Analgesic and Anti-Inflammatory Activity of 5-Aryl-4-Aroyl-3-Hydroxy-1-Carboxymethyl-3-Pyrrolin-2-Ones

The analgesic activity of previously synthesized 5-aryl-4-aroyl-3-hydroxy-1-carboxymethyl-3-pyrrolin-2- ones was studied in the hot-plate and acetic acid-induced writhing tests. Their anti-inflammatory activity was determined using the model of aseptic carrageenan-induced inflammation. Biological screening revealed compounds exhibiting analgesic activity comparable to that of the reference drug metamizole sodium and a pronounced anti-exudative effect not inferior to that of nimesulide. The probability of manifestation of analgesic and anti-inflammatory activity is shown to increase with the introduction of a p-halophenyl substituent in the 5-position or a p-alkylbenzoyl fragment in the 4-position of the heterocycle. The search in this series for pharmacologically active compounds of interest as potential drugs is shown to be promising.