Hallot, Andre published the artcileSynthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy, Quality Control of 58059-33-9, the main research area is hydroxypolymethyleneamino pyridazine preparation anticonvulsant; piperidinopyridazine chlorophenylhydroxy preparation anticonvulsant.
Title pyridazines, e.g. I (R = ClC6H4, Cl2C6H3, thienyl, pyridyl), were 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 test. The anticonvulsant activity of the most potent compounds was examined in kindled amygdaloid rats and in photoepileptic Papio papio baboons. Structure-activity relationships were examined by either varying the aryl ring in the 6-position of the pyridazine ring or by modifying the 3-amino side chain. Only the compounds with a Ph ring in the 6-position of the pyridazine ring exhibited appreciable anticonvulsant activity, and a 4-hydroxypiperidine side chain in the 3-position of the pyridazine ring appeared essential for anticonvulsant activity. Substituting the Ph ring with a Cl in the 2-position led to a substantial increase of activity and disubstituting the Ph ring with a Cl in the 2- and 4-positions yielded the most potent compounds, some of which were as potent as, or more potent than, phenobarbital. 6-(2-Chlorophenyl)-3-(4-hydroxypiperidino)pyridazine and 6-(2,4-dichlorophenyl-3-(4-hydroxypiperidino)pyridazine were selected for further studies.
Journal of Medicinal Chemistry published new progress about Anticonvulsants. 58059-33-9 belongs to class pyridazine, name is 3-Chloro-6-(3-nitrophenyl)pyridazine, and the molecular formula is C10H6ClN3O2, Quality Control of 58059-33-9.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem