title: Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators.
abstract: AMPA receptors (AMPARs) have been demonstrated to be an important therapeutic CNS target. A series of substituted benzotriazinone and benzopyrimidinone derivatives were prepared with the aim to improve in vivo activity over the previously reported bis-benzoxazinone based AMPAKINE series from our laboratory. These compounds were shown to be potent, positive allosteric AMPAR modulators that have better in vivo activity and improved metabolic stability over the analogous benzoxazinone derivatives.
authors: Cortex Pharmaceuticals Inc., 15231 Barranca Parkway, Irvine, CA 92618, USA. rudolfmueller@yahoo.com
authors: Rudolf
authors: R
authors: Mueller
authors: Stanislaw
authors: S
authors: Rachwal
authors: Steven
authors: S
authors: Lee
authors: Sheng
authors: S
authors: Zhong
authors: Yong-Xin
authors: YX
authors: Li
authors: Peter
authors: P
authors: Haroldsen
authors: Todd
authors: T
authors: Herbst
authors: Susan
authors: S
authors: Tanimura
authors: Mark
authors: M
authors: Varney
authors: Steven
authors: S
authors: Johnson
authors: Gary
authors: G
authors: Rogers
authors: Leslie J
authors: LJ
authors: Street
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D015195:Drug Design; D006624:Hippocampus / Q000187:drug effects; D006801:Humans; D011744:Pyrimidinones / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D018091:Receptors, AMPA / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D011744:Pyrimidinones; D018091:Receptors, AMPA; D014227:Triazines