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Repository of Research and Investigative Information

Baqiyatallah University of Medical Sciences

Docking, synthesis, and pharmacological evaluation of isoindoline derivatives as anticonvulsant agents

(2013) Docking, synthesis, and pharmacological evaluation of isoindoline derivatives as anticonvulsant agents. Medicinal Chemistry Research. pp. 3177-3184. ISSN 1054-2523

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Abstract

Eleven analogs of N-arylisoindoline pharmacophore were synthesized and evaluated for their anticonvulsant activities. The in vivo screening data acquired indicate that all the analogs have the ability to protect against pentylenetetrazole-induced seizure. Compounds 2, 6, and 11 elevated clonic seizure thresholds at 30 min which were more active than reference drug phenytoin, and compounds 2, 7, and 11 showed marked anticonvulsant activity on tonic seizure. The most potent compounds were 2 and 11 which had comparative activity to the phenytoin. Using a model of the open pore of the Na channel, we have docked all compounds. Docking studies have revealed that these compounds interacted mainly with residues II-S6 of NaV1.2 by making hydrogen bonds and have additional hydrophobic interactions with other domains in the channel's inner pore.

Item Type: Article
Keywords: Anticonvulsant Docking Isoindoline Na channel Seizure epilepsy phenytoin binding Pharmacology & Pharmacy
Divisions:
Page Range: pp. 3177-3184
Journal or Publication Title: Medicinal Chemistry Research
Journal Index: ISI
Volume: 22
Number: 7
Identification Number: https://doi.org/10.1007/s00044-012-0256-y
ISSN: 1054-2523
Depositing User: مهندس مهدی شریفی
URI: http://eprints.bmsu.ac.ir/id/eprint/6020

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