Anticonvulsant Activity of 2-(Substituted-imino)thiazolidin-4-ones

G.-H. Gong; D. Wang; J.-F. Zhang; C.-X. Wei; Z.-S. Quan

doi:10.1055/s-0033-1349095

Drug Research, Table of Contents

Drug Res (Stuttg) 2014; 64(01): 5-9
DOI: 10.1055/s-0033-1349095

Original Article

Anticonvulsant Activity of 2-(Substituted-imino)thiazolidin-4-ones

G.-H. Gong

¹College of Pharmacy, Yanbian University, Yanji, China

²Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China

,

D. Wang

¹College of Pharmacy, Yanbian University, Yanji, China

²Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China

,

J.-F. Zhang

²Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China

,

C.-X. Wei

²Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China

,

Z.-S. Quan

¹College of Pharmacy, Yanbian University, Yanji, China

› Author Affiliations

Abstract

A novel series of 2-(substituted-imino)thiazolidin-4-ones were synthesized and evaluated for anticonvulsant activity using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (Sc-PTZ) assays and their neurotoxicity was measured by the rotarod test. The results of these tests demonstrated that 2-(4-(pentyloxy)phenylimino)thiazolidin-4-one (5d) was the most potent anticonvulsant, with ED₅₀ value of 18.5 mg/kg and 15.3 mg/kg in the MES and Sc-PTZ tests, and protective index (PI=TD₅₀/ED₅₀) values of 10.6 and 12.8 respectively. 5d was much safer than a reference drug Carbamazepine.

Key words

thiazolidin-4-one - anticonvulsant - MES - Sc-PTZ - neurotoxicity

Full Text

References

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