title: 1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.
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.
authors.affiliation: 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
authors.forename: Chul Min
authors.initials: CM
authors.lastname: Park
authors.forename: Jin Il
authors.initials: JI
authors.lastname: Choi
authors.forename: Jung Hwan
authors.initials: JH
authors.lastname: Choi
authors.forename: So Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Woo Kyu
authors.initials: WK
authors.lastname: Park
authors.forename: Churl Min
authors.initials: CM
authors.lastname: Seong
mesh_terms: D000818:Animals; D002460:Cell Line; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D011485:Protein Binding; D015363:Quinolones / Q000737:chemistry* / Q000494:pharmacology*; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D015363:Quinolones; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C097216:serotonin 6 receptor