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1. Optimization of O3-Acyl Kojic Acid Derivatives as Potent and SelectiveHuman Neutrophil Elastase Inhibitors.

Author

Lucas, Susana D., Gonçalves, Lídia M., Carvalho, Luís A.R., Correia, Henrique F., Da Costa, Eduardo M. R., Guedes, Romina A., Moreira, Rui, and Guedes, Rita C.

Subjects
*LEUCOCYTE elastase, *ACYL group, *MATHEMATICAL optimization, *INFLAMMATION, *LUNG disease treatment, *CELL-mediated cytotoxicity
Abstract

Humanneutrophil elastase (HNE) is an attractive target for treating chronicand acute inflammatory lung diseases. An optimization campaign ofthe kojic acid scaffold to develop new potent HNE inhibitors is reported. O3-Pivaloyl derivatives were shown to be themost potent inhibitors with IC5ovalues down to 80 nM.These compounds presented excellent selectivity and cytotoxicity profileswith suitable ligand efficiency. [ABSTRACT FROM AUTHOR]

Published
2013
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