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Review
. 2025 Sep;17(18):2251-2279.
doi: 10.1080/17568919.2025.2557184. Epub 2025 Sep 7.

Synthetic approaches and therapeutic potential of thiophene derivatives as COX and LOX inhibitors

Affiliations
Review

Synthetic approaches and therapeutic potential of thiophene derivatives as COX and LOX inhibitors

Suman Lata et al. Future Med Chem. 2025 Sep.

Abstract

Thiophene derivatives have gained considerable interest lately due to their potential as anti-inflammatory agents. Their structural flexibility and capacity to interact with key enzymes involved in inflammatory processes position them as promising candidates for drug development. This review provides a comprehensive overview of the latest research, focusing on the synthesis and therapeutic evaluation of thiophene-based compounds that act as inhibitors of cyclooxygenase (COX) and lipoxygenase (LOX) enzymes. It discusses synthetic methodologies, structure-activity relationship (SAR) patterns, and the biological activities of these compounds, with a particular focus on those demonstrating dual COX/LOX inhibition. By consolidating recent findings, the review aims to enhance ongoing efforts to develop more effective and safer anti-inflammatory agents that utilize thiophene as a core scaffold. By summarizing research data from 2018 to 2025 using databases such as Google Scholar, Web of Science, PubMed, and Scopus, this review article aims to contribute to the development of novel lead molecules, offer promising avenues for future drug discovery, and therapeutic innovation in inflammation-related diseases.

Keywords: Cyclooxygenase; anti-oxidants; enzyme inhibitors; inflammation; lipoxygenase; thiophene derivatives.

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Conflict of interest statement

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

References

    1. Khalil NA, Ahmed EM, Tharwat T, et al. Nsaids between past and present; a long journey towards an ideal COX-2 inhibitor lead. RSC Adv. 2024;14(42):30647–30661. doi: 10.1039/D4RA04686B - DOI - PMC - PubMed
    1. Kumar D, Verma D, Abbot V.. A review on pharmaceutical, pharmacological and chemical aspects of serratiopeptidase as anti-inflammatory agent. Mater Today Proc [Internet]. 2023. [cited 2025 Mar 21]. doi: 10.1016/j.matpr.2023.01.256 - DOI
    1. Saraf P, Bhardwaj B, Verma A, et al. Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity. RSC Med Chem. 2025;16(1):200–220. doi: 10.1039/D4MD00471J - DOI - PMC - PubMed
    1. Li B, Gao Q, Wu Y, et al. Broad-spectrum anti-inflammatory and antioxidant therapy of inflammatory-storm actuated diseases via programmable self-derived cryo-dead neutrophils. Chem Eng J. 2025;507:160643. doi: 10.1016/j.cej.2025.160643 - DOI
    1. Cifuentes M, Verdejo HE, Castro PF, et al. Low-grade chronic inflammation: a shared mechanism for chronic diseases. Physiology. 2025;40(1):4–25. doi: 10.1152/physiol.00021.2024 - DOI - PubMed

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