Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
- Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
- 강석연; 박은정; 박우규; 김현정; 정대영; 정명은; 송광섭; 이석호; 서희정; 김민주; 이민우; 한호견; 손은정; 배애님; 김정민; 이진화
- Depression; Antidepressant; Serotonin; Piperazine; Pyrrole
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 20, NO 5, 1705-1711
- 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-HT2A, 5-HT2C 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
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