Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds

Novel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA4 hydrolase (LTA4H). Most potent compounds showed good potency in both enzymatic and functional human whole blood assay. Crystallography studies further confirmed observed structure–activity relationship and LTA4H binding mode for analogs from the piperidine series.

Graphical abstractNovel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA4 hydrolase (LTA4H). Most potent compounds showed good potency in both enzymatic and functional human whole blood assay. Crystallography studies further confirmed observed structure–activity relationship and LTA4H binding mode for analogs from the piperidine series.Figure optionsDownload full-size imageDownload as PowerPoint slide