Determination of COX, LOX inhibition activities of some 1,2,4-triazole derivatives

COX-1, COX-2 and 5-LOX enzyme inhibition activities and intestinal absorption of six 1,2,4 triazole derivatives, which have anti-inflammatory effect potential due to their triazole ring structure, were investigated. The cytotoxic effect and enzyme inhibition activities of such 1,2,4-triazole derivative compounds on Caco-2 (colon adenocarcinoma) cells were evaluated in comparison with cyclooxygenase (COX) and lipoxygenase (LOX) selective inhibitors. PAMPA and Caco-2 transport tests were applied to determine the intestinal absorption of triazoles derivatives. All of the 1,2,4-triazole derivatives have inhibitory activity on COX and LOX enzymes, but lower inhibition than selective inhibitors. It can be considered that the enzyme inhibition activity of the B6 triazole derivative is more effective than other test substances, and its absorption is observed to be high, so the potential of this compound can be used as a candidate drug molecule. Due to the high selectivity of the COX-2 enzyme, the B3 compound also holds promise as an effective inhibitor of inflammation pathogenesis. Keywords: 1,2,4-Triazole, İnhibion, Cyclooxigenase, Lipoxygenase, Caco-2