Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A4 hydrolase aminopeptidase inhibitors

Novel 1,2,3-triazin-4-one derivatives incorporating 4-thiazolidinone moieties were designed and synthesized. Many of them exhibited moderate to good inhibitory activity against LTA4H aminopeptidase at 10 μmol/L, the compound IV-16 with best bioactivity was also tested the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA4H enzyme by molecular docking was studied. It indicated that 1,2,3-triazin-4-one was a very promising scaffold to study further.