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Bioorg Med Chem Lett. 2011 Aug 1;21(15):4612-6. doi: 10.1016/j.bmcl.2011.05.097. Epub 2011 Jun 13.

Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.

Author information

1
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, Leicestershire, UK. steve.connolly@astrazeneca.com

Abstract

Starting with the molecular scaffold of the DA(2)/β(2) dual agonist sibenadet (Viozan™), a number of molecular changes were incorporated, which were designed to increase the potency and selectivity of the target molecule, and improve its pharmacokinetics. Through this process a novel, high potency, full β(2)-agonist with high selectivity and long duration capable of being dosed once daily has been discovered.

PMID:
21723724
DOI:
10.1016/j.bmcl.2011.05.097
[Indexed for MEDLINE]

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