1. Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
- Author
-
Connolly S, Alcaraz L, Bailey A, Cadogan E, Christie J, Cook AR, Fisher AJ, Hill S, Humphries A, Ingall AH, Kane Z, Paine S, Pairaudeau G, Stocks MJ, and Young A
- Subjects
- Adrenergic beta-2 Receptor Agonists chemical synthesis, Adrenergic beta-2 Receptor Agonists pharmacokinetics, Animals, Bronchodilator Agents chemical synthesis, Bronchodilator Agents pharmacokinetics, Drug Design, Drug Evaluation, Preclinical, Guinea Pigs, Receptors, Adrenergic, beta-2 metabolism, Structure-Activity Relationship, Thiazoles chemical synthesis, Thiazoles pharmacokinetics, Adrenergic beta-2 Receptor Agonists chemistry, Bronchodilator Agents chemistry, Receptors, Adrenergic, beta-2 chemistry, Thiazoles chemistry
- 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., (Copyright © 2011. Published by Elsevier Ltd.)
- Published
- 2011
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