|
|||||
|
|
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists |
|
| Authors: | Prat Maria Buil María Antonia Fernández Maria Dolors Castro Jordi Monleón Juan Manuel Tort Laia Casals Gaspar Ferrer Manuel Huerta Josep Maria Espinosa Sònia López Manuel Segarra Victor Gavaldà Amadeu Miralpeix Montserrat Ramos Israel Vilella Dolors González Marisa Córdoba Mònica Cárdenas Alvaro Antón Francisca Beleta Jorge Ryder Hamish |
| Institution: | a Almirall, R&D Centre, Laureà Miró 408-410, Sant Feliu de Llobregat, 08980 Barcelona, Spain b Thomson Reuters, Provenza 398, 08025 Barcelona, Spain c UCB Pharma S.A. , Avenue de l’Industrie, 1420 Braine-l’Alleud, Belgium d Laboratorios Lesvi, S.L., Avenida Barcelona 69, Sant Joan Despí, 08970 Barcelona, Spain e Cancer Research Technology Ltd., CRT Discovery Laboratories, 12 Rosemary Lane, Cambridge CB1 3LQ, UK |
| Abstract: | Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M3 muscarinic antagonists with long duration of action in an in vivo model of bronchoconstriction. These compounds have also presented a high level of metabolic transformation (human liver microsomes). The synthesis, structure-activity relationships and biological evaluation of these compounds are reported. |
| Keywords: | (3R)-Quinuclidinyl carbamates M3 Muscarinic antagonists Long acting bronchodilators Low systemic exposure COPD |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |