Anticonvulsant activity of 3-oxo-5-substituted benzylidene-6-methyl-(4H)-2-pyridazinylacetamides and 2-pyridazinylacetylhydrazides.
A series of 3-oxo-5-substituted-benzylidene-6-methyl-(4H)-2- pyridazinylacetamides and 2-pyridazinylacetylhydrazides were synthesized and evaluated for anticonvulsant activity against electrically and chemically induced seizures. In the maximal electroshock-induced seizures test, most of the derivatives showed an anticonvulsant effect better than that of sodium valproate, a commonly used anticonvulsant drug. At 100 mg/kg orally, compounds 5a and 5b respectively protected 50 and 60% of the mice against pentylentetrazole-induced seizures. In addition, these two derivatives showed significant anticonvulsant properties at doses that did not produce ataxia or sedation. The title compounds were also tested for their ability to antagonize convulsions induced by bicuculline and strychnine. Their effect on tremors induced by oxotremorine in mice was also evaluated.
Rubat
C
C
Laboratoire de Pharmacologie et de Pharmacie Clinique, Faculté de Pharmacie Université de Clermont-Ferrand, France.
Coudert
P
P
Refouvelet
B
B
Tronche
P
P
Bastide
P
P
Bastide
J
J
D000081:Acetamides / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D006834:Hydrazines / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology
D000081:Acetamides; D000927:Anticonvulsants; D001597:Benzylidene Compounds; D006834:Hydrazines; D011724:Pyridazines