Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas

Jian Jin, Yonghui Wang, Dongchuan Shi, Feng Wang, Wei Fu, Roderick S. Davis, Qi Jin, James J. Foley, Henry M. Sarau, Dwight M. Morrow, Michael L. Moore, Ralph A. Rivero, Michael Palovich, Michael Salmon, Kristen E. Belmonte, Jakob Busch-Petersen

Research output: Contribution to journalArticlepeer-review

4 Scopus citations


SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M3 over M1. The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.

Original languageEnglish
Pages (from-to)5481-5486
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
StatePublished - 15 Oct 2008
Externally publishedYes


  • Asthma
  • COPD
  • M3 mAChR
  • Muscarinic acetylcholine receptor antagonists
  • SAR
  • Subtype selectivity
  • Tyrosine ureas


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