Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy

• Published in: Journal of medicinal chemistry Vol. 29; no. 3; pp. 369 - 375
• Main Authors: Hallot, Andre, Brodin, Roger, Merlier, Josiane, Brochard, Joelle, Chambon, Jean Pierre, Biziere, Kathleen
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 01.03.1986
• Subjects: Animals; Anticonvulsants - chemical synthesis; Bicuculline - antagonists & inhibitors; Chemistry; Disease Models, Animal; Dose-Response Relationship, Drug; Electroshock; Exact sciences and technology; Female; Heterocyclic compounds; Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings; Hypnotics and Sedatives; Kindling, Neurologic - drug effects; Male; Mice; Motor Skills - drug effects; Organic chemistry; Papio; Pentylenetetrazole - antagonists & inhibitors; Photic Stimulation; Preparations and properties; Pyridazines - chemical synthesis; Pyridazines - pharmacology; Rats; Rats, Inbred Strains; Seizures - chemically induced; Seizures - drug therapy; Seizures - etiology; Structure-Activity Relationship; In vivo; Nitrogen heterocycle; Animal; Six membered ring; Benzenic compound; Anticonvulsant; Sedative; Biological activity

A series of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines derivatives was synthesized and evaluated for anticonvulsant activity. The compounds were screened in mice for their ability to antagonize maximal electroshock- and bicuculline-induced seizures; neurotoxicity was evaluated in the rotorod te...