Antidepressant activity of new 3-amino-5-disubstituted benzylidene-6-methyl-(4H)-pyridazine derivatives.

By the reaction of various amines with 3-chloropyridazines,several minaprine analogues were prepared.Most of them exhibited significant antidepressant activity.Compound 2a antagonizes reserpine action and neuroleptic-induced catalepsy in a dose-dependent manner. Keywords-disubstituted benzylidene pyridazine;3-amino pyridazine derivative,minaprine analogue;antidepressant activity Recently,it was reported that minaprine proved to be effective in the treatment of various depressive disorders.1)This 3-amino-6-phenylpyridazine derivative is known to represent a new class of psychotropic drugs.2)This prompted us to synthesize analogues containing a 5-disubstituted benzylidene pyridazine moiety.Most of them were found to be effective in antidepressant activity tests. minaprine Results and Discussion The selected compounds were synthesized according to the scheme shown. 1 2a-9 3-Chloro-5-disubstituted benzylidene-6-methyl-4H-pyridazines(1)were prepared as described in a previous paper.3)They were refluxed with an excess of the requisite amine to afford 3-amino-5-disubstituted benzylidene-6-methyl-4H-pyridazine derivatives(2a-g).All compounds were evaluated for antidepressant activity as described in the experimental section.Physical and spectral data are summarized in Tables I and II:pharmacological data are reported in Table III.