4.7 Article

Antioxidant Activity, Molecular Docking, Quantum Studies and In Vivo Antinociceptive Activity of Sulfonamides Derived From Carvacrol

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FRONTIERS IN PHARMACOLOGY
卷 12, 期 -, 页码 -

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FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2021.788850

关键词

sulfonamides; pain; carvacrol; molecular modeling; antioxidant

资金

  1. National Council for Scientific and Technological Development (CNPq)
  2. Coordination for the Improvement of Higher Education Personnel (CAPES) [001]
  3. Sao Paulo Research Foundation (FAPESP CIBFar grant) [2013/07600-3]

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The study reported the synthesis and activities of sulfonamides derived from carvacrol, showing promising antioxidant properties, with one derivative demonstrating excellent antinociceptive and antiedematogenic activities. The mechanism underlying the pain relief effects of these compounds remains partially elucidated, but the study suggests that the antinociceptive activity may be partially mediated by antagonism of glutamatergic signaling. Compound S1 showed promising efficacy, making it an interesting starting point for the development of new compounds for the treatment of pain and inflammation.
The synthesis and antioxidant, antinociceptive and antiedematogenic activities of sulfonamides derived from carvacrol-a druglike natural product-are reported. The compounds showed promising antioxidant activity, and sulfonamide derived from morpholine (S1) demonstrated excellent antinociceptive and antiedematogenic activities, with no sedation or motor impairment. The mechanism that underlies the carvacrol and derived sulfonamides' relieving effects on pain has not yet been fully elucidated, however, this study shows that the antinociceptive activity can be partially mediated by the antagonism of glutamatergic signaling. Compound S1 presented promising efficacy and was predicted to have an appropriate medicinal chemistry profile. Thus, derivative S1 is an interesting starting point for the design of new leads for the treatment of pain and associated inflammation and prooxidative conditions.

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