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Lipoxygenases (LOXs) are a group of enzymes that catalyze the oxidation of polyunsaturated fatty acids and initiate the biosynthesis of secondary metabolites that are involved to control inflammation. In search of new and more potent LOX inhibitors, a series of new 3-(5-(4-chlorophenyl)-4-(2-furylmethyl)-1,2,4-triazole hybrids was prepared and screened for its LOX inhibitory potential. 4-Chlorobenzoic acid ( a ) was metamorphosed into  N -furfuryl-5-(4-chlorophenyl)-4-(2-furylmethyl)-1,2,4-triazole ( 4 ) via intermediates like benzoate ( 1 ), hydrazide ( 2 ) and semicarbazide ( 3 ). Finally, triazole ( 4 ) was fused with propionamides ( 6a–o ) and transformed it into the aimed derivatives ( 7a–o ). The structural interpretations of the prepared derivatives ( 7a–o ) were accomplished via FTIR,  1 H-,  13 C-NMR spectroscopy, EI-MS and HR-EI-MS spectrometry. The inhibitory potency of the compounds against soybean 15-LOX was determined by  in vitro  assay using chemiluminescence method. Compounds  7a  and  7f  exhibited potent LOX inhibitory profiles with IC 50  21.83 ± 0.56 and 25.72 ± 0.51 µM, whereas  7d  and  7e  showed comparable inhibitory potential with IC 50  values of 34.52 ± 0.39 and 39.12 ± 0.46 µM, respectively. Compounds  7a ,  7f ,  7d  and  7e  exhibited 65.58 ± 1.4%, 54.72 ± 1.3%, 58.52 ± 1.2% and 63.56 ± 1.4% blood mononuclear cells viability, respectively. Density functional theory and molecular docking studies further strengthened the studies of the synthesized compounds and these derivatives perceived to be potential ‘lead’ compounds in drug discovery as anti-LOX. Communicated by Ramaswamy H. Sarma

journal of biomolecular structure and dynamics

Targeting new N-furfurylated 4-chlorophenyl-1,2,4-triazolepropionamide hybrids as potential 15-lipoxygenase inhibitors supported with  in vitro  and  in silico  studies