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 12-580nM. 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.
Yoon
Juhee
J
School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
Yoo
Eun A
EA
Kim
Ji-Yeon
JY
Pae
Ae Nim
AN
Rhim
Hyewhon
H
Park
Woo-Kyu
WK
Kong
Jae Yang
JY
Park Choo
Hea-Young
HY
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008968:Molecular Conformation; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000187:drug effects*; D011994:Recombinant Proteins / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D010879:Piperazines; D011985:Receptors, Serotonin; D011994:Recombinant Proteins; C104425:serotonin 7 receptor