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Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione
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 H(1)NMR. In-vivo screening data acquired indicate that most of analogs have...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Shaheed Beheshti University of Medical Sciences
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5603866/ https://www.ncbi.nlm.nih.gov/pubmed/29721024 |
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author | Iman, Maryam Saadabadi, Atefeh Davood, Asghar Shafaroodi, Hamed Nikbakht, Ali Ansari, Abdollah Abedini, Masood |
author_facet | Iman, Maryam Saadabadi, Atefeh Davood, Asghar Shafaroodi, Hamed Nikbakht, Ali Ansari, Abdollah Abedini, Masood |
author_sort | Iman, Maryam |
collection | PubMed |
description | 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 H(1)NMR. 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. |
format | Online Article Text |
id | pubmed-5603866 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-56038662018-05-02 Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione Iman, Maryam Saadabadi, Atefeh Davood, Asghar Shafaroodi, Hamed Nikbakht, Ali Ansari, Abdollah Abedini, Masood Iran J Pharm Res Original Article 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 H(1)NMR. 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. Shaheed Beheshti University of Medical Sciences 2017 /pmc/articles/PMC5603866/ /pubmed/29721024 Text en © 2017 by School of Pharmacy Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Article Iman, Maryam Saadabadi, Atefeh Davood, Asghar Shafaroodi, Hamed Nikbakht, Ali Ansari, Abdollah Abedini, Masood Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione |
title | Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione |
title_full | Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione |
title_fullStr | Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione |
title_full_unstemmed | Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione |
title_short | Docking, Synthesis and Anticonvulsant Activity of N-substituted Isoindoline-1,3-dione |
title_sort | docking, synthesis and anticonvulsant activity of n-substituted isoindoline-1,3-dione |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5603866/ https://www.ncbi.nlm.nih.gov/pubmed/29721024 |
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