Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5221-4. doi: 10.1016/j.bmcl.2010.06.150. Epub 2010 Jul 23.

Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.

Author information

1
Medicinal Chemistry Research Center, Bio-Organic Division, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon, South Korea. parkcm@krict.re.kr

Abstract

(Piperazin-1-yl-phenyl)-arylsulfonamides were synthesized and identified to show high affinities for both 5-HT(2C) and 5-HT(6) receptors. Among them, naphthalene-2-sulfonic acid isopropyl-[3-(4-methyl-piperazin-1-yl)-phenyl]-amide (6b) exhibits the highest affinity towards both 5-HT(2C) (IC(50)=4 nM) and 5-HT(6) receptors (IC(50)=3 nM) with good selectivity over other serotonin (5-HT(1A), 5-HT(2A), and 5-HT(7)) and dopamine (D(2)-D(4)) receptor subtypes. In 5-HT(2C) and 5-HT(6) receptor functional assays, this compound showed considerable antagonistic activity for both receptors.

PMID:
20655748
DOI:
10.1016/j.bmcl.2010.06.150
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center