Discovery of novel and long acting muscarinic acetylcholine receptor antagonists

Jian Jin, Yonghui Wang, Dongchuan Shi, Feng Wang, Roderick S. Davis, Qi Jin, Wei Fu, James J. Foley, Edward F. Webb, Chris J. Dehaas, Manuela Berlanga, Miriam Burman, Henry M. Sarau, Dwight M. Morrow, Parvathi Rao, Lorena A. Kallal, Michael L. Moore, Ralph A. Rivero, Michael Palovich, Michael SalmonKristen E. Belmonte, Jakob Busch-Petersen

Research output: Contribution to journalArticlepeer-review

17 Scopus citations


High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.

Original languageEnglish
Pages (from-to)4866-4869
Number of pages4
JournalJournal of Medicinal Chemistry
Issue number16
StatePublished - 28 Aug 2008
Externally publishedYes


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