title: N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
abstract: A series of N(1)-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)indole derivatives was designed and synthesized. These compounds were shown to have high affinity for the 5-HT(6) receptor. Two analogs, 4-[3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-1-sulfonyl]-phenylamine 15g and 4-[3-(1,2,3,6-tetrahydropyridin-4-yl)-5-methoxy-1H-indole-1-sulfonyl]-phenylamine 15y, had 0.4 and 3.0 nM affinity, respectively, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. coledc@wyeth.com
authors.forename: Derek C
authors.initials: DC
authors.lastname: Cole
authors.forename: John W
authors.initials: JW
authors.lastname: Ellingboe
authors.forename: William J
authors.initials: WJ
authors.lastname: Lennox
authors.forename: Hossein
authors.initials: H
authors.lastname: Mazandarani
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Joseph R
authors.initials: JR
authors.lastname: Stock
authors.forename: Guoming
authors.initials: G
authors.lastname: Zhang
authors.forename: Ping
authors.initials: P
authors.lastname: Zhou
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C097216:serotonin 6 receptor; D000262:Adenylyl Cyclases