Preparation of piperazine derivatives as 5-HT7 receptor antagonists.

Abstract:

: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.

journal_name

Bioorg Med Chem

authors

Yoon J,Yoo EA,Kim JY,Pae AN,Rhim H,Park WK,Kong JY,Park Choo HY

doi

10.1016/j.bmc.2008.04.023

subject

Has Abstract

pub_date

2008-05-15 00:00:00

pages

5405-12

issue

10

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00351-9

journal_volume

16

pub_type

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