Bioorganic & Medicinal Chemistry Letters 2011-01-01

Substituted benzoxazinones as potent positive allosteric AMPA receptor modulators: Part II

Rudolf Mueller, Stanislaw Rachwal, Martina E. Tedder, Yong-Xin Li, Sheng Zhong, Aidan Hampson, Jolanta Ulas, Mark Varney, Lena Nielsson, Gary Rogers, Rudolf Mueller, Stanislaw Rachwal, Martina E. Tedder, Yong-Xin Li, Sheng Zhong, Aidan Hampson, Jolanta Ulas, Mark Varney, Lena Nielsson, Gary Rogers

Index: Bioorg. Med. Chem. Lett. 21(13) , 3927-30, (2011)

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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.Copyright © 2011 Elsevier Ltd. All rights reserved.