In Vitro SAR of Pyrrolidine-Containing Histamine H3 Receptor Antagonists: Trends Across Multiple Chemical Series

Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. doi: 10.1016/j.bmcl.2007.10.067. Epub 2007 Oct 24.


Structure-activity relationships (SAR) were analyzed within a library of diverse yet simple compounds prepared as histamine H3 antagonists. The libraries were constructed with a variety of low molecular weight pyrrolidines, selected from (R)-2-methylpyrrolidine, (S)-2-methylpyrrolidine, and pyrrolidine.

MeSH terms

  • Animals
  • Histamine H3 Antagonists / chemistry*
  • Histamine H3 Antagonists / pharmacology*
  • Humans
  • Kinetics
  • Pyrrolidines / chemistry*
  • Pyrrolidines / pharmacology*
  • Rats
  • Structure-Activity Relationship


  • 2-methylpyrrolidine
  • Histamine H3 Antagonists
  • Pyrrolidines