RESUMO
The effect of ethanol and acetone extracts of Malvastrum coramandelianum were investigated for antipyretic analgesic activity. The model used for antipyretic studies was pyrexia-induced rat model and for analgesic studies was tail tlick method in rats. These studies indicate that both extracts were showing significant antipyretic and analgesic properties. The preliminary phytochemical investigation indicates the presence of saponins and steroids
Assuntos
Animais de Laboratório , Medicina Tradicional , Analgésicos não Narcóticos/síntese química , Analgésicos/síntese química , Plantas MedicinaisRESUMO
Ten new synthetic thiazolidine-4-ones derivatives (5 chlorothiazolidine-4-ones, 3 methoxythiazolidine-4-ones and 2 hydoxythiazolidine-4-ones) having different substituents at R1, R2 and R3 were evaluated for their analgesic activity using different animal models and their structure activity relationship was also elucidated. Chlorothiazolidine-4-ones and methoxythiazolidine-4-ones exhibited analgesic activity in tail flick test, tail immersion test and acetic acid writhing test. C-III (chloride substituents at R1 and R2) produced higher latencies than any other compounds in tail flick test and C-I (no substituents at R1 and R2) was not effective in acetic acid writhing test. Hydroxythiazolidine-4-ones did not show analgesic activity in any of the animal models used. In conclusion, the character of substituents at R3 of thiazolidine moiety position may have an effect on the analgesic activity of thiazolidine-4-ones and either chloride or methoxy substitution may be necessary to produce analgesic activity. Two chloride substituents in a compound may increase the central analgesic activity of the compound.
Assuntos
Analgésicos não Narcóticos/síntese química , Animais , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Camundongos , Medição da Dor , Ratos , Ratos Wistar , Relação Estrutura-Atividade , Tiazóis/síntese químicaRESUMO
The biologically active 4H-pyrido [1, 2-a] pyrimidin-4-ones [1] including some hexahydro derivatives [2] are non acidic non-steroidal anti-inflammatory agents. Other pyrido [1, 2-a] pyrimidines were reported as analgetic anti-inflammatory agents [3-8]. In a search of analgetic pharmacophore in condensed pyrimidines, the chemistry and analgetic activity of the bioisoster pyrimido-[1, 2-a] azepine [9] 1 was reported. This work found that ester, carbamate, thiosemicarbazide, semicarbazide, urea and acyl urea groups are of special value in the analgetic activity of 1. On the other h and, it was assumed that any changes in the structure of 1, that might add to its analgetic effect, would be beneficial