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Substituted benzoxazinones as potent positive allosteric AMPA receptor modulators: part II
Authors:Mueller Rudolf  Rachwal Stanislaw  Tedder Martina E  Li Yong-Xin  Zhong Sheng  Hampson Aidan  Ulas Jolanta  Varney Mark  Nielsson Lena  Rogers Gary
Institution:Cortex Pharmaceuticals Inc., 15231 Barranca Parkway, Irvine, CA 92618, USA
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.
Keywords:AMPA  Receptor  Modulator  Synthesis
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