Repository of Research and Investigative Information

Repository of Research and Investigative Information

Baqiyatallah University of Medical Sciences

Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione

(2017) Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione. Iranian Journal of Pharmaceutical Research. pp. 586-595. ISSN 1735-0328

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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 AutoDock 4.2 program. Docking study 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.

Item Type: Article
Keywords: Anticonvulsant Design Isoindoline Seizure Synthesis sodium-channel 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent derivatives 1,4-dihydropyridines seizure binding analogs qsar Pharmacology & Pharmacy
Divisions:
Page Range: pp. 586-595
Journal or Publication Title: Iranian Journal of Pharmaceutical Research
Journal Index: ISI
Volume: 16
Number: 2
ISSN: 1735-0328
Depositing User: مهندس مهدی شریفی
URI: http://eprints.bmsu.ac.ir/id/eprint/4510

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