title: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.
abstract: A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.
authors.affiliation: Roche Pharmaceuticals, Medicinal Chemistry, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. shu-hai.zhao@roche.com
authors.forename: Shu-Hai
authors.initials: SH
authors.lastname: Zhao
authors.forename: Jacob
authors.initials: J
authors.lastname: Berger
authors.forename: Robin D
authors.initials: RD
authors.lastname: Clark
authors.forename: Steven G
authors.initials: SG
authors.lastname: Sethofer
authors.forename: Nancy E
authors.initials: NE
authors.lastname: Krauss
authors.forename: Julie M
authors.initials: JM
authors.lastname: Brothers
authors.forename: Renee S
authors.initials: RS
authors.lastname: Martin
authors.forename: Dinah L
authors.initials: DL
authors.lastname: Misner
authors.forename: Dietmar
authors.initials: D
authors.lastname: Schwab
authors.forename: Ludmila
authors.initials: L
authors.lastname: Alexandrova
mesh_terms: D000818:Animals; D008956:Models, Chemical; D010078:Oxazines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C522193:3,4-dihydro-2H-benzo(1,4)oxazine; D010078:Oxazines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C097216:serotonin 6 receptor