The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea group
| Autor: | Brian Edgar Looker, Victoria J. Barrett, Gillian Elizabeth Lunniss, Alison J. Ford, Claire E. Smith, Deborah Needham, Panayiotis A. Procopiou, Graham Somers |
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| Rok vydání: | 2011 |
| Předmět: |
medicine.medical_specialty
Adrenergic receptor Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Guinea pig chemistry.chemical_compound In vivo Internal medicine Drug Discovery medicine Molecular Biology Organic Chemistry respiratory system In vitro respiratory tract diseases Bioavailability Endocrinology chemistry Urea Microsome Molecular Medicine Salmeterol hormones hormone substitutes and hormone antagonists medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 19:6026-6032 |
| ISSN: | 0968-0896 |
| Popis: | A series of novel, potent and selective human β(2) adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of (R)-salmeterol is presented. Urea 9j had long duration of action in vitro on guinea pig trachea, and also in vivo similar to that of salmeterol. It had lower oral absorption and bioavailability than salmeterol in both rat and dog. It had a turnover ratio similar to salmeterol, with no evidence for formation of any aniline metabolites in human liver microsomes and hepatocytes. However no crystalline salts suitable for inhaled delivery were identified. |
| Databáze: | OpenAIRE |
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