title: Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.
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.
authors.affiliation: Medicinal Chemistry Research Center, Bio-Organic Division, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon, South Korea. parkcm@krict.re.kr
authors.forename: Chul Min
authors.initials: CM
authors.lastname: Park
authors.forename: So Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Woo Kyu
authors.initials: WK
authors.lastname: Park
authors.forename: Jung Hwan
authors.initials: JH
authors.lastname: Choi
authors.forename: Churl Min
authors.initials: CM
authors.lastname: Seong
mesh_terms: D014150:Antipsychotic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry; D011985:Receptors, Serotonin / Q000145:classification / Q000187:drug effects; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D014150:Antipsychotic Agents; D010879:Piperazines; D011985:Receptors, Serotonin; D013449:Sulfonamides