Literature DB >> 21195615

Imidazolylchromanone oxime ethers as potential anticonvulsant agents: Anticonvulsive evaluation in PTZ-kindling model of epilepsy and SAR study.

Saeed Emami1, Abbas Kebriaeezadeh, Nematollah Ahangar, Reza Khorasani.   

Abstract

As a continuation of our efforts to develop the azolylchromanone derivatives as potential anticonvulsant agents, we explored (Z)- and (E)-oxime ether derivatives of imidazolylchromanones bearing different lipophilic O-benzyl groups and tested their anticonvulsant activities in PTZ-kindling model of epilepsy. O-(2,4-Dichlorobenzyl) oximes 8a, 16a and 20a were significantly effective in delaying the onset of the PTZ-evoked seizures at the dose of 30mg/kg in kindled animals. The most effective compounds in delaying seizures were 7-chlorochromanone-O-(2,4-dichlorobenzyl) oximes 8a and 20a. SAR studies showed that introduction of a chlorine atom to the 7-position and/or a methyl group to the 2-position of the chroman ring resulted in an improvement of anti-seizure efficacy in O-(2,4-dichlorobenzyl) oxime series. Copyright Â
© 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 21195615     DOI: 10.1016/j.bmcl.2010.12.021

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


  2 in total

1.  Pentylenetetrazole-Induced Kindling Mouse Model.

Authors:  Tadayuki Shimada; Kanato Yamagata
Journal:  J Vis Exp       Date:  2018-06-12       Impact factor: 1.355

Review 2.  Chromanone-A Prerogative Therapeutic Scaffold: An Overview.

Authors:  Sonia Kamboj; Randhir Singh
Journal:  Arab J Sci Eng       Date:  2021-06-30       Impact factor: 2.807

  2 in total

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