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

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,...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-08, Vol.21 (15), p.4612-4616
Main Authors: CONNOLLY, Stephen, ALCARAZ, Lilian, KANE, Zoe, PAINE, Stuart, PAIRAUDEAU, Garry, STOCKS, Michael J, YOUNG, Alan, BAILEY, Andrew, CADOGAN, Elaine, CHRISTIE, Jadeen, COOK, Anthony R, FISHER, Adrian J, HILL, Stephen, HUMPHRIES, Alexander, INGALL, Anthony H
Format: Article
Language:English
Subjects:
Adrenergic beta-2 Receptor Agonists - chemical synthesis
Adrenergic beta-2 Receptor Agonists - chemistry
Adrenergic beta-2 Receptor Agonists - pharmacokinetics
Animals
Biological and medical sciences
Bronchodilator Agents - chemical synthesis
Bronchodilator Agents - chemistry
Bronchodilator Agents - pharmacokinetics
Catecholaminergic system
Drug Design
Drug Evaluation, Preclinical
Guinea Pigs
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Receptors, Adrenergic, beta-2 - chemistry
Receptors, Adrenergic, beta-2 - metabolism
Respiratory system
Structure-Activity Relationship
Thiazoles - chemical synthesis
Thiazoles - chemistry
Thiazoles - pharmacokinetics
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.05.097