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Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds |
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| Authors: | Vincent Sandanayaka Bjorn Mamat Nikhil Bhagat Louis Bedell Gudrun Halldorsdottir Heida Sigthorsdottir Þorkell Andrésson Alex Kiselyov Mark Gurney Jasbir Singh |
| Affiliation: | 1. Medicinal Chemistry Department, deCODE Chemistry, Inc. 2501 Davey Road, Woodridge, IL 60517, United States;2. deCODE Genetics, Inc., Sturlugata 8, IS-101, ReykjaVik, Iceland |
| Abstract: | 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. |
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