Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

Abstract

Arylpiperzine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated as novel antidepressant compounds. The various analogues were efficiently prepared and bio-assayed for binding to 5-HT(2A), 5-HT(2C) receptor, and 5-HT transporter. Based on their in vitro and in vivo activities as well as selectivity over other neurotransmitter receptors and PK profiles, 33 and 34 were identified as lead compounds. Consequently, this pyrrole series of compounds appears to be promising enough to warrant further investigation.

DOI: 10.1016/j.bmcl.2010.01.093

Cite this paper

@article{Kang2010ArylpiperazinecontainingP3, title={Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.}, author={Suk Youn Kang and Eun-Jung Park and Woo-Kyu Park and Hyun Jung Kim and Daeyoung Jeong and Myung Eun Jung and Kwang-Seop Song and Suk Ho Lee and Hee Jeong Seo and Min Ju Kim and Minwoo Lee and Ho-Kyun Han and Eun-Jung Son and Ae Nim Pae and Jeongmin Kim and Jinhwa Lee}, journal={Bioorganic & medicinal chemistry letters}, year={2010}, volume={20 5}, pages={1705-11} }