct 20.

From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.

Author information

1
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK. dr.lilian.alcaraz@gmail.com

Abstract

Libraries of dibasic compounds designed around the molecular scaffold of the DA(2)/β(2) dual agonist sibenadet (Viozan™) have yielded a number of promising starting points that have been further optimised into novel potent and selective target molecules with required pharmacokinetic properties. From a shortlist, 31 was discovered as a novel, high potency, and highly efficacious β(2)-agonist with high selectivity and a duration of action commensurable with once daily dosing.

PMID:
22079756
DOI:
10.1016/j.bmcl.2011.10.049
[Indexed for MEDLINE]

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