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. 2010 May 1;20(9):2851-4.
doi: 10.1016/j.bmcl.2010.03.047. Epub 2010 Mar 12.

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

Vincent Sandanayaka  1 , Bjorn Mamat, Nikhil Bhagat, Louis Bedell, Gudrun Halldorsdottir, Heida Sigthorsdottir, Thorkell Andrésson, Alex Kiselyov, Mark Gurney, Jasbir Singh
Affiliations

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

Vincent Sandanayaka et al. Bioorg Med Chem Lett. .

Abstract

Novel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA(4) hydrolase (LTA(4)H). Most potent compounds showed good potency in both enzymatic and functional human whole blood assay. Crystallography studies further confirmed observed structure-activity relationship and LTA(4)H binding mode for analogs from the piperidine series.

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