Avaliação antinociceptiva de 2,3-substituídos-1,3-tiazolidin-4-onas mediante estimulo térmico em camundongos

Abstract

To contribute with the development of new analgesic drugs added to the fact that 4- thiazolidinones are an important scaffold associated with many pharmacological activity, the present study assessed the 2,3-substituted-1,3-thiazolidin-4-ones potential antinociceptive through the acute nociception model, induced by thermal stimulation in mice. The synthesized compounds were characterized by GC/MS and NMR of 1H and 13C and administered at dose 100 mg/kg (ip) (hydrochloride salt). Sodium dipyrone (250 e 500 mg/Kg; ip), tramadol hydrochloride (25 e 50mg/Kg; ip) was used with positive controls. The hot plate test was done at temperature of 50±0,1ºC and animals assess in times of 30, 60 and 90 minutes after administration drugs. From the fourteen compounds tested, nine (5Aa, 5Ab, 5Ac, 5Ad, 5Ba, 5Bb, 5Bd, 5Ea, 5Fa) showed significant increases in latency time when compared to saline (negative control), and three (5Ab, 5Ac and 5Ad) presented no significant difference compared to sodium dipyrone (500 mg/Kg; ip) in assess of 30 minutes. The highest latency times were obtained at the 3-(2-piperidin-1-yl)ethyl)thiazolidin-4- one derivatives (5Ab, 5Ac and 5Ad).Moreover, substituents 2-butyl (b), 2-phenyl (c) and 2-cyclohexane (d) promote greater increases in the latency time than 4- fluorophenyl (a). The compound2-(4-fluorophenyl)-3-(pyridin-2-ylmethyl)thiazolidin-4- one (5Ea) was the only that retained the antinociceptive effect in assessment of 30, 60 and 90 minutes. Moreover, the substitution of 4-nitrophenyl (e) or 4- methoxyphenyl (f) did not prove to be favorable for antinociceptive activity of these compounds. Key-words: antinociception; 4-t