| Summary: | Thirty-four new benzo[<i>d</i>]thiazol derivatives <b>2a</b>−<b>2i</b>, <b>3a</b>−<b>3r</b>, and <b>4a</b>−<b>4g</b> were synthesized and investigated for their potential antidepressant and anticonvulsant effects. In a forced swimming test, <b>2c</b> and <b>2d</b> showed the highest antidepressant and anticonvulsant effects. <b>2c</b> and <b>2d</b> displayed a higher percentage decrease in immobility duration (89.96% and 89.62%, respectively) than that of fluoxetine (83.62%). In the maximal electroshock seizure test, <b>3n</b> and <b>3q</b> showed the highest anticonvulsant effect, with ED<sub>50</sub> values of 46.1 and 64.3 mg kg<sup>−</sup><sup>1</sup>, and protective indices of 6.34 and 4.11, respectively, which were similar to those of phenobarbital or valproate. We also found that the mechanism for the antidepressant activity of <b>2c</b> and <b>2d</b> may be via increasing the concentrations of serotonin and norepinephrine.
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