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Bioorg Med Chem Lett. 2011 Oct 15;21(20):6170-5. doi: 10.1016/j.bmcl.2011.07.098. Epub 2011 Aug 12.

Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators.

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

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.

PMID:
21889339
DOI:
10.1016/j.bmcl.2011.07.098
[Indexed for MEDLINE]
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