1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands

Chul Min Park; Jin Il Choi; Jung Hwan Choi; So Young Kim; Woo Kyu Park; Churl Min Seong

doi:10.1016/j.bmcl.2010.12.007

1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands

Bioorg Med Chem Lett. 2011 Jan 15;21(2):698-703. doi: 10.1016/j.bmcl.2010.12.007. Epub 2010 Dec 8.

Authors

Chul Min Park¹, Jin Il Choi, Jung Hwan Choi, So Young Kim, Woo Kyu Park, Churl Min Seong

Affiliation

¹ Medicinal Chemistry Research Center, Bio-Organic Division, Korea Research Institute of Chemical Technology, Sinseongno 19, Yuseong-gu, Daejeon 305-600, South Korea. parkcm@krict.re.kr

PMID: 21190848
DOI: 10.1016/j.bmcl.2010.12.007

Abstract

Piperazinyl derivatives of 1-(arylsulfonyl)-2,3-dihydro-1H-quinolin-4-ones have been identified with high binding affinities for 5-HT(6) receptor. In particular, 2-methyl-5-(N-methyl-piperazin-1-yl)-1-(naphthalene-2-sulfonyl)-2,3-dihydro-1H-quinolin-4-one (8g) exhibits high binding affinity toward 5-HT(6) (IC(50)=8nM) receptor with good selectivity over other serotonin and dopamine receptors.

MeSH terms

Animals
Cell Line
Humans
Ligands
Models, Molecular
Protein Binding
Quinolones / chemistry*
Quinolones / pharmacology*
Receptors, Serotonin / metabolism*
Serotonin Antagonists / chemistry*
Serotonin Antagonists / pharmacology*
Structure-Activity Relationship

Substances

Ligands
Quinolones
Receptors, Serotonin
Serotonin Antagonists
serotonin 6 receptor