Bioorganic & Medicinal Chemistry Letters 2011-01-01

Benzoxazinones as potent positive allosteric AMPA receptor modulators: Part I

Rudolf Mueller, Yong-Xin Li, Aidan Hampson, Sheng Zhong, Clayton Harris, Christopher Marrs, Stanislaw Rachwal, Jolanta Ulas, Lena Nielsson, Gary Rogers, Rudolf Mueller, Yong-Xin Li, Aidan Hampson, Sheng Zhong, Clayton Harris, Christopher Marrs, Stanislaw Rachwal, Jolanta Ulas, Lena Nielsson, Gary Rogers

Index: Bioorg. Med. Chem. Lett. 21(13) , 3923-6, (2011)

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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.Copyright © 2011 Elsevier Ltd. All rights reserved.