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THE ANALGESIC EFFECT OF 1,3-THIAZOLIDIN-4-ONE DERIVATIVES AS POTENTIAL MODULATORS OF THE SEROTONINERGIC SYSTEM

IWONA PIĄTKOWSKA-CHMIEL 1*, ŁUKASZ POPIOŁEK 2, MONIKA GAWROŃSKA-GRZYWACZ 1, DOROTA NATORSKA-CHOMICKA 1, MAGDALENA IZDEBSKA 1, MARIOLA HERBET 1, JAROSŁAW DUDKA 1, EWA POLESZAK 3, MONIKA WUJEC 2

1.Department of Toxicology, Medical University of Lublin, 8b Jaczewski St., PL 20-090 Lublin, Poland
2.Department of Organic Chemistry, Medical University of Lublin, 4a Chodźki St., PL 20-093 Lublin, Poland
3.Department of Applied Pharmacy Faculty of Pharmacy, Medical University of Lublin, 1 Chodźki St., PL 20-093 Lublin, Poland

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This study presents the synthesis and evaluation of the analgesic effect of 1,3-thiazolidin-4-one derivatives. Tested compounds were prepared by the cyclization reaction of appropriate N-substituted carboxylic acid hydrazide derivatives with mercaptoacetic acid. The purpose of this study was the evaluation of the analgesic properties of 1,3-thiazolidin-4-one derivatives. In addition to this, we tried to explain the role of serotonin receptors in the antinociceptive mechanisms of tested compounds. The experiments were carried out using male Albino Swiss mice (20-25g). The compounds were administered intraperitoneally (ip) and were analysed for analgesic activities in models of pain in mice. Additionally, they were tested for safety on the central nervous system of mice in selected behavioural tests. Our results revealed an interesting analgesic activity of the tested compounds. The tested derivatives showed low toxicity, reflected by their LD50 value. Moreover, none of these compounds exhibited neurotoxic properties or impaired the cognitive activity of mice, even at the highest doses used. All tested derivatives showed analgesic activity. Among the tested compounds, N-[2-(4-methylphenyl)-4-oxo-1,3-thiazolidin-3-yl] acetamide seems to be the most effective painkiller. It has a pronounced antinociceptive effect towards thermal and mechanical pain stimulation. The present results support the idea that 5-HT receptors play an important role in the control of pain. The compounds that modulate 5-HT receptors activity may have clinical utility in pain therapy.