Preparation of piperazine derivatives as 5-HT7 receptor antagonists

Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] benzene sulfonamides and N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT(7) receptor antagonists. Most of the compounds showed the IC(50) values of 12-58...

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Published in:Bioorganic & medicinal chemistry 2008-05, Vol.16 (10), p.5405-5412
Main Authors: JUHEE YOON, YOO, Eun A, KIM, Ji-Yeon, AE NIM PAE, RHIM, Hyewhon, PARK, Woo-Kyu, JAE YANG KONG, HEA-YOUNG PARK CHOO
Format: Article
Language:English
Subjects:
Animals
Binding Sites - drug effects
Biological and medical sciences
CHO Cells
Cricetinae
Cricetulus
Drug Evaluation, Preclinical
Humans
Medical sciences
Molecular Conformation
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacology
Radioligand Assay
Receptors, Serotonin - drug effects
Recombinant Proteins - drug effects
Serotoninergic system
Stereoisomerism
Structure-Activity Relationship
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Summary:Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] benzene sulfonamides and N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT(7) receptor antagonists. Most of the compounds showed the IC(50) values of 12-580nM. Four methyl branched analogues were also obtained, but the activity for methyl branched analogues was almost same as its straight chain congeners. Among the synthesized compounds, 3c showed a good activity on 5-HT(7) receptors and a good selectivity on 5-HT(1a), 5-HT(2a), 5-HT(2c), and 5-HT(6) receptors.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2008.04.023