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Discovery of Diaryl Imidazolidin-2-one Derivatives, a Novel Class of Muscarinic M3 Selective Antagonists (Part 2)

2007; American Chemical Society; Volume: 50; Issue: 7 Linguagem: Inglês

10.1021/jm061160+

1520-4804

Ilaria Peretto, Claudia Fossati, Giuseppe Giardina, Alessandra Giardini, Matilde Guala, Elena La Porta, Paola Petrillo, Stefano Radaelli, Luigi Radice, Luca F. Raveglia, Enza Santoro, Roberta Scudellaro, Francesca Scarpitta, Alberto Cerri, Sergio Menegon, Giulio Dondio, Andrea Rizzi, Elisabetta Armani, Gabriele Amari, Maurizio Civelli, Gino Villetti, Riccardo Patacchini, M. A. C. M. Bergamaschi, Franco Bassani, Maurizio Delcanale, Bruno P. Imbimbo,

Neuropeptides and Animal Physiology

Synthesis and biological activity of a novel class of quaternary ammonium salt muscarinic M3 receptor antagonists, showing high selectivity versus the M2 receptor, are described. Selected compounds exhibited potent anticholinergic properties, in isolated guinea-pig trachea, and good functional selectivity for trachea over atria. In vivo, the same compounds potently inhibited acetylcholine-induced bronchoconstriction after intratracheal administration in the guinea pig.