title: Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.
abstract: As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT(6) antagonists. The synthesis and detailed SAR of this class of compounds are reported.
authors.affiliation: Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA. liuk@lundbeck.com
authors.forename: Kevin G
authors.initials: KG
authors.lastname: Liu
authors.forename: Albert J
authors.initials: AJ
authors.lastname: Robichaud
authors.forename: Alexander A
authors.initials: AA
authors.lastname: Greenfield
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Lo
authors.forename: Cristina
authors.initials: C
authors.lastname: Grosanu
authors.forename: James F
authors.initials: JF
authors.lastname: Mattes
authors.forename: Yanxuan
authors.initials: Y
authors.lastname: Cai
authors.forename: Guo Ming
authors.initials: GM
authors.lastname: Zhang
authors.forename: Jean Y
authors.initials: JY
authors.lastname: Zhang
authors.forename: Dianne M
authors.initials: DM
authors.lastname: Kowal
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Li
authors.initials: L
authors.lastname: Di
authors.forename: Edward H
authors.initials: EH
authors.lastname: Kerns
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Comery
mesh_terms: D006367:HeLa Cells; D006801:Humans; D007191:Indazoles / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D018697:Nootropic Agents / Q000737:chemistry / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000737:chemistry / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship
chemical_list: D007191:Indazoles; D018697:Nootropic Agents; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C097216:serotonin 6 receptor