Metil sülfonil farmakofor taşıyan yeni bileşiklerin sentezive seçici COX-2 inhibitör aktivitelerinin değerlendirilmesi

Cyclooxygenase, also known as prostaglandin H2 synthase (PGH2), is one of the most important enzymes in pharmacology because inhibition of COX is the mechanism of action of most nonsteroidal anti-inflammatory drugs. In this study, ten thiazole derivative compounds had synthesized. The analysis of the obtained compounds was performed by 1H NMR (Proton Nuclear Magnetic Resonance) and 13C NMR (Carbon-13 Nuclear Magnetic Resonance) methods. By this method, the obtained compounds could be elucidated. The inhibitory effect of the obtained compounds on cyclooxygenase (COX) enzymes investigated. The encoded compounds 5a, 5b, and 5c were found to be the most potent compared to the reference compounds ibuprofen, celecoxib, and nimesulide. The inhibitory activity of 5a, 5b, and 5c is approximate, but the 5a derivative proved to be the most active in the series with an IC50 value of 0.180 ± 0.002 μM. The most potent COXs inhibitor was 5a, which further investigated for its potential binding mode by molecular docking study. Compound 5a found to be localized at the active site of the enzyme, similar to celecoxib, which has a remarkable effect on COXs enzymes.