Structures of zileuton, representative dual COX-2/5-LOX inhibi-tors and lead compound 1.

December 26, 2023

• Title:

  Structures of zileuton, representative dual COX-2/5-LOX inhibi-tors and lead compound 1.

• Image Source:

  Discovery of potential anti-inflammatory drugs: Diaryl-1,2,4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase

• Mark:

  Fig. 1

• Associated context:

  Various structures of dual COX/5-LOX inhibitors have been  developed, and the representatives are tepoxalin, licofelone  and ZD-2138 (Fig. 1). Tepoxalin has been approved for the  treatment of OA in dogs in the United States and the European  Union. Licofelone is a promising dual COX/5-LOX inhibi-  tor. The results of Phase III clinical trials suggested that lico-  felone is effective in the treatment of OA with reduced  gastrointestinal (GI) toxicity and thromboembolic risk compared  to traditional NSAIDs and COX-2 selective inhibitors.  Besides the above-mentioned dual inhibitors, natural products  are also an important source of dual inhibitors, among  them, flavocoxid (Limbrel®) has been launched to market as an  FDA-regulated medical food for the clinical dietary management  of the metabolic aspects of OA in the United States.