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

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.

SAR around R1, R2 and R3 are reported.Figure optionsDownload as PowerPoint slide