Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.

@article{Shao2011SynthesisAP,
  title={Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.},
  author={L. Shao and M. Hewitt and S. Malcolm and Fengjiang Wang and J. Ma and U. Campbell and Nancy A Spicer and S. Engel and L. Hardy and Zhi-Dong Jiang and R. Schreiber and K. Spear and M. Varney},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 15},
  pages={
          5283-95
        }
}
The present work expands the chemical space known to offer potent inhibition of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) and discloses novel bicyclic octahydrocyclopenta[c]pyrrole and octahydro-1H-isoindole scaffolds as potent triple reuptake inhibitors (TRIs) for the potential treatment of depression. Optimized compounds 22a (SERT, NET, DAT, IC(50) = 20, 109, 430 nM), 23a (SERT, NET, DAT, IC(50) = 29, 85, 168 nM), and 26a (SERT, NET… Expand
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