Title:Synthesis and Study of Analgesic and Anti-inflammatory Activities of Amide Derivatives of Ibuprofen
Volume: 17
Issue: 9
Author(s): Abbas Ahmadi*, Mohsen Khalili, Zahra Olama, Shirin Karami and Babak Nahri-Niknafs
Affiliation:
- Department of Medicinal Chemistry, Faculty of Science, Islamic Azad University, P.O. Box: 31485- 313, Karaj,Iran
Keywords:
Analgesic, anti-inflammatory, ibuprofen, NSAIDs, pharmacological heterocyclic amides.
Abstract: 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.
Objective: 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.
Method: 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.
Results & Conclusion: The results revealed that all the synthesized compounds (III-VI) exhibited more
analgesic and anti-inflammatory 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.
