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2000
Volume 22, Issue 4
  • ISSN: 1573-4072
  • E-ISSN: 1875-6646

Abstract

Inflammation is a defense response of the body that occurs due to injury or bacterial infection, allergens, autoimmune disease, . PGs (Prostaglandins), leukotrienes, histamine, BK (bradykinin), and ILs (interleukins) are the main chemical mediators involved in inflammation and its associated diseases. The major pathway is the formation of arachidonic acid connected with the cyclooxygenase (COX) enzyme and 5-lipoxygenase enzyme in the synthesis of prostaglandins and leukotrienes, respectively. Anti-inflammatory agents primarily target cyclooxygenases (COX 1 and 2), phospholipase A2 (PLA2), and lipoxygenase (LOX). Some major patents are covered in this review article. This review also covers the journey of anti-inflammatory activities of tetrahydrocarbazole structure-based derivatives from 1976 till date. Researchers around the world have designed and synthesized novel tetrahydrocarbazoles based on the indomethacin structure under the NSAIDs category using Structure-based Drug Design (SBBD), which have displayed significant and anti-inflammatory activities. Tetrahydrocarbazole structures linked with other potential pharmacophores, including chalconyl, isoxazolinyl, pyrazolinyl and diazoles, have also been evaluated for anti-inflammatory activities. Major substitutions, either halogen or electron-releasing groups on tetrahydrocarbazole structure, play a crucial role in its anti-inflammatory activities. Moreover, reported N-9 substituted tetrahydrocarbazoles have been observed to display significant anti-inflammatory activities. These THCz derivatives target the COX-2 enzyme, which plays a crucial role in inflammation and also in cancer. Lastly, this review encourages scientists to design and synthesize novel compounds based on tetrahydrocarbazole structure to address inflammation and its associated diseases.

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Anti-inflammatory Activities of Tetrahydrocarbazoles (THCz): A Review
Curr. Bioact. Compd. 22, E15734072349578 (2026); https://doi.org/10.2174/0115734072349578250312005557
/content/journals/cbc/10.2174/0115734072349578250312005557
/content/journals/cbc/10.2174/0115734072349578250312005557
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  • Article Type:     Review Article
Keyword(s): 1,2,3,4-tetrahydrocarbazole (THC); anti-inflammatory agents; Arachidonic acid (AA); autoimmune disease; cyclooxygenase enzyme (COX-1 & COX-2); phospholipase A2 (PLA2)

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