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Novel Conjugates of Aspirin with Phenolic Acid as Anti‐inflammatory Agents Having Significantly Reduced Gastrointestinal Toxicity
Author(s) -
Jiang Shan,
Ding Ning,
Zhang Wei,
Zhang Yichun,
Geng Meiyu,
Li Yingxia
Publication year - 2010
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900217
Subject(s) - aspirin , chemistry , antioxidant , anti inflammatory , toxicity , pharmacology , in vivo , in vitro , acute toxicity , linker , biochemistry , medicine , biology , organic chemistry , microbiology and biotechnology , computer science , operating system
A series of novel conjugates of aspirin with natural phenolic acid antioxidants connected through a diol linker were designed and synthesized as potential bifunctional agents combining antioxidant and anti‐inflammatory activity for reducing gastrointestinal toxicity. In general, the conjugates were found to be efficient antioxidants and many of them demonstrated much more potent anti‐inflammatory activity than aspirin. Among them, 5a and 5b which bear the best anti‐inflammatory activity exhibited significantly reduced ulcerogenic potency and toxicity compared to aspirin. However, it is evident that the anti‐inflammatory activity of these dual‐acting molecules in vivo , was not simply consistent with their antioxidant ability in vitro .