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Synthesis and Evaluation of Anti-Epileptic Properties of New Phthalimide-4,5-Dihydrothiazole-Amide Derivatives Publisher



Tabatabaei Rafiei LS1 ; Asadi M2 ; Hosseini FS2 ; Amanlou A3 ; Biglar M4 ; Amanlou M2, 5
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Faculty of Specialized Veterinary Sciences, Science and Research Branch, Islamic Azad University, Tehran, Iran
  4. 4. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Experimental Medicine Research Center, Tehran University of Medical Sciences, Tehran, Iran

Source: Polycyclic Aromatic Compounds Published:2022


Abstract

In this work, a novel series of phthalimide-4,5-dihydrothiazole-amide derivatives 5a–f have been synthesized and evaluated for their anti-epileptic activities against pentylenetetrazole (PTZ)-induced seizure in mice. Among the synthesized compounds, the most potent was 4-chloro derivative 5b with zero mortality in PTZ test. Molecular docking was performed to investigate the modes of interactions between GABAA receptor and synthetized compounds. Docking results were in good agreement with observed experimental data and indicate that among six new derivatives, compound 5b with highest effective anticonvulsant properties, had lowest binding energy. This compound also exhibited better anti-epileptic activity and lower binding energy for connect to GABAA receptor in comparison to thalidomide as standard anti-epileptic agent. © 2020 Taylor & Francis Group, LLC.
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Mahmood Biglar (3)
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