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Bioorg Med Chem Lett. 2011 Jul 1;21(13):3927-30. doi: 10.1016/j.bmcl.2011.05.024. Epub 2011 May 14.

Substituted benzoxazinones as potent positive allosteric AMPA receptor modulators: part II.

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1
Cortex Pharmaceuticals Inc., 15231 Barranca Parkway, Irvine, CA 92618, USA. rudolfmueller@yahoo.com

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.

PMID:
21636273
DOI:
10.1016/j.bmcl.2011.05.024
[Indexed for MEDLINE]
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