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Anticonvulsant activity and succinate dehydrogenase inhibitory property of new substituted thiobarbiturates
Author(s) -
Dhasmana Anjali,
Barthwal J. P.,
Pandey B. R.,
Ali B.,
Bhargava K. P.,
Parmar S. S.
Publication year - 1981
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570180341
Subject(s) - chemistry , succinate dehydrogenase , pentylenetetrazol , anticonvulsant , inhibitory postsynaptic potential , in vitro , toxicity , dehydrogenase , aryl , pharmacology , stereochemistry , biochemistry , enzyme , organic chemistry , medicine , epilepsy , alkyl , neuroscience , biology
Eight 1‐aryl‐3‐(2‐pyridyl)thiobarbiturates were synthesized and evaluated for their anticonvulsant property and their ability to inhibit succinate dehydrogenase activity of rat brain homogenates. These substituted thiobarbiturates (100 mg./kg., i.p.) provided 20–60% protection against pentylenetetrazol‐induced convulsions in albino mice. Low toxicity of these compounds was reflected by their high approximate LD 50 values which were found to range from 500–1000 mg./kg. All substituted thiobarbiturates (Im M ) inhibited in vitro succinate dehydrogenase activity and the degree of inhibition ranged from 10–72%.