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Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.

Journal of medicinal chemistry (2013-11-15)
Susana D Lucas, Lídia M Gonçalves, Luís A R Carvalho, Henrique F Correia, Eduardo M R Da Costa, Romina A Guedes, Rui Moreira, Rita C Guedes
ABSTRACT

Human neutrophil elastase (HNE) is an attractive target for treating chronic and acute inflammatory lung diseases. An optimization campaign of the kojic acid scaffold to develop new potent HNE inhibitors is reported. O3-Pivaloyl derivatives were shown to be the most potent inhibitors with IC5o values down to 80 nM. These compounds presented excellent selectivity and cytotoxicity profiles with suitable ligand efficiency.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Kojic acid
Sigma-Aldrich
Elastase from human leukocytes, lyophilized powder, ≥50 units/mg protein (Bradford)