Synthesis, Evaluation of Analgesic and Gastric Ulcerogenic Activities and the Metabolites in Rat Plasma of Hydantoin Ibuprofen Conjugates

Previous studies demonstrated that hydantoin ibuprofen conjugates had effective anti-inflammatory and antitussive activities. In this study, we evaluated their analgesic and gastric ulcerogenic activities. Our results showed that these compounds retained analgesic activity from ibuprofen, more important, could suppress gastric ulceration. Furthermore, by analyzing the metabolites of the compounds in rat plasma using LC-MS/MS, we found that the compounds were hydrolyzed to hydantoin and ibuprofen, and then followed by ibuprofen conjugation to glucuronic acid.