In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: Trends across multiple chemical series

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.

The SAR of a 60-compound library of H3 antagonists comprising 20 different core moieties each incorporating pyrrolidine, (R)-2-methylpyrrolidine, and (S)-2-methylpyrrolidine is discussed.Figure optionsDownload as PowerPoint slide