title: Synthesis and antidepressant-like activity evaluation of sulphonamides and sulphonyl-hydrazones.
abstract: 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 (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.
authors.affiliation: Departamento de Química, Universidade Federal de Santa Catarina, UFSC, Florianópolis, CCS/PMCF/UNIVALI, 88302-202, Itajaí, SC, Brazil.
authors.forename: Kely Navakoski
authors.initials: KN
authors.lastname: de Oliveira
authors.forename: Philipe
authors.initials: P
authors.lastname: Costa
authors.forename: José Roberto
authors.initials: JR
authors.lastname: Santin
authors.forename: Leonor
authors.initials: L
authors.lastname: Mazzambani
authors.forename: Cristiani
authors.initials: C
authors.lastname: Bürger
authors.forename: Cristiano
authors.initials: C
authors.lastname: Mora
authors.forename: Ricardo José
authors.initials: RJ
authors.lastname: Nunes
authors.forename: Márcia Maria
authors.initials: MM
authors.lastname: de Souza
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects*; D013237:Stereoisomerism; D013315:Stress, Psychological; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013550:Swimming / Q000523:psychology
chemical_list: D000928:Antidepressive Agents; D006835:Hydrazones; D013449:Sulfonamides