Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists
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.
Prat, Maria,Buil, María Antonia,Fernández, Maria Dolors,Castro, Jordi,Monleón, Juan Manuel,Tort, Laia,Casals, Gaspar,Ferrer, Manuel,Huerta, Josep Maria,Espinosa, Snia,López, Manuel,Segarra, Victor,Gavald, Amadeu,Miralpeix, Montserrat,Ramos, Israel,Vilella, Dolors,González, Marisa,Córdoba, Mnica,Cárdenas, Alvaro,Antón, Francisca,Beleta, Jorge,Ryder, Hamish
p. 3457 - 3461
(2011/06/24)
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