Ibuprofen amino acid derivatives: synthesis, docking and biological studies

Document Type : Original Article

Authors

1 Chemistry Department, Faculty of Science, Al-Azhar University (Boys' Branch), Nasr City, Cairo, Egypt

2 Organometallic and Organometalloid Chemistry, Chemical Industries Research Institute, National Research Centre

3 Department of Pharmacology, Toxicology and Biochemistry, Future University in Egypt, Cairo, Egypt.

4 Chemistry Department, Faculty of Science, Al-Azhar University (Boys' Branch), Nasr City, Cairo, Egypt

Abstract

This work aimed to synthesize new Ibuprofen amino acid derivatives as safe non-steroidal anti-inflammatory drugs (NSAIDs). The structures of the synthesized compounds have been determined using various spectral data. For tested compounds , molecular docking was performed into the cyclooxygnase-2 (COX-2) active site. The lowest root-mean-square deviation of atomic positions (RMSD) pose has been chosen for the binding affinity discussion. Docking protocol revealed that the binding interaction increased by the presence of hydrazide fragment in the tested compounds. Passed compounds through docking profile were examined for their anti -inflammatory and analgesic activities. Using a carrageenan-induced mouse model of hind paw edoema, we investigated the potential anti-inflammatory efficacy of the synthetic compounds in comparison to their parent molecule, ibuprofen. In addition to assessing the antinociceptive and ulcerogenic properties of the synthesized compounds

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History

  • Receive Date: 30 March 2022
  • Revise Date: 02 June 2022
  • Accept Date: 04 June 2022

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