title: The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
abstract: Antagonists of the 5-HT(6) receptor have been shown to improve cognitive function in a wide range of animal models and as such may prove to be attractive agents for the symptomatic treatment of cognitive disorders such as Alzheimer's disease (AD) and schizophrenia. We report herein the identification and SAR around N-(2-aminoalkyl)-1-(arylsulfonyl)indoline-3-carboxamides-a novel chemotype of 5-HT(6) antagonists.
authors.affiliation: Department of Chemistry, Schering-Plough Research Institute, Newhouse, Lanarkshire, UK. mark.reid@spcorp.com
authors.forename: Mark
authors.initials: M
authors.lastname: Reid
authors.forename: Ian
authors.initials: I
authors.lastname: Carlyle
authors.forename: Wilson L
authors.initials: WL
authors.lastname: Caulfield
authors.forename: Tom R
authors.initials: TR
authors.lastname: Clarkson
authors.forename: Fiona
authors.initials: F
authors.lastname: Cusick
authors.forename: Ola
authors.initials: O
authors.lastname: Epemolu
authors.forename: Robert
authors.initials: R
authors.lastname: Gilfillan
authors.forename: Richard
authors.initials: R
authors.lastname: Goodwin
authors.forename: David
authors.initials: D
authors.lastname: Jaap
authors.forename: Elise C
authors.initials: EC
authors.lastname: O'Donnell
authors.forename: Jeremy
authors.initials: J
authors.lastname: Presland
authors.forename: Zoran
authors.initials: Z
authors.lastname: Rankovic
authors.forename: Daniel
authors.initials: D
authors.lastname: Spinks
authors.forename: Gayle
authors.initials: G
authors.lastname: Spinks
authors.forename: Anne M
authors.initials: AM
authors.lastname: Thomson
authors.forename: Fiona
authors.initials: F
authors.lastname: Thomson
authors.forename: James
authors.initials: J
authors.lastname: Strain
authors.forename: Grant
authors.initials: G
authors.lastname: Wishart
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D001682:Biological Availability; D055808:Drug Discovery; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D008861:Microsomes; D010599:Pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000187:drug effects*; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D007211:Indoles; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; C097216:serotonin 6 receptor; C057812:indoline