title: Substituted benzoxazinones as potent positive allosteric AMPA receptor modulators: part II.
abstract: AMPA receptors (AMPARs) are an important therapeutic target in the CNS. A series of substituted benzoxazinone derivatives with good to very good in vitro activity as positive allosteric AMPAR modulators was synthesized and evaluated. The appropriate substituent choice on the benzoxazinone fragment improved the affinity towards the AMPA receptor significantly in comparison to our lead molecule CX614.
authors.affiliation: Cortex Pharmaceuticals Inc., 15231 Barranca Parkway, Irvine, CA 92618, USA. rudolfmueller@yahoo.com
authors.forename: Rudolf
authors.initials: R
authors.lastname: Mueller
authors.forename: Stanislaw
authors.initials: S
authors.lastname: Rachwal
authors.forename: Martina E
authors.initials: ME
authors.lastname: Tedder
authors.forename: Yong-Xin
authors.initials: YX
authors.lastname: Li
authors.forename: Sheng
authors.initials: S
authors.lastname: Zhong
authors.forename: Aidan
authors.initials: A
authors.lastname: Hampson
authors.forename: Jolanta
authors.initials: J
authors.lastname: Ulas
authors.forename: Mark
authors.initials: M
authors.lastname: Varney
authors.forename: Lena
authors.initials: L
authors.lastname: Nielsson
authors.forename: Gary
authors.initials: G
authors.lastname: Rogers
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D048588:Benzoxazines / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D016548:Prosencephalon / Q000187:drug effects; D011760:Pyrrolidinones / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D018091:Receptors, AMPA / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D048588:Benzoxazines; D011760:Pyrrolidinones; D018091:Receptors, AMPA; C036466:aniracetam