title: Benzoxazinones as potent positive allosteric AMPA receptor modulators: part I.
abstract: AMPA receptors (AMPARs) are an increasingly important therapeutic target in the CNS. Aniracetam, the first identified potentiator of AMPARs, led to the rigid and more potent CX614. This lead molecule was optimized in order to increase affinity towards the AMPA receptor. The substitution of the dioxine with a benzoxazinone ring system increased the activity and allowed further investigation of the sidechain SAR.
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: Yong-Xin
authors.initials: YX
authors.lastname: Li
authors.forename: Aidan
authors.initials: A
authors.lastname: Hampson
authors.forename: Sheng
authors.initials: S
authors.lastname: Zhong
authors.forename: Clayton
authors.initials: C
authors.lastname: Harris
authors.forename: Christopher
authors.initials: C
authors.lastname: Marrs
authors.forename: Stanislaw
authors.initials: S
authors.lastname: Rachwal
authors.forename: Jolanta
authors.initials: J
authors.lastname: Ulas
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; D018697:Nootropic Agents / Q000494:pharmacology; D016548:Prosencephalon / Q000187:drug effects; D011760:Pyrrolidinones / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D018091:Receptors, AMPA / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D048588:Benzoxazines; D018697:Nootropic Agents; D011760:Pyrrolidinones; D018091:Receptors, AMPA; C036466:aniracetam