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

2011; Elsevier BV; Volume: 21; Issue: 11 Linguagem: Inglês

10.1016/j.bmcl.2011.03.096

1464-3405

María Prat, María Antonia Buil, Maria Dolors Fernández, Jordi Castro, Juan Manuel Monleón, Laia Tort, Gaspar Casals, Manuel Ferrer, José María Huerta, Sònia Espinosa, Manuel López, Vı́ctor Segarra, Amadeu Gavaldà, Montserrat Miralpeix, Israel Ramos, Dolors Vilella, Marisa González, Mònica Córdoba, Á. de Pablo Cárdenas, Francisca Antón, Jörge Beleta, Hamish Ryder,

Respiratory and Cough-Related Research

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.