RESUMEN
This work evaluates the antinociceptive properties of benzofuranones using chemically induced models of pain and the hot plate test. All the compounds exhibited significant antinociceptive activity, with 3-[2-(4-chlorophenyl)-2-oxoetil]-2-benzofuran-1(3H)-one (3d) being the most active. According to the application of the Topliss method, the 2π-π(2) parameter was the preponderant one, indicating that the hydrophobicity (π) seems to be more involved in the antinociceptive activity. Based on the table of other possible substituents proposed by Topliss, three derived from compound 3d were tested. 3-[2-(3-methoxyphenyl)-2-oxoetil]-2-benzofuran-1(3H)-one (3g) showed greater antinociceptive activity with better pharmacokinetic properties predicted. These results show the efficiency of the Topliss Method as a research tool for the discovery of potential candidate molecules for a new antinociceptive drug.
Asunto(s)
Analgésicos/uso terapéutico , Conducta Animal/efectos de los fármacos , Benzofuranos/uso terapéutico , Dolor/tratamiento farmacológico , Analgésicos/síntesis química , Analgésicos/química , Animales , Benzofuranos/síntesis química , Benzofuranos/química , Relación Dosis-Respuesta a Droga , Masculino , Ratones , Estructura Molecular , Dolor/inducido químicamente , Dimensión del Dolor , Relación Estructura-ActividadRESUMEN
In this study, we investigated the analgesic activity of crude aqueous and methanol extracts obtained from Abarema cochliacarpos bark in mice, and analyzed its phytochemical profile. All the extracts exhibited analgesic properties against the writhing test in mice, but the aqueous and methanol extracts were more active, and more potent than two known analgesic and anti-inflammatory drugs used as reference. They were also active against the capsaicin-model, but inactive when evaluated in the hot-plate test. Phytochemical studies revealed the presence of saponins, catechins, tannins, phenols and anthraquinones.
No presente trabalho foram avaliados a atividade antinociceptiva e o perfil fitoquímico dos extratos aquosos e metanólico produzidos com a casca do caule de Abarema cochliacarpos, uma espécie de Mata Atlântica com diversas indicações populares. Todos os extratos apresentaram atividade analgésica quando avaliados pelo teste das contorções abdominais induzidas pelo ácido acético via intraperitonial, apresentando respostas superiores às drogas usadas como referência, bem como no modelo da dor induzida por capsaicina. A avaliação fitoquímica demonstrou a presença de saponinas, catequinas, taninos, fenóis e antraquinonas.