Synthesis and antidepressant-like activity evaluation of sulphonamides and sulphonyl-hydrazones

In this study a series of sulphonamides and sulphonyl hydrazones of maleimide, naphthalimide and phthalimide derivatives was synthesized. The antidepressant effect of these compounds was evaluated by the forced-swimming test in mice. The behavioural parameter observed in this test is a reduction in...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2011-07, Vol.19 (14), p.4295-4306
Hauptverfasser: de Oliveira, Kely Navakoski, Costa, Philipe, Santin, José Roberto, Mazzambani, Leonor, Bürger, Cristiani, Mora, Cristiano, Nunes, Ricardo José, de Souza, Márcia Maria
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Sprache:eng
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Zusammenfassung:In this study a series of sulphonamides and sulphonyl hydrazones of maleimide, naphthalimide and phthalimide derivatives was synthesized. The antidepressant effect of these compounds was evaluated by the forced-swimming test in mice. The behavioural parameter observed in this test is a reduction in the immobility time, which is indicative of antidepressant activity. All compounds, except 8, 11 and 24, were active as antidepressants. The most active compound was the sulphonyl-hydrazone 10 which showed an activity of around 72.02% at 60mg/kg, it thus being more active than imipramine (10mg/kg, ip), a commercial antidepressant. Other important results were obtained for the benzylnaphthalimide derivatives, the sulphonamides 21 and 22 showing activity of 64% at 10mg/kg, also being more active than imipramine. These results indicate that the sulphonamides and sulphonyl-hydrazone cyclic imide derivatives are potential compounds for use in the designing of new candidates for the treatment of depression.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2011.05.056