4.7 Article

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

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 14, 页码 4295-4306

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.05.056

关键词

Antidepressant effect; Sulphonamides; Sulphonyl-hydrazones; Cyclic imides

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  1. CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico)

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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 60 mg/kg, it thus being more active than imipramine (10 mg/kg, ip), a commercial antidepressant. Other important results were obtained for the benzylnaphthalimide derivatives, the sulphonamides 21 and 22 showing activity of 64% at 10 mg/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. (C) 2011 Elsevier Ltd. All rights reserved.

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