Literature DB >> 32599366

Design, synthesis and anticonvulsant activity of new imidazolidindione and imidazole derivatives.

Adel A Marzouk1, Amr K A Bass2, Montaser Sh Ahmed3, Antar A Abdelhamid4, Yaseen A M M Elshaier5, Asmaa M M Salman6, Omar M Aly7.   

Abstract

New imidazolidindiones and tetra-substituted imidazole derivatives were designed, synthesized, and evaluated for the anticonvulsant activity through pentylenetetrazole (PTZ)-induced seizures and maximal electroshock (MES) tests using valproate sodium and phenytoin sodium as reference drugs, respectively. Most of the target compounds showed excellent activity against pentylenetetrazole (PTZ)-induced seizures with fair to no-activity against MES. Compounds 3d, 4e, 11b, and 11e showed higher activity (120%) than that of valproate sodium in PTZ model. Almost all compounds showed no neurotoxicity, as indicated by the rotarod test. Estimation of physicochemical properties and pharmacokinetic profiles of the target compounds were studied. The chemical structures of the target compounds were characterized by different spectrometric methods and elemental analysis.
Copyright © 2020 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Anticonvulsant activity; Imidazoles; Imidazolidinediones; Neurotoxicity; Shape similarity; Spiro[fluorene-9,4ʹ-imidazolidine]

Year:  2020        PMID: 32599366     DOI: 10.1016/j.bioorg.2020.104020

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  3 in total

1.  Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors.

Authors:  Lamya H Al-Wahaibi; Amer A Amer; Adel A Marzouk; Hesham A M Gomaa; Bahaa G M Youssif; Antar A Abdelhamid
Journal:  Pharmaceuticals (Basel)       Date:  2021-04-22

2.  Pyromellitic diamide-diacid bridged mesoporous organosilica nanospheres with controllable morphologies: a novel PMO for the facile and expeditious synthesis of imidazole derivatives.

Authors:  Ehsan Valiey; Mohammad G Dekamin
Journal:  Nanoscale Adv       Date:  2021-11-04

Review 3.  Animal Models of Epilepsy: A Phenotype-oriented Review.

Authors:  Yilin Wang; Penghu Wei; Feng Yan; Yumin Luo; Guoguang Zhao
Journal:  Aging Dis       Date:  2022-02-01       Impact factor: 6.745

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.