Back to Search
Start Over
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Aug 01; Vol. 21 (15), pp. 4612-6. Date of Electronic Publication: 2011 Jun 13. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2011. Published by Elsevier Ltd.)
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21723724
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.05.097