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Drug Res (Stuttg) 2014; 64(01): 5-9
DOI: 10.1055/s-0033-1349095
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

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

G.-H. Gong
1   College of Pharmacy, Yanbian University, Yanji, China
2   Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China
,
D. Wang
1   College of Pharmacy, Yanbian University, Yanji, China
2   Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China
,
J.-F. Zhang
2   Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China
,
C.-X. Wei
2   Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China
,
Z.-S. Quan
1   College of Pharmacy, Yanbian University, Yanji, China
› Author Affiliations
Further Information

Publication History

received 18 July 2012

accepted 13 February 2013

Publication Date:
16 August 2013 (online)

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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
 

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