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

Lucas SD, Gonçalves LM, Carvalho LA, Correia HF, Da Costa EM, Guedes RA, Moreira R, Guedes RC.

J Med Chem. 2013 Dec 12;56(23):9802-6.

Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa , Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.

Abstract

Human neutrophil elastase (HNE) is an attractive target for treating chronic and acute inflammatory lung diseases. An optimization campaign of thekojic acid scaffold to develop new potent Human neutrophil elastase 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.

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Optimization of O3-Acyl Kojic Acid Derivatives as Potent and Selective Human Neutrophil Elastase Inhibitors- Global Medical Discovery