Abstract
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.
Keywords: Analgesic activity; Gastric ulcerogenic activity, Metabolites, Hydantoin, Ibuprofen, Synthesis.
Letters in Drug Design & Discovery
Title:Synthesis, Evaluation of Analgesic and Gastric Ulcerogenic Activities and the Metabolites in Rat Plasma of Hydantoin Ibuprofen Conjugates
Volume: 10 Issue: 9
Author(s): Cuiying Mao, Ping Yang, Yongsheng Wang, Lan Qiao, Bing Chen, Shihan Wang, Yang Xu and Haibin Lu
Affiliation:
Keywords: Analgesic activity; Gastric ulcerogenic activity, Metabolites, Hydantoin, Ibuprofen, Synthesis.
Abstract: 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.
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Mao Cuiying, Yang Ping, Wang Yongsheng, Qiao Lan, Chen Bing, Wang Shihan, Xu Yang and Lu Haibin, Synthesis, Evaluation of Analgesic and Gastric Ulcerogenic Activities and the Metabolites in Rat Plasma of Hydantoin Ibuprofen Conjugates, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/15701808113109990005
DOI https://dx.doi.org/10.2174/15701808113109990005 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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