학술논문
Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds
Document Type
Article
Author
Source
Subject
*LEUKOTRIENE antagonists
*HYDROLASES
*ENZYME inhibitors
*PIPERIDINE
*CRYSTALLOGRAPHY
*STRUCTURE-activity relationships
*PIPERAZINE
*DRUG development
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Language
ISSN
0960-894X
Abstract
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. [Copyright &y& Elsevier]