title: Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
abstract: 5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT(6) receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC(50) values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, New York 10965, USA. coledc@wyeth.com
authors.forename: Derek C
authors.initials: DC
authors.lastname: Cole
authors.forename: William J
authors.initials: WJ
authors.lastname: Lennox
authors.forename: Sabrina
authors.initials: S
authors.lastname: Lombardi
authors.forename: John W
authors.initials: JW
authors.lastname: Ellingboe
authors.forename: Ronald C
authors.initials: RC
authors.lastname: Bernotas
authors.forename: Gregory J
authors.initials: GJ
authors.lastname: Tawa
authors.forename: Hossein
authors.initials: H
authors.lastname: Mazandarani
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Guoming
authors.initials: G
authors.lastname: Zhang
authors.forename: Joseph
authors.initials: J
authors.lastname: Coupet
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
mesh_terms: D000242:Cyclic AMP / Q000819:agonists / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007211:Indoles; D011759:Pyrrolidines; D011985:Receptors, Serotonin; D013449:Sulfonamides; C097216:serotonin 6 receptor; D000242:Cyclic AMP