Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5481-6. doi: 10.1016/j.bmcl.2008.09.020. Epub 2008 Sep 10.

Abstract

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 M(3) over M(1). The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.

MeSH terms

  • Asthma / drug therapy
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Models, Chemical
  • Molecular Structure
  • Muscarinic Antagonists / chemical synthesis*
  • Muscarinic Antagonists / pharmacology
  • Receptors, Muscarinic / chemistry*
  • Salts / chemistry
  • Structure-Activity Relationship
  • Tyrosine / chemistry*
  • Urea / chemistry*

Substances

  • Muscarinic Antagonists
  • Receptors, Muscarinic
  • Salts
  • Tyrosine
  • Urea