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, Neurophysiology Research Center, Shahed University, Tehran, Department of Chemistry, Faculty of Science, Karaj Branch, Islamic Azad University, Karaj, Department of Chemistry, Faculty of Science, Karaj Branch, Islamic Azad University, Karaj, Department of Medicinal Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran
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.
