SYNTHESIS
AND EVALUATION OF THE ANTICONVULSANT ACTIVITIES OF SOME
5-(4-SUBSTITUTEDBENZYLIDENE)-6-METHYL-4,5-DIHYDROPYRIDAZINE-3(2H)-ONES
Oya ÜNSAL*, *Ayla BALKANo*, Cenk AYPAK**,
Berna TERZÝOÐLU**, M. Zafer GÖKER**
*
Hacettepe University, Faculty of Pharmacy, Department
of Pharmaceutical Chemistry, 06100 Sýhhiye, Ankara-TURKEY.
** Marmara University, School of Medicine, Department
of Pharmacology and Clinical Pharmacology, 81326, Haydarpaþa,
Ýstanbul - TURKEY.
oCorresponding Author
Summary
In this study, starting from 3-benzylidene-4-oxopentanoic
acid derivatives (1a-e), having 5-benzylidene-6-methyl-4,5-dihydropyridazine-3(2H)-one
(2a-e) structure and their ester (3a-e), hydrazide (4a-e)
and acetic acid (5a-e) derivatives were synthesized. The
physical properties and UV absorptions of the five starting
compounds (1a-e) and twenty target compounds (2a-5e) were
determined. Their chemical structures were achieved by
IR and 1 H-NMR spectral data. Additionally, elemental
analysis data of the new compounds (1b, 2b, 3b, 4b, 5b,
3c, 4c, 5c, 2e, 3e, 4e and 5e) were done to identify the
structures.
Anticonvulsant activities of the target compounds (2a-5e)
were screened by pentylenetetrazole seizure model. It
was observed that compound 2a showed an anticonvulsant
effect similar to ethosuximide concerning the seizure
grade
Key Words :
4,5-dihydropyridazine-3(2H)-one, 6-oxo-5,6-dihydropyridazinylacetate,
6-oxo-5,6-dihyd-ropyridazinylacetohydrazide, 6-oxo-5,6-dihyd-ropyridazinylacetic
acid, anticonvulsant activity