Literature DB >> 25466174

Microwave assisted synthesis and docking study of N-(2-oxo-2-(4-oxo-2-substituted thiazolidin-3ylamino)ethyl)benzamide derivatives as anticonvulsant agents.

Anna Pratima G Nikalje1, Arfat N Shaikh2, Sameer I Shaikh2, Firoz A Kalam Khan2, Jaiprakash N Sangshetti2, Devanand B Shinde3.   

Abstract

Herewith, we report the design and synthesis of a series of N-(2-oxo-2((4-oxo-2-substituted thiazolidin-3yl)amino)ethyl) benzamide derivatives 7(a-j) under microwave irradiation, based on four component pharmacophoric model to get structural prerequisite indispensable for anticonvulsant activity. The synthesized derivatives were investigated in maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening. All the test compounds were administered at a dose of 30, 100 and 300 mg/kg body weight at the time interval of 0.5 h and 4 h. The compounds were also evaluated for behavioral activity and toxicity study. The compound 7 h was found to be most active in MES model. The anticonvulsant screening data shows that 65% of the compounds were found active against MES model when compared to 35% sc-PTZ model. The computational parameter such as docking study, logP determination and ADME prediction were performed to exploit the results.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anticonvulsant evaluation; Benzamide; Computational studies; Microwave irradiation; Thiazolidinone

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Year:  2014        PMID: 25466174     DOI: 10.1016/j.bmcl.2014.11.016

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


  2 in total

1.  Synthesis and biological evaluation of benzothiazin-4-ones: a possible new class of acetylcholinesterase inhibitors.

Authors:  Gabriele A Berwaldt; Daniela P Gouvêa; Daniel S da Silva; Adriana M das Neves; Mayara S P Soares; Juliana H Azambuja; Geonir M Siqueira; Roselia M Spanevello; Wilson Cunico
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

Review 2.  Saturated Five-Membered Thiazolidines and Their Derivatives: From Synthesis to Biological Applications.

Authors:  Nusrat Sahiba; Ayushi Sethiya; Jay Soni; Dinesh K Agarwal; Shikha Agarwal
Journal:  Top Curr Chem (Cham)       Date:  2020-03-23
  2 in total

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