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Synthesis of New Acetaminophen Analogs and Their Ibuprofen Conjugates as Novel Analgesic Drugs

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Pharmaceutical Chemistry Journal Aims and scope

In this research, new analogs of acetaminophen (paracetamol, I) with dimethyl and ethyl substitutions on phenyl moiety and sulfonamide modified by inserting alkylpiperazine derivatives were synthesized (II – V). Then, their conjugated compounds with ibuprofen were also synthesized (VI – IX) and the analgesic and anti-inflammatory activities of new drugs (II – IX) were evaluated in formalin tests on rats. Results indicated that the best analgesic activity was observed for compounds II and VI in diminishing chronic and VI – IX in acute thermal pain tests; in addition, compound VIII showed the best activity in diminishing inflammation. It was concluded that chemical structural binding of the potent synthesized drugs (II – V) with ibuprofen produced new superior antinociceptive and anti-inflammatory drugs (VI – IX) which could alleviate both pain and inflammation.

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Acknowledgments

This work was a research project at Islamic Azad University, Karaj Branch, Iran and authors would like to express their gratitude to it. They thank Fariba Ansari for her assistance with the pharmacological tests. They appreciate Mojtaba Chaichi, EFL educator at Safir English Language Academy, for proofreading the initial draft of this article.

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Authors and Affiliations

  1. Department of Chemistry, Faculty of Science, Karaj Branch, Islamic Azad University, Karaj, Iran

    Abbas Ahmadi, Samira Sadeghi, Neda Soleimani & Babak Nahri-Niknafs

  2. Neurophysiology Research Center, Shahed University, Tehran, Iran

    Mohsen Khalili

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  1. Abbas Ahmadi
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  2. Mohsen Khalili
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  3. Samira Sadeghi
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  4. Neda Soleimani
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Correspondence to Abbas Ahmadi.

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This research is not a part of our normal lecturing, employment, consultation and involvement. No institution will require any rights from this work too. In addition, no patent has been applied. No commercial right has been given to any company and/or institution, or it will not be done later either.

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Ahmadi, A., Khalili, M., Sadeghi, S. et al. Synthesis of New Acetaminophen Analogs and Their Ibuprofen Conjugates as Novel Analgesic Drugs. Pharm Chem J 50, 369–376 (2016). https://doi.org/10.1007/s11094-016-1454-6

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  • DOI: https://doi.org/10.1007/s11094-016-1454-6

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