Pharmacological evaluation of some new 1-substituted-4-hydroxy-phthalazines.
In the present study, a series of 1-substituted-4-hydroxyphthalazines were synthesized and characterized by IR, 1H-NMR and Elemental analysis. The compounds were assayed against seizures induced by maximal electroshock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The decrease in the elevated motor activity by introceptive chemical stimuli (amphetamine antagonistic activity) was studied at the dose level of 25 and 50 mg kg(-1) and cardiac activity was also studied. All the compounds exhibited significant anticonvulsant activity. Compounds 4, 12, 13 and 17 were most active of the seriesagainst MES-induced seizures. Compounds 2, 4, 13 and 17 exhibited significant decrease in the elevated motor activity at the dose of 50 mg kg(-1). Remarkable sympathetic blocking activity was observed with 3, 5, 6, 7, 9 and 15 only.
Sivakumar
Ramaiya
R
Department of Pharmaceutical Chemistry and Pharmacology, Vel's College of Pharmacy, Old Pallavaram, Chennai 600 117, India.
Kishore Gnanasam
Sundararaj
S
Ramachandran
Somasundaram
S
Leonard
Joseph Thomas
JT
D000661:Amphetamine / Q000037:antagonists & inhibitors; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D004837:Epinephrine / Q000494:pharmacology; D006321:Heart / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D010433:Pentylenetetrazole / Q000633:toxicity; D010634:Phenobarbital / Q000494:pharmacology; D010793:Phthalazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011898:Ranidae; D012640:Seizures / Q000139:chemically induced; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D010793:Phthalazines; D000661:Amphetamine; D010433:Pentylenetetrazole; D004837:Epinephrine; D010634:Phenobarbital