Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors

The design, synthesis and in vitro assay evaluation of a novel series of 3,4-diarylpyrrolidin-2-one is described as a triple reuptake inhibitor. Most of compounds showed good efficacy as a dopamine transporter inhibitors and norepinephrine transporter inhibitors. The compounds 2a, and 2b with comparable activities in binding and reuptake inhibition were obtained for further optimization as an antidepressant.