Synthesis and anticonvulsant activity of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones.
The synthesis and pharmacological evaluation of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones (4a--l, 5a--j) as potential anticonvulsant agents are described. The compounds were tested in vivo for the anticonvulsant activity. The compound which have maximum protection against MES induced seizures is 1-[3-(2-aminophenylamino)-2-hydroxypropyl)-1,2-dihydro-pyridazine-3,6-dione 4h (ED(50)=44.7 mg x kg(-1) i.p.) 1-[2-hydroxy-3-piperazin1-yl-propyl)-1,2-dihydro-pyridazine-3,6-dione 4c (ED(50)=72 mg x kg(-1) i.p.) and 1-[2-hydroxy-3-imidazol-1-yl-propyl)-1,2-dihydro-pyridazine-3,6-dione 4d (ED(50)=79 mg x kg(-1) i.p.) were also found to have maximum protection against MES induced seizures. Whereas all these compounds failed to protect the animals from subcutaneous pentylenetetrazole (Metrozol) seizure threshold test (sc-Met).
Sivakumar
Ramaiah
R
Department of Pharmaceutical Chemistry and Pharmacology, Vel's College of Pharmacy, India.
Anbalagan
Navaneetharaman
N
Gunasekaran
Vedachalam
V
Leonard
Joseph Thomas
JT
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D004095:Dihydropyridines; D005260:Female; D008297:Male; D051379:Mice; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D012640:Seizures / Q000517:prevention & control; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D004095:Dihydropyridines; D011724:Pyridazines; C038806:1,4-dihydropyridine