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Synthesis of 1‐( N ‐piperidinoacetyl)‐4‐arylthiosemicarbazides as possible anticonvulsants
Author(s) -
Misra R. S.,
Parmar S. S.,
Kishore V.,
Ali B.,
Gupta T. K.
Publication year - 1979
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.5570160345
Subject(s) - chemistry , hydrazide , hydrazine (antidepressant) , pentylenetetrazol , monoamine oxidase , anticonvulsant , hydrate , hemolysis , pharmacology , medicinal chemistry , nuclear chemistry , chromatography , organic chemistry , epilepsy , enzyme , medicine , neuroscience , biology
Several 1‐( N ‐piperidinoacetyl)‐4‐arylthiosemicarbazides were synthesized from N ‐piperidinoacetyl hydrazide, which was obtained by the reaction of hydrazine hydrate with ethyl N ‐piperidinoacetate. The anticonvulsant activity of these substituted thiosemicarbazides was reflected by their ability to provide 10–50% protection against pentylenetetrazol‐induced convulsions in mice. All substituted thiosemicarbazides (0.3 m M ) inhibited in vitro monoamine oxidase activity of rat brain homogenates and provided 21–86% protection against hypoosmotic hemolysis at a final concentration of 0.1 m M .