Anticonvulsant and neurotoxicity evaluation of some 6-chlorobenzothiazolyl-2-thiosemicarbazones

Ten 6-chlorobenzothiazolyl-2-thiosemicarbazones were synthesised and screened for anticonvulsant and neurotoxic properties. Most of the compounds showed anticonvulsant activity against both maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole screens. Eight compounds have shown goo...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2002-03, Vol.37 (3), p.231-236
Main Authors: Yogeeswari, Perumal, Sriram, Dharmarajan, Sunil Jit, Logantha Ramamoorthy Jeewanlal, Kumar, Sathiyanesan Sathish, Stables, James P
Format: Article
Language:English
Subjects:
Amygdala - drug effects
Amygdala - physiology
Animals
Anticonvulsants - administration & dosage
Anticonvulsants - chemical synthesis
Anticonvulsants - therapeutic use
Anticonvulsants - toxicity
Anticonvulsants. Antiepileptics. Antiparkinson agents
Benzothiazolylthiosemicarbazones
Biological and medical sciences
Drug Evaluation, Preclinical
Electroshock
Fully kindled
Kindling, Neurologic - drug effects
Medical sciences
Mice
Molecular Structure
Neuropharmacology
Neurotoxicity
Pentylenetetrazole
Pharmacology. Drug treatments
Rats
Seizures - chemically induced
Seizures - drug therapy
Thiosemicarbazones - administration & dosage
Thiosemicarbazones - chemical synthesis
Thiosemicarbazones - therapeutic use
Thiosemicarbazones - toxicity
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Summary:Ten 6-chlorobenzothiazolyl-2-thiosemicarbazones were synthesised and screened for anticonvulsant and neurotoxic properties. Most of the compounds showed anticonvulsant activity against both maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole screens. Eight compounds have shown good protection in the rat p.o. MES test at 30 mg kg −1. Compound 1 [4-(6-chlorobenzothiazol-2-yl)-1-(3-isatinimino)thiosemicarbazone] emerged as the most promising one with an ED 50 of 17.86 and 6.07 mg kg −1 in mice i.p. and rat p.o., respectively. Compound 1 showed a weak ability to block the expression of fully kindled seizures.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(02)01338-7