Literature DB >> 21636275

Benzoxazinones as potent positive allosteric AMPA receptor modulators: part I.

Rudolf Mueller1, Yong-Xin Li, Aidan Hampson, Sheng Zhong, Clayton Harris, Christopher Marrs, Stanislaw Rachwal, Jolanta Ulas, Lena Nielsson, Gary Rogers.   

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.

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Year:  2011        PMID: 21636275     DOI: 10.1016/j.bmcl.2011.05.026

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  AMPAKINE enhancement of social interaction in the BTBR mouse model of autism.

Authors:  J L Silverman; C F Oliver; M N Karras; P T Gastrell; J N Crawley
Journal:  Neuropharmacology       Date:  2012-07-16       Impact factor: 5.250

2.  ZnCl2-promoted domino reaction of 2-hydroxybenzonitriles with ketones for synthesis of 1,3-benzoxazin-4-ones.

Authors:  Ziqi Su; Hongxin Chai; Juan Xu; Jiarong Li
Journal:  RSC Adv       Date:  2021-09-06       Impact factor: 4.036

  2 in total

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