Toward developing safer pharmacotherapeutics for eating disorders, obesity or addiction, a series of rigid amine-containing chiral pyrrolidinones   have been developed   as CB1 receptor ligands. To explore the synthetic landscape at C3, rigid amines 1-aminoindane (n=1)   and tetrahydro-1-naphthylamine (n=2) have been appended. These novel compounds have shown excellent CB1 selectivity and affinity (1-30 nm). Ligands will be evaluated in vitro and in vivo as CB1-selective inverse agonists or neutral antagonists. The synthetic scheme, stereoisomer characterization and assay results will be discussed. 

Rigid amine-containing pyrrolidinones as CB<sub>1</sub> antagonists

243rd National Meeting (2012)

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Rigid amine-containing pyrrolidinones as CB1 antagonists

Rigid amine-containing pyrrolidinones as CB₁ antagonists