Synthesis of some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activity
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, cilt.197, sa.11, ss.1123-1135, 2022 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Derleme
- Cilt numarası: 197 Sayı: 11
- Basım Tarihi: 2022
- Doi Numarası: 10.1080/10426507.2022.2062756
- Dergi Adı: PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core
- Sayfa Sayıları: ss.1123-1135
- Anahtar Kelimeler: 1, 2, 4-Triazine, diaryl heterocylics, thiazole, cyclooxygenase inhibition, COX-2 inhibitor, anti-inflammatory, molecular docking, ANTIINFLAMMATORY DRUGS, BIOLOGICAL EVALUATION, ITAZIGREL, DOCKING, ASPIRIN, EVENTS
- Anadolu Üniversitesi Adresli: Evet
Özet
Within this study, 20 2-[(5,6-diaryl-1,2,4-triazin-3-yl)thio]-N-(benzo/thiazol-2-yl)acetamide derivatives (4a-4t) were synthesized and COX inhibitory activities of the compounds were investigated. Compounds 4k-4o, which have a 4-methoxyphenyl group within their structures, showed strong inhibitory activity on COX-2 enzyme, even compound 4k, namely 2-{[5,6-bis(4-methoxyphenyl)-1,2,4-triazin-3-yl]thio}-N-(thiazol-2-yl)acetamide exhibited higher selectivity on this enzyme (IC50:3.06 mu M). Molecular docking studies were performed for compound 4k on COX-1 and COX-2 enzymes and the results were found to support the molecule's COX-2 selectivity.