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Design, Synthesis, Pharmacological Evaluation, and Docking Study of New Acridone-Based 1,2,4-Oxadiazoles As Potential Anticonvulsant Agents Publisher Pubmed



Mohammadikhanaposhtani M1 ; Shabani M2 ; Faizi M3 ; Aghaei I4 ; Jahani R3 ; Sharafi Z5 ; Shamsaei Zafarghandi N1 ; Mahdavi M1 ; Akbarzadeh T1, 6 ; Emami S7 ; Shafiee A1 ; Foroumadi A1, 8
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran
  3. 3. Department of Pharmacology and Toxicology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  4. 4. Social Determinants of Health Research Center, Guilan University of Medical Sciences, Rasht, Iran
  5. 5. Department of Pharmaceutical Biotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  6. 6. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
  7. 7. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
  8. 8. Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran

Source: European Journal of Medicinal Chemistry Published:2016


Abstract

A number of acridone-based oxadiazoles 11a–n have been synthesized and evaluated for their anticonvulsant activity against pentylenetetrazole (PTZ)- and maximal electroshock (MES)-induced seizures in mice. Also, their neurotoxicity was evaluated by the rotarod test. Most of the compounds exhibited better anticonvulsant activity and higher safety respect to the standard drug, phenobarbital. Among the tested derivatives, compounds 11l with ED50value of 2.08 mg/kg was the most potent compound in the PTZ test. The anticonvulsant effect of compound 11l was blocked by flumazenil, suggesting the involvement of benzodiazepine (BZD) receptors in the anticonvulsant activity of prototype compound 11l. Also, docking study of compound 11l in the BZD-binding site of GABAAreceptor confirms possible binding of compound 11l with BZD receptors. © 2016 Elsevier Masson SAS
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