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

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

  • Bioorg Med Chem Lett. 2011 Jun 1;21(11):3457-61. doi: 10.1016/j.bmcl.2011.03.096.
Maria Prat 1,  María Antonia Buil,  Maria Dolors Fernández,  Jordi Castro,  Juan Manuel Monleón,  Laia Tort,  Gaspar Casals,  Manuel Ferrer,  Josep Maria Huerta,  Sònia Espinosa,  Manuel López,  Victor Segarra,  Amadeu Gavaldà,  Montserrat Miralpeix,  Israel Ramos,  Dolors Vilella,  Marisa González,  Mònica Córdoba,  Alvaro Cárdenas,  Francisca Antón,  Jorge Beleta,  Hamish Ryder
Affiliations

Affiliation

  • 1 Almirall, R&D Centre, Laureà Miró 408-410, Sant Feliu de Llobregat, 08980 Barcelona, Spain. maria.prat@almirall.com
PMID: 21524581 DOI: 10.1016/j.bmcl.2011.03.096
Abstract

Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M(3) 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.

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