title: Synthesis and Study of Analgesic and Anti-inflammatory Activities of Amide Derivatives of Ibuprofen.
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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Science, Islamic Azad University, P.O. Box: 31485- 313, Karaj, Iran.
authors.forename: Abbas
authors.initials: A
authors.lastname: Ahmadi
authors.affiliation: Neurophysiology Research Center, Shahed University, Tehran, Iran.
authors.forename: Mohsen
authors.initials: M
authors.lastname: Khalili
authors.affiliation: Department of Chemistry, Faculty of Science, Karaj Branch, Islamic Azad University, Karaj, Iran.
authors.forename: Zahra
authors.initials: Z
authors.lastname: Olama
authors.affiliation: Department of Chemistry, Faculty of Science, Karaj Branch, Islamic Azad University, Karaj, Iran.
authors.forename: Shirin
authors.initials: S
authors.lastname: Karami
authors.affiliation: Department of Medicinal Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran.
authors.forename: Babak
authors.initials: B
authors.lastname: Nahri-Niknafs
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007052:Ibuprofen / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007052:Ibuprofen
keywords: Analgesic; NSAIDs; anti-inflammatory; ibuprofen; pharmacological heterocyclic amides