Research of anti-inflammatory and analgetic activity of 1, 4-dicarboxylic acids derivatives

The search for new compounds with anti-inflammatory and analgesic effects is relevant. The goal - the search for compounds with anti-inflammatory and analgesic activities among monosubstituted amides and hydrazides of 1, 4-dicarboxylic acids. Material and methods. Objects of study - acylamides and acylhydrazides of 1, 4-dicarboxylic acids. A study of anti-inflammatory activity was carried out for 11 compounds on white non-linear rats of both sexes weighing 190-220 g (6 animals) in a model of acute inflammatory edema (administration of 0.1 ml of a 1% aqueous solution of carrageenin). An increase in foot volume was evaluated on-cometrically before administration and 3 hours after administration of carrageenin. The test substances were administered orally at a dose of 50 mg / kg 1 hour before the administration of the phlogogenic agent. Standard: the drug «Nimesulide-MBF» Control: animals not receiving the drug. The presence of anti-inflammatory action was judged by the severity of inhibition of the inflammatory reaction. Analgesic activity was determined for 9 compounds on white non-linear mice weighing 25-30 g (8 animals) according to the method of «hot plate». Compounds were administered intraperitoneally 30 minutes before testing at a dose of 50 mg / kg. Standard: the drug «Metamizole Sodium» The animals were placed on a metal surface heated to 56 ° C. The time was recorded from the moment it was placed on a hot surface until a behavioral response to pain irritation appeared. A criterion for the analgesic effect was considered a significant increase in the latent period of the reaction after administration of the substance. The animals of the control group were injected with an equivolume amount of physiological sodium chloride solution. Results. It was found that maleic acid 2-pyrimidylamide, 4-methyl-2-pyridylamide and citraconic acid 2-thiazolylamide showed pronounced anti-inflammatory activity. High analgesic activity was found for 3-hydroxy-4-carboxyphenylamide maleic acid and 4-methoxybenzoylhydrazide phthalic acid. 4-Methyl-2-pyridylamide of citraconic acid exceeds the effect of the drug «Metamizole sodium» and has an anti-inflammatory effect at the level of the drug «Nimesulide». Findings. It is recommended to continue the search among the derivatives of 1,4-dicarboxylic acids for compounds with antiinflammatory and analgesic effects.

derivatives of 1, 4-dicarboxylic acids, analgesic, anti-inflammatory activity