Anti-inflammation and antimalarial profile of 5-pyridin-2-yl-1H-[1,2,4]triazole-3-carboxylic acid ethyl ester as a low molecular intermediate for hybrid drug synthesis

A novel 1,2,4-triazole intermediate 5-pyridin-2-yl-1H-[1,2,4]triazole-3-carboxylic acid ethyl ester was prepared by the reaction of N’-aminopiridyne-2-carboximidamine and an excess monoethyl oxalyl chloride and screened for biological activities. The compound was structurally characterized by nuclear magnetic resonance spectroscopy, elemental analysis, infrared spectroscopy, and single-crystal X-ray diffraction. Bioassays indicated that the compound exhibits potent anti-inflammation activity in vitro. An egg albumin denaturation assay to assess the anti-inflammatory effect of the synthesized compound showed a significant inhibition of protein with a maximum inhibition of 71.1% at the highest tested concentration (1000 µg/mL) compared to 81.3% for Aspirin as standard drug. The antimalarial activity on the 3D7 P. falciparum strain was determined to be IC₅₀ 176 µM and was obtained prior to connection with pharmacophoric groups.