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



Faizi M1 ; Jahani R1 ; Ebadi SA2 ; Tabatabai SA3 ; Rezaee E3 ; Lotfaliei M3 ; Amini M4 ; Almasirad A2
Authors

Source: EXCLI Journal Published:2017


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 5i, 4-chloro-N-(2-(4-methoxy-phenyl)-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 5i indicating that benzodiazepine receptors are highly involved in the pharmacological properties of the novel compounds. © 2017, Leibniz Research Centre for Working Environment and Human Factors. All rights reserved.
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