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New Diclofenac Derivatives as Anti-Microbial, Anti-Inflammatory Agents: Design, Synthesis, Biological Screening, and Molecular Docking Study

Abstract

Diclofenac is considered one of the best drugs used as anti-inflammatory agent, so in the present work new diclofenac derivatives containing bioactive moieties, such as triazole, oxadiazole, and thiadiazol, were synthesized. The structures of the new compounds were established based on spectral and elemental analysis. The new synthesized compounds were tested against anti-inflammatory agents and exhibited high activity as expected. The binding position of new diclofenac derivatives toward Cox-1 and Cox-2 enzymes was proved by molecular docking. Also, some of the new compounds were tested against bacteria and displayed high activity.

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ACKNOWLEDGMENTS

The authors are very grateful to Mr. Abdelreheem Abdelfattah Saddik, assistant lecturer, Department of Chemistry, Faculty of Science, Assiut University for your contributions in the study of some of my samples (13C, 1H-NMR) at Materials Science and Technology Department, National Chiao Tung University, Taiwan. I also thank Dr. Mostafa Ahmed, assistant professor, Department of Chemistry, Faculty of Science, New Valley University for his constant efforts and his view Constructive during the course of the preparation of the manuscript We also take this opportunity to thank Dr. Omneya Ahmed Ibrahim Faculty of Pharmacy, Assiut University, particularly in the field of molecular docking research, with many thanks.

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Correspondence to Mahmoud S. Tolba.

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This article does not contain any studies involving human participants performed by any of the authors. All procedures performed in studies involving animals were in accordance with the ethical standards of the institution or practice at which the studies were conducted.

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The authors declare that they have no conflicting financial interest.

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Mahmoud M. Hamed, El-Dean, A.M., Abdel-Mohsen, S.A. et al. New Diclofenac Derivatives as Anti-Microbial, Anti-Inflammatory Agents: Design, Synthesis, Biological Screening, and Molecular Docking Study. Russ J Bioorg Chem 47, 208–220 (2021). https://doi.org/10.1134/S1068162021010088

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Keywords:

  • diclofenac derivatives
  • anti-microbial
  • anti-inflammatory
  • molecular docking
  • COX enzymes