Anticonvulsant and monoamine oxidase inhibitory activity of substituted oxadiazol-thiones.
Several 1,3,4-oxadiazol-thiones were synthesised and characterized by their melting points elemental analysis and I.R. spectra. All the oxadiazol-thiones possessed anticonvulsant activity which was reflected by protection upto 80% against pentylenetetrazole induced seizures and 40% protection against maximal electroshock induced seizures. Substantiations at position-3 of oxadiazol-thiones have shown marked effect on MAO inhibitory activity. No definite correlation between monoamine oxidase inhibitory and anticonvulsant activity could be established. It was observed that by the substitution of one, two and three methyl groups in the phenyl ring of 2-arylamino methyl side chain anticonvulsant activity against both maximal electroshock induced convulsions and pentylenetetrazol induced convulsions decreases i.e. the order of activity was found to be unsubstituted greater than monomethyl greater than dimethyl greater than trimethyl.
D000818:Animals; D000927:Anticonvulsants; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D005260:Female; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013871:Thiones / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity
D000927:Anticonvulsants; D008996:Monoamine Oxidase Inhibitors; D010069:Oxadiazoles; D013871:Thiones