Docking, Synthesis and anticonvulsant activity of N-substituted isoindoline-1,3-dione

Document Type: Research article

Authors

1 Chemical Injuries Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran.

2 Department of Medicinal Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran

3 Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran (IAUPS).

4 Department of Pharmacology, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran

Abstract

A series of compounds related to ameltolide were studied for anticonvulsant potential in the subcutaneous pentylenetetrazol (sc Ptz) test in mice. These compounds were synthesized and characterized by TLC followed by IR and H1NMR. In vivo screening data acquired indicate that most of analogs have the ability to protect against PTZ-induced seizure. Phenytoin (PHT) was employed as the reference prototype antiepileptic drug. All compounds exerted their maximal effects 30 min after administration. Out of the 6 compounds, compound 2 at 40 mg/kg dose is more potent than phenytoin (reference drug) on clonic seizure. Using a model of the open pore of the Na channel, docking study was performed by AutoDock4.2 program. Docking studies has revealed that these compounds are stabilized through at least one hydrogen bond rises from ketone of phthalimide and residue Thr-87 of domain G of sodium channel.

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Iranian Journal of Pharmaceutical Research

Volume 16, Issue 2
Spring 2017
Pages 586-595

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