2. Academic Validation
  3. Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists

Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists

  • Bioorg Med Chem Lett. 2015 Apr 15;25(8):1736-1741. doi: 10.1016/j.bmcl.2015.02.065.
Maria Prat 1,  María Antonia Buil 2,  Maria Dolors Fernández 3,  Laia Tort 2,  Juan Manuel Monleón 2,  Gaspar Casals 2,  Manuel Ferrer 2,  Jordi Castro 2,  Amadeu Gavaldà 2,  Montserrat Miralpeix 2,  Israel Ramos 2,  Dolors Vilella 2,  Josep Maria Huerta 2,  Sònia Espinosa 2,  Begoña Hernández 2,  Victor Segarra 2,  Mònica Córdoba 2
Affiliations

Affiliations

  • 1 Almirall, R&D Centre, Laureà Miró 408-410, Sant Feliu de Llobregat, 08980 Barcelona, Spain. Electronic address: maria.prat@almirall.com.
  • 2 Almirall, R&D Centre, Laureà Miró 408-410, Sant Feliu de Llobregat, 08980 Barcelona, Spain.
  • 3 Thomson Reuters, Provenza 398, 08025 Barcelona, Spain.
PMID: 25800115 DOI: 10.1016/j.bmcl.2015.02.065
Abstract

Novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides have been identified as potent M3 muscarinic antagonists with a long duration of action in an in vivo model of bronchoconstriction. The synthesis, structure-activity relationships and biological evaluation of this series of compounds are reported.

Keywords

(3R)-Quinuclidinyl amides; COPD; Long acting bronchodilators; Low systemic exposure; M(3) muscarinic antagonists.

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