Synthesis and Study of Analgesic and Anti-inflammatory Activities of Amide Derivatives of Ibuprofen

Abbas Ahmadi | Mohsen Khalili | Zahra Olama | Shirin Karami | Babak Nahri-Niknafs

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URL :   http://research.shahed.ac.ir/WSR/WebPages/Report/PaperView.aspx?PaperID=106256
Date :  2017/10/12
Publish in :    Mini-reviews in Medicinal Chemistry
DOI :  https://doi.org/10.2174/1389557516666161226155951

Keywords :Synthesis, Analgesic, Anti-inflammatory, Ibuprofen

Abstract :

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used drugs worldwide and represent a mainstay in the therapy of acute and chronic pain and inflammation. The traditional NSAIDs like ibuprofen (I) contain free carboxylic acid group which can produce gastrointestinal (GI) damage for long-term use. In order to obtain the novel NSAIDs with less side effects; carboxylic acid moiety has been modified into various amide groups which is the most active area of research in this family. In this research, synthesis of various pharmacological heterocyclic amides of ibuprofen is described. All the new compounds were tested for their analgesic and anti-inflammatory activities in mice and compared with standard (Ibuprofen) and control (saline) groups. The results revealed that all the synthesized compounds (III-VI) exhibited more analgesic and antiinflammatory activities in tail immersion (as a model of acute thermal pain), formalin (as a model of acute chemical and chronic pain) and paw edema (as a model of acute inflammation) tests when compared with standard and control animals. These pharmacological activities were significant for VI compared to other new compounds (III-V) which may be concern to more effective role of morpholin for the reduction of pain and inflammation compared to other used heterocyclic amines