2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3540-4. doi: 10.1016/j.bmcl.2010.04.128. Epub 2010 May 17.

Abstract

Biaryl amides were discovered as novel and subtype selective M(1) muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M(1) agonist potency and intrinsic activity, and subtype selectivity for M(1) over M(2-5), are described.

MeSH terms

  • Amides / chemical synthesis*
  • Amides / pharmacology
  • Drug Discovery
  • Hydrocarbons, Aromatic / chemical synthesis*
  • Hydrocarbons, Aromatic / pharmacology
  • Molecular Structure
  • Receptor, Muscarinic M1 / agonists*
  • Structure-Activity Relationship

Substances

  • Amides
  • Hydrocarbons, Aromatic
  • Receptor, Muscarinic M1