Novel 4-thiazolidinone Derivatives As Agonists of Benzodiazepine Receptors: Design, Synthesis and Pharmacological Evaluation

Overview

Journal EXCLI J

Specialty Biology

Date 2017 Apr 25

PMID 28435427

Citations 11

Authors

Mehrdad Faizi

Reza Jahani

Seyed Abbas Ebadi

Sayyed Abbas Tabatabai

Elham Rezaee

Mehrnaz Lotfaliei

Mohsen Amini

Ali Almasirad

Affiliations

Soon will be listed here.

Abstract

A new series of 4-chloro-N-(2-(substitutedphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide derivatives were designed, synthesized and biologically evaluated as anticonvulsant agents. The designed compounds have the main essential functional groups for binding to the benzodiazepine receptors and 4-thiazolidinone ring as an anticonvulsant pharmacophore. Some of the new synthesized compounds showed considerable anticonvulsant activity in electroshock and pentylenetetrazole-induced lethal convulsion tests. Compound , 4-chloro-N-(2-(4-methoxyphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide, with the best activity was selected for evaluation of other benzodiazepine pharmacological effects. This compound induced significant sedative-hypnotic activity. However, it does not impair the learning and memory in the experimental condition. Flumazenil was able to antagonize the sedative-hypnotic and anticonvulsant effects of compound indicating that benzodiazepine receptors are highly involved in the pharmacological properties of the novel compounds.

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